Ronald T. Borchardt

Ronald T. Borchardt's AcademicInfluence.com Rankings

Ronald T. Borchardt

Chemistry

#1577

World Rank

#2335

Historical Rank

Organic Chemistry

#200

World Rank

#252

Historical Rank

chemistry Degrees

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Chemistry

Ronald T. Borchardt's Degrees

PhD Pharmaceutical Chemistry University of Kansas
Masters Pharmaceutical Chemistry University of Kansas
Bachelors Pharmacy University of Kansas

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Ronald T. Borchardt's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. (1989) (2179)
Stability of Protein Pharmaceuticals (1989) (831)
Enzymes involved in the bioconversion of ester-based prodrugs. (2006) (319)
VEGF increases BMEC monolayer permeability by affecting occludin expression and tight junction assembly. (2001) (275)
Intestinal Drug Absorption and Metabolism in Cell Cultures: Caco-2 and Beyond (1997) (257)
Chemical instability of protein pharmaceuticals: Mechanisms of oxidation and strategies for stabilization. (1995) (251)
The Use of Surfactants to Enhance the Permeability of Peptides Through Caco-2 Cells by Inhibition of an Apically Polarized Efflux System (1996) (245)
A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. (2002) (223)
Formulation considerations for proteins susceptible to asparagine deamidation and aspartate isomerization. (2006) (214)
In vitro systems for studying intestinal drug absorption (1995) (183)
Bovine Brain Microvessel Endothelial Cell Monolayers as a Model System for the Blood‐Brain Barrier a (1987) (183)
Paracellular diffusion in Caco-2 cell monolayers: effect of perturbation on the transport of hydrophilic compounds that vary in charge and size. (1997) (182)
S-adenosyl-L-homocysteine hydrolase as a target for antiviral chemotherapy. (1991) (177)
Structural requirements for intestinal absorption of peptide drugs (1996) (175)
Neplanocin A. A potent inhibitor of S-adenosylhomocysteine hydrolase and of vaccinia virus multiplication in mouse L929 cells. (1984) (174)
Chemical Pathways of Peptide Degradation. II. Kinetics of Deamidation of an Asparaginyl Residue in a Model Hexapeptide (1990) (173)
Transport of a large neutral amino acid (phenylalanine) in a human intestinal epithelial cell line: Caco-2. (1990) (163)
How structural features influence the biomembrane permeability of peptides. (1996) (162)
Are MDCK Cells Transfected with the Human MDR1 Gene a Good Model of the Human Intestinal Mucosa? (2002) (162)
S-Adenosyl-L-methionine-dependent macromolecule methyltransferases: potential targets for the design of chemotherapeutic agents. (1980) (152)
The Use of Cultured Epithelial and Endothelial Cells for Drug Transport and Metabolism Studies (1990) (150)
Effects of poly(ethylene glycol) on efflux transporter activity in Caco-2 cell monolayers. (2002) (148)
Sinefungin, a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. (1978) (142)
Mechanistic roles of neutral surfactants on concurrent polarized and passive membrane transport of a model peptide in Caco-2 cells. (1997) (141)
Transport of bile acids in a human intestinal epithelial cell line, Caco-2. (1990) (140)
Effect of Size and Charge on the Passive Diffusion of Peptides Across Caco-2 Cell Monolayers via the Paracellular Pathway (1997) (138)
Aggregation and precipitation of human relaxin induced by metal-catalyzed oxidation. (1995) (132)
Structure and function of S-adenosylhomocysteine hydrolase (2007) (131)
Catechol O-methyltransferase. 5. Structure-activity relationships for inhibition by flavonoids. (1975) (129)
Models for Assessing Drug Absorption and Metabolism (1996) (125)
Structure determination of selenomethionyl S-adenosylhomocysteine hydrolase using data at a single wavelength (1998) (121)
Hydrogen Bonding Potential as a Determinant of the in Vitro and in Situ Blood–Brain Barrier Permeability of Peptides (1994) (120)
Biological Methylation and Drug Design (1986) (120)
Characteristics of the Large Neutral Amino Acid Transport System of Bovine Brain Microvessel Endothelial Cell Monolayers (1986) (120)
Vascular endothelial growth factor affects permeability of brain microvessel endothelial cells in vitro. (1996) (114)
[34] Catechol O-methyltransferase (1981) (113)
Broad-spectrum antiviral activities of neplanocin A, 3-deazaneplanocin A, and their 5'-nor derivatives (1989) (112)
Chemical Pathways of Peptide Degradation. III. Effect of Primary Sequence on the Pathways of Deamidation of Asparaginyl Residues in Hexapeptides (1990) (112)
Aspartate isomerization in the complementarity-determining regions of two closely related monoclonal antibodies. (2007) (107)
Chemical Pathways of Peptide Degradation. IV. Pathways, Kinetics, and Mechanism of Degradation of an Aspartyl Residue in a Model Hexapeptide (2004) (107)
Are MDCK Cells Transfected with the Human MRP2 Gene a Good Model of the Human Intestinal Mucosa? (2004) (106)
Summary workshop report: biopharmaceutics classification system--implementation challenges and extension opportunities. (2004) (105)
Characterization of an In Vitro Blood–Brain Barrier Model System for Studying Drug Transport and Metabolism (1986) (104)
.alpha.-Deuterium and carbon-13 isotope effects for methyl transfer catalyzed by catechol O-methyltransferase. SN2-like transition state (1979) (102)
Effects of reducing sugars on the chemical stability of human relaxin in the lyophilized state. (1996) (99)
Biochemistry of S-Adenosylmethionine and Related Compounds (1982) (98)
Prodrug strategies based on intramolecular cyclization reactions. (1997) (95)
Studies of inhibition of rat spermidine synthase and spermine synthase. (1980) (93)
Composition and evolution of the lunar crust in the Descartes highlands, Apollo 16. (1985) (93)
Characterization of the Unstirred Water Layer in Caco-2 Cell Monolayers Using a Novel Diffusion Apparatus (1991) (92)
Effects of adenosine dialdehyde on S-adenosylhomocysteine hydrolase and S-adenosylmethionine-dependent transmethylations in mouse L929 cells. (1984) (90)
Effects of inhibitors of spermidine and spermine synthesis on polyamine concentrations and growth of transformed mouse fibroblasts. (1981) (90)
Catechol O-methyltransferase. (1981) (89)
A Functional Assay for Quantitation of the Apparent Affinities of Ligands of P-Glycoprotein in Caco-2 Cells (2001) (82)
Synthesis of analogs of neplanocin A: utilization of optically active dihydroxycyclopentenones derived from carbohydrates (1987) (81)
Hexose uptake in primary cultures of bovine brain microvessel endothelial cells. I. Basic characteristics and effects of D-glucose and insulin. (1991) (80)
Application of cultured endothelial cells of the brain microvasculature in the study of the blood-brain barrier (1992) (79)
Efficient enantioselective syntheses of carbocyclic nucleoside and prostaglandin synthons (1990) (79)
Kinetics of diketopiperazine formation using model peptides. (1998) (78)
Pharmaceutical profiling in drug discovery for lead selection (2004) (78)
Rational approaches to the design of antiviral agents based on S-adenosyl-L-homocysteine hydrolase as a molecular target. (1992) (78)
Catalytic strategy of S-adenosyl-L-homocysteine hydrolase: transition-state stabilization and the avoidance of abortive reactions. (2003) (73)
The effect of verapamil on the transport of peptides across the blood-brain barrier in rats: kinetic evidence for an apically polarized efflux mechanism. (1995) (73)
Sinefungin, a potent inhibitor or S-adenosylmethionine: protein O-methyltransferase. (1979) (72)
Chiral instability at sulfur of S-adenosylmethionine. (1983) (71)
Stereopopulation control. II. Rate enhancement of intramolecular nucleophilic displacement. (1972) (71)
Chemical stability of peptides in polymers. 1. Effect of water on peptide deamidation in poly(vinyl alcohol) and poly(vinyl pyrrolidone) matrixes. (1999) (71)
Catecholamine‐Metabolizing Enzymes of Bovine Brain Microvessel Endothelial Cell Monolayers (1986) (69)
Demonstration and structural comparison of receptors for insulin-like growth factor-I and -II (IGF-I and -II) in brain and blood-brain barrier. (1987) (68)
Catechol O-methyltransferase. 1. Kinetics of tropolone inhibition. (1973) (68)
Effect of 'pH' on the rate of asparagine deamidation in polymeric formulations: 'pH'-rate profile. (2001) (67)
Chemical Pathways of Peptide Degradation. VI. Effect of the Primary Sequence on the Pathways of Degradation of Aspartyl Residues in Model Hexapeptides (1994) (67)
Brain microvessel endothelial cell culture systems. (1996) (67)
A Kinetic Evaluation of the Absorption, Efflux, and Metabolism of Verapamil in the Autoperfused Rat Jejunum (2003) (67)
Silica gel-assisted reduction of nitrostyrenes to 2-aryl-1-nitroalkanes with sodium borohydride (1983) (66)
Directed Drug Delivery (1985) (66)
Binding of epidermal growth factor by human colon carcinoma cell (Caco-2) monolayers. (1989) (65)
Bidirectional transport of rhodamine 123 and Hoechst 33342, fluorescence probes of the binding sites on P-glycoprotein, across MDCK-MDR1 cell monolayers. (2004) (65)
Inhibition of Newcastle disease virion messenger RNA (guanine-7-)-methyltransferase by analogues of S-adenosylhomocysteine. (1977) (65)
The Mass Spectrometry of Helical Unfolding in Peptides (1994) (64)
Transport of a large neutral amino acid in a human intestinal epithelial cell line (Caco-2): uptake and efflux of phenylalanine. (1992) (64)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 1. Modification of the amino acid portion of S-adenosylhomocysteine. (1974) (64)
The lactonization of 2'-hydroxyhydrocinnamic acid amides: a potential prodrug for amines (1990) (64)
Chemical stability of peptides in polymers. 2. Discriminating between solvent and plasticizing effects of water on peptide deamidation in poly(vinylpyrrolidone). (1999) (64)
Quantitative Approaches to Delineate Passive Transport Mechanisms in Cell Culture Monolayers (1999) (63)
Stereopopulation control. 3. Facilitation of intramolecular conjugate addition of the carboxyl group. (1972) (63)
9-(trans-2',trans-3'-Dihydroxycyclopent-4'-enyl)-adenine and -3-deazaadenine: analogs of neplanocin A which retain potent antiviral activity but exhibit reduced cytotoxicity (1987) (63)
Blood-brain barrier: transport studies in isolated brain capillaries and in cultured brain endothelial cells. (1991) (62)
A Correlation Between the Permeability Characteristics of a Series of Peptides Using an in Vitro Cell Culture Model (Caco-2) and Those Using an in Situ Perfused Rat Ileum Model of the Intestinal Mucosa (1993) (62)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 11. Molecular dissections of neplanocin A as potential inhibitors of S-adenosylhomocysteine hydrolase. (1988) (61)
Optimizing oral absorption of peptides using prodrug strategies. (1999) (60)
Identification and distribution of insulin receptors on cultured bovine brain microvessel endothelial cells: Possible function in insulin processing in the blood–brain barrier (1994) (57)
4'-modified analogues of aristeromycin and neplanocin A: synthesis and inhibitory activity toward S-adenosyl-L-homocysteine hydrolase. (1992) (57)
Effect of Restricted Conformational Flexibility on the Permeation of Model Hexapeptides Across Caco-2 Cell Monolayers (1997) (57)
The Effect of β-Turn Structure on the Passive Diffusion of Peptides Across Caco-2 Cell Monolayers (1997) (56)
Effects of S-adenosylhomocysteine analogues on vaccinia viral messenger ribonucleic acid synthesis and methylation. (1982) (55)
Synthesis of analogs of L-valacyclovir and determination of their substrate activity for the oligopeptide transporter in Caco-2 cells. (2002) (53)
Prodrug strategies to enhance the intestinal absorption of peptides (1997) (53)
Synthesis and evaluation of the physicochemical properties of esterase-sensitive cyclic prodrugs of opioid peptides using coumarinic acid and phenylpropionic acid linkers. (1999) (52)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 4. Further modifications of the amino and base portions of S-adenosyl-L-homocysteine. (1976) (51)
Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells. (1991) (51)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 2. Modification of the base portion of S-adenosylhomocysteine (1974) (51)
Design and synthesis of S-adenosylhomocysteine hydrolase inhibitors as broad-spectrum antiviral agents (1996) (51)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 5. Role of the asymmetric sulfonium pole in the enzymatic binding of S-adenosyl-L-methionine. (1976) (50)
Relationship of octanol/buffer and octanol/water partition coefficients to transcellular diffusion across brain microvessel endothelial cell monolayers (1986) (50)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 3. Modifications of the sugar portion of S-adenosylhomocysteine. (1975) (49)
The effect of conformation on the membrane permeation of coumarinic acid- and phenylpropionic acid-based cyclic prodrugs of opioid peptides. (1999) (49)
Mechanism of inactivation of S-adenosylhomocysteine hydrolase by (Z)-4',5'-didehydro-5'-deoxy-5'-fluoroadenosine. (1993) (49)
Evaluation of the Permeation Characteristics of a Model Opioid Peptide, H-Tyr-d-Ala-Gly-Phe-d-Leu-OH (DADLE), and Its Cyclic Prodrugs across the Blood-Brain Barrier Using an In Situ Perfused Rat Brain Model (2002) (49)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 6. Structural modifications of S-adenosylmethionine. (1976) (49)
Brain uptake of drugs : the influence of chemical and biological factors (1992) (49)
Delta-sleep-inducing peptide: solution conformational studies of a membrane-permeable peptide. (1994) (48)
Synthesis of a Novel Esterase-Sensitive Cyclic Prodrug System for Peptides That Utilizes a “Trimethyl Lock”-Facilitated Lactonization Reaction (1997) (48)
The purification and kinetic properties of liver microsomal-catechol-o-methyltransferase. (1974) (47)
Absorption barriers in the rat intestinal mucosa. 3: Effects of polyethoxylated solubilizing agents on drug permeation and metabolism. (2010) (47)
Enantiospecific syntheses of aristeromycin and neplanocin A (1990) (46)
Carrier-Mediated Transport of Baclofen Across Monolayers of Bovine Brain Endothelial Cells in Primary Culture (1988) (46)
Nucleic acid related compounds. 84. Synthesis of 6'-(E and Z)-halohomovinyl derivatives of adenosine, inactivation of S-adenosyl-L-homocysteine hydrolase, and correlation of anticancer and antiviral potencies with enzyme inhibition. (1994) (46)
Chemical Pathways of Peptide Degradation. VII. Solid State Chemical Instability of an Aspartyl Residue in a Model Hexapeptide (1994) (44)
A convenient preparation of S-adenosylhomocysteine and related compounds. (1976) (43)
Pancreatic exocrine secretion is blocked by inhibitors of methylation. (1997) (43)
SYNTHESIS OF A NOVEL ESTERASE-SENSITIVE CYCLIC PRODRUG OF A HEXAPEPTIDE USING AN (ACYLOXY)ALKOXY PROMOIETY (1997) (43)
Isolation and Characterization of Caco-2 Subclones Expressing High Levels of Multidrug Resistance Protein Efflux Transporter (2003) (42)
Relationship between intracellular concentration of S-adenosylhomocysteine and inhibition of vaccinia virus replication and inhibition of murine L-929 cell growth (1989) (42)
In Vitro Stability and In Vivo Pharmacokinetic Studies of a Model Opioid Peptide, H-Tyr-d-Ala-Gly-Phe-d-Leu-OH (DADLE), and Its Cyclic Prodrugs (2002) (41)
The Application of Bovine Brain Microvessel Endothelial-Cell Monolayers Grown onto Polycarbonate Membranes in Vitro to Estimate the Potential Permeability of Solutes Through the Blood–Brain Barrier (1989) (41)
A single mutation at lysine 426 of human placental S-adenosylhomocysteine hydrolase inactivates the enzyme. (1994) (41)
Coumarinic Acid-Based Cyclic Prodrugs of Opioid Peptides that Exhibit Metabolic Stability to Peptidases and Excellent Cellular Permeability (2004) (40)
Chemical Pathways of Peptide Degradation. I. Deamidation of Adrenocorticotropic Hormone (1990) (40)
Optimizing the "drug-like" properties of leads in drug discovery (2006) (40)
Esterase-Sensitive Cyclic Prodrugs of Peptides: Evaluation of an Acyloxyalkoxy Promoiety in a Model Hexapeptide (1996) (40)
Acyloxyalkoxy-Based Cyclic Prodrugs of Opioid Peptides: Evaluation of the Chemical and Enzymatic Stability as Well as Their Transport Properties Across Caco-2 Cell Monolayers (2004) (40)
9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl) derivatives of adenine and 3-deazaadenine: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase. (1988) (40)
Inhibitory effect of sugars and polyols on the metal-catalyzed oxidation of human relaxin. (1996) (40)
Permeability and Mechanism of Albumin, Cationized Albumin, and Glycosylated Albumin Transcellular Transport Across Monolayers of Cultured Bovine Brain Capillary Endothelial Cells (1989) (40)
Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues. (1997) (40)
Effect of secondary structure on the rate of deamidation of several growth hormone releasing factor analogs. (2009) (39)
Purification and characterization of rat liver microsomal thiol methyltransferase. (1978) (39)
Racemization of an asparagine residue during peptide deamidation. (2003) (38)
Mechanism of L-α-Methyldopa Transport Through a Monolayer of Polarized Human Intestinal Epithelial Cells (Caco-2) (1990) (38)
Recent advances in S-adenosyl-L-homocysteine hydrolase inhibitors and their potential clinical applications (1999) (38)
Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine). (1998) (37)
The role of nicotinamide adenine dinucleotide in the inhibition of bovine liver S-adenosylhomocysteine hydrolase by neplanocin A. (1987) (37)
Orally active peptidomimetic RGD analogs that are glycoprotein IIb/IIIa antagonists. (2000) (37)
Purification and characterization of rat heart and brain catechol methyltransferase. (1978) (37)
The effect of cosolutes on the isomerization of aspartic acid residues and conformational stability in a monoclonal antibody. (2007) (36)
Epinephrine in rat hypothalamus: antagonism by desipramine of 6-hydroxydopamine-induced depletion (1978) (36)
Iron-thiolate induced oxidation of methionine to methionine sulfoxide in small model peptides. Intramolecular catalysis by histidine. (1993) (36)
Synthesis of hydroxylated cyclohexenyl- and cyclohexanyladenines as potential inhibitors of S-adenosylhomocysteine hydrolase (1992) (36)
Characterization of the Efflux Transporter(s) Responsible for Restricting Intestinal Mucosa Permeation of the Coumarinic Acid-Based Cyclic Prodrug of the Opioid Peptide DADLE (2002) (36)
Hidalgo, I. J., Raub, T. J., and Borchardt, R. T.: Characterization of the Human Colon Carcinoma Cell Line (Caco-2) as a Model System for Intestinal Epithelial Permeability, Gastroenterology, 96, 736–749, 1989—The Backstory (2011) (36)
Chemical Modification and Site-directed Mutagenesis of Cysteine Residues in Human Placental S-Adenosylhomocysteine Hydrolase* (1996) (36)
Chemical Pathways of Peptide Degradation. V. Ascorbic Acid Promotes Rather than Inhibits the Oxidation of Methionine to Methionine Sulfoxide in Small Model Peptides (1993) (36)
Mechanism of alkaline hydrolysis of S-adenosyl-L-methionine and related sulfonium nucleosides (1979) (35)
Antiviral drug ribavirin is a selective inhibitor of S‐adenosyl‐L‐homocysteine hydrolase from Trypanosoma cruzi (2006) (35)
Determination of O-methylated metabolites of cathecholamines using high-performance liquid chromatography and electrochemical detection. (1978) (35)
Estimating intestinal mucosal permeation of compounds using Caco-2 cell monolayers. (2001) (35)
General method for the synthesis of phthalaldehydic acids and phthalides from o-bromobenzaldehydes via ortho-lithiated aminoalkoxides (1983) (35)
Amine Prodrugs Which Utilize Hydroxy Amide Lactonization. I. A Potential Redox-Sensitive Amide Prodrug (2004) (35)
Substrate binding stabilizes S-adenosylhomocysteine hydrolase in a closed conformation. (2000) (35)
Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor1 (1999) (35)
Characterization of specific receptors for atrial natriuretic factor on cultured bovine brain capillary endothelial cells. (1988) (35)
Phenylpropionic Acid-Based Cyclic Prodrugs of Opioid Peptides that Exhibit Metabolic Stability to Peptidases and Excellent Cellular Permeation (2004) (34)
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations. (2004) (34)
A liquid chromatographic assay for phenylethanolamine N-methyltransferase. (1977) (34)
Quantitative analysis of a model opioid peptide and its cyclic prodrugs in rat plasma using high-performance liquid chromatography with fluorescence and tandem mass spectrometric detection. (2002) (34)
Distribution and provenance of lunar highland rock types at North Ray Crater, Apollo 16 (1982) (33)
Phosphate Prodrugs for Amines Utilizing a Fast Intramolecular Hydroxy Amide Lactonization (1996) (33)
Transport characteristics of peptides and peptidomimetics: I. N-methylated peptides as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. (2001) (33)
A rapid spectrophotometric assay for catechol-O-methyltransferase. (1974) (33)
Inhibition of indolethylamine-N-methyltransferase by analogs of S-adenosylhomocysteine. (1975) (32)
Hexose uptake in primary cultures of bovine brain microvessel endothelial cells. II. Effects of conditioned media from astroglial and glioma cells. (1991) (32)
Adenine nucleoside dialdehydes: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase. (1985) (32)
A 9-step enantiospecific synthesis of (-)-aristeromycin from D-ribonic acid γ-lactone (1989) (32)
Effects of acidic N + 1 residues on asparagine deamidation rates in solution and in the solid state. (2005) (32)
Nucleic acid related compounds. 74. Synthesis and biological activity of 2'(and 3')-deoxy-2'(and 3')-methylenenucleoside analogues that function as mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase. (1992) (32)
Synthesis and evaluation of the physicochemical properties of esterase-sensitive cyclic prodrugs of opioid peptides using an (acyloxy)alkoxy linker. (1999) (31)
The application of cell culture systems in drug discovery and development. (1995) (31)
Adenosine dialdehyde: a potent inhibitor of vaccinia virus multiplication in mouse L929 cells. (1987) (30)
Physico‐Chemical and Biological Factors that Influence a Drug's Cellular Permeability by Passive Diffusion (2008) (30)
Esterase-Sensitive Cyclic Prodrugs of Peptides: Evaluation of a Phenylpropionic Acid Promoiety in a Model Hexapeptide (2004) (30)
Stability of oxymethyl-modified coumarinic acid cyclic prodrugs of diastereomeric opioid peptides in biological media from various animal species including human. (2005) (30)
Asparagine deamidation in recombinant human lymphotoxin: hindrance by three-dimensional structures. (2003) (30)
Reactivity toward deamidation of asparagine residues in beta-turn structures. (2000) (30)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 8. Molecular dissections of carbocyclic 3-deazaadenosine as inhibitors of S-adenosylhomocysteine hydrolase. (1985) (29)
A coumarin-based prodrug strategy to improve the oral absorption of RGD peptidomimetics. (2000) (29)
Automated analysis of polyethylene glycol-induced inhibition of P-glycoprotein activity in vitro. (2003) (29)
Effects of 9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl)-adenine and -3-deazaadenine on the metabolism of S-adenosylhomocysteine in mouse L929 cells. (1988) (29)
Nucleic Acid Related Compounds. 80. Synthesis of 5'-S-(Alkyl and aryl)-5'-fluoro-5'-thioadenosines with Xenon Difluoride or (Diethylamido)sulfur Trifluoride, Hydrolysis in Aqueous Buffer, and Inhibition of S-Adenosyl-L-homocysteine hydrolase by derived "Adenosine 5'-Aldehyde" Species (1994) (29)
Comparison of the rates of deamidation, diketopiperazine formation, and oxidation in recombinant human vascular endothelial growth factor and model peptides (2000) (28)
The effect of conformation of the acyloxyalkoxy-based cyclic prodrugs of opioid peptides on their membrane permeability. (1999) (28)
Combined modulation of S-adenosylmethionine biosynthesis and S-adenosylhomocysteine metabolism enhances inhibition of nucleic acid methylation and L1210 cell growth. (1990) (28)
Amine Prodrugs Which Utilize Hydroxy Amide Lactonization. II. A Potential Esterase-Sensitive Amide Prodrug (1991) (28)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 9. 2',3'-Dialdehyde derivatives of carbocyclic purine nucleosides as inhibitors of S-adenosylhomocysteine hydrolase. (1985) (28)
Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its "hydrolytic activity": synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine. (1998) (28)
The Effect of Conformation on Membrane Permeability of an Acyloxyalkoxy-linked Cyclic Prodrug of a Model Hexapeptide (1996) (27)
Evaluation of the bile acid transporter in enhancing intestinal permeability to renin-inhibitory peptides. (1993) (27)
Affinity Labeling of Catechol O-Methyltransferase by the Oxidation Products of 6-Hydroxydopamine (1975) (27)
Chemical Pathways of Peptide Degradation. VIII. Oxidation of Methionine in Small Model Peptides by Prooxidant/Transition Metal Ion Systems: Influence of Selective Scavengers for Reactive Oxygen Intermediates (1995) (27)
Catechol O-methyltransferase. 4. In vitro inhibition by 3-hydroxy-4-pyrones, 3-hydroxy-2-pyridones, and 3-hydroxy-4-pyridones. (1973) (27)
Utilization of a Human Intestinal Epithelial Cell Culture System (Caco-2) for Evaluating Cytoprotective Agents (1993) (27)
Reaction of a peptide with polyvinylpyrrolidone in the solid state. (2003) (26)
Evidence for the involvement of histidine A(12) in the aggregation and precipitation of human relaxin induced by metal-catalyzed oxidation. (2000) (26)
Metabolism and Mechanism of Action of Neplanocin A — A Potent Inhibitor of S-Adenosylhomocysteine Hydrolase (1986) (26)
Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects. (2002) (26)
pH-induced change in the rate-determining step for the hydrolysis of the Asp/Asn-derived cyclic-imide intermediate in protein degradation (1996) (26)
Characterization of the Efflux Transporter(s) Responsible for Restricting Intestinal Mucosa Permeation of an Acyloxyalkoxy-Based Cyclic Prodrug of the Opioid Peptide DADLE (2002) (26)
Silica gel assisted reductive cyclization of alkoxy-2, .beta.-dinitrostyrenes to alkoxyindoles (1983) (25)
Chemical Pathways of Peptide Degradation: IX. Metal-Catalyzed Oxidation of Histidine in Model Peptides (1998) (25)
Effects of 4'-modified analogs of aristeromycin on the metabolism of S-adenosyl-L-homocysteine in murine L929 cells. (1993) (25)
A comparison of the effects of p-glycoprotein inhibitors on the blood-brain barrier permeation of cyclic prodrugs of an opioid peptide (DADLE). (2009) (25)
Effects of solution polarity and viscosity on peptide deamidation. (2000) (25)
Molecular mechanism of action of 5,6-dihydroxytryptamine. Synthesis and biological evaluation of 4-methyl-, 7-methyl-, and 4,7-dimethyl-5,6-dihydroxytryptamines. (1985) (24)
Synthesis and conformational analysis of a coumarinic acid-based cyclic prodrug of an opioid peptide with modified sensitivity to esterase-catalyzed bioconversion. (2002) (24)
Metabolism, Uptake, and Transepithelial Transport of the Diastereomers of Val-Val in the Human Intestinal Cell Line, Caco-2 (1996) (24)
Guinea Pig Brain Histamine N‐Methyltransferase: Purification and Partial Characterization (1983) (24)
Synthesis and biological activity of 2- and 4-substituted 6,7-dihydroxy-1,2,3,4-tetrahydroisoquinolines. (1976) (24)
Metabolism of L-alpha-methyldopa in cultured human intestinal epithelial (Caco-2) cell monolayers. Comparison with metabolism in vivo. (1994) (24)
Integration of pharmaceutical discovery and development : case histories (1998) (23)
Biological Methylation and Drug Design: Experimental and Clinical Role of S-Adenosylmethionine (1986) (23)
Domain motions and the open-to-closed conformational transition of an enzyme: a normal mode analysis of S-adenosyl-L-homocysteine hydrolase. (2005) (23)
(E)-5',6'-didehydro-6'-deoxy-6'-fluorohomoadenosine: a substrate that measures the hydrolytic activity of S-adenosylhomocysteine hydrolase. (1994) (23)
Molecular mechanism of biological action of the serotonergic neurotoxin 5,7-dihydroxytryptamine (1988) (23)
Nucleic Acid Related Compounds. 101.S-Adenosyl-l-homocysteine Hydrolase Does Not Hydrate (5‘-Fluoro)vinyl or (6‘-Halo)homovinyl Analogues Derived from 3‘-Deoxyadenosine or 3‘-(Chloro or Fluoro)-3‘-deoxyadenosine1 (1998) (22)
A Modified Coumarinic Acid-Based Cyclic Prodrug of an Opioid Peptide: Its Enzymatic and Chemical Stability and Cell Permeation Characteristics (2002) (22)
Transport of Macromolecules Across the Capillary Endothelium (1991) (22)
In Vitro Drug Absorption Models. I. Brush Border Membrane Vesicles, Isolated Mucosal Cells and Everted Intestinal Rings: Characterization and Salicylate Accumulation (1985) (22)
S-Adenosylmethionine and its analogs. Structural features correlated with synthesis and methylation of mRNAs of cytoplasmic polyhedrosis virus. (1980) (22)
Probing the helical content of growth hormone-releasing factor analogs using electrospray ionization mass spectrometry (1993) (22)
Absorption barriers in the rat intestinal mucosa: 2. Application of physiologically based mathematical models to quantify mechanisms of drug permeation and metabolism. (2010) (22)
Mechanism of inactivation of S-adenosylhomocysteine hydrolase by (E)-5',6'-didehydro-6'-deoxy-6'-halohomoadenosines. (1994) (21)
Synthesis and evaluation of novel coumarin-based esterase-sensitive cyclic prodrugs of peptidomimetic RGD analogs with improved membrane permeability. (1999) (21)
Deamidation of asparaginyl residues in proteins: a potential pathway for chemical degradation of proteins in lyophilized dosage forms. (1990) (21)
Catechol O-methyltransferase. 12. Affinity labeling the active site with the oxidation products of 5,6-dihydroxyindole. (1982) (21)
Phenol sulfotransferase. II. Inactivation by phenylglyoxal, N-ethylmaleimide and ribonucleotide 2',3'-dialdehydes. (1982) (21)
Metabolic conversion of neplanocin A to S-neplanocylmethionine by mouse L 929 cells. (1984) (21)
Overexpression, purification, and characterization of S-adenosylhomocysteine hydrolase from Leishmania donovani. (2000) (21)
An Ecteola-cellulose chromatography assay for 3'-phosphoadenosine 5'-phosphosulfate: phenol sulfotransferase. (1983) (21)
Targeting 5'-deoxy-5'-(methylthio)adenosine phosphorylase by 5'-haloalkyl analogues of 5'-deoxy-5'-(methylthio)adenosine. (1991) (21)
A Novel Mechanism-based Inhibitor (6′-Bromo-5′,6′-didehydro-6′-deoxy-6′-fluorohomoadenosine) That Covalently Modifies Human Placental S-Adenosylhomocysteine Hydrolase* (1998) (21)
Catechol O-methyltransferase. 2. In vitro inhibition by substituted 8-hydroxyquinolines. (1973) (21)
(1′R, 2′S, 3′R)-9-(2′, 3′-Dihydroxycyclopentan-1′-yl)-Adenine and −3-Deaza-Adenine: Analogues of Aristeromycin Which Exhibit Potent Antiviral Activity with Reduced Cytotoxicity (1993) (21)
Catechol O-methyltransferase. 7. Affinity labeling with the oxidation products of 6-aminodopamine. (1976) (20)
IMMUNOLOGICAL CHARACTERIZATION OF CATECHOL-O-METHYLTRANSFERASE (1973) (20)
Biotin transport in a human intestinal epithelial cell line (Caco-2). (1993) (20)
Contributions of active site residues to the partial and overall catalytic activities of human S-adenosylhomocysteine hydrolase. (2002) (20)
Chapter 3 – N- and O-Methylation (1980) (20)
Development of a Novel Redox-Sensitive Protecting Group for Amines Which Utilizes a Facilitated Lactonization Reaction (1995) (20)
Carrier-mediated transport of the antitumor agent acivicin across the blood-brain barrier. (1995) (20)
STRUCTURAL ANALYSIS OF A FACILE LACTONIZATION SYSTEM FACILITATED BY A TRIMETHYL LOCK (1996) (20)
The effects of a histidine residue on the C-terminal side of an asparaginyl residue on the rate of deamidation using model pentapeptides. (2000) (20)
Purification of catechol-O-methyltransferase by affinity chromatography. (1975) (19)
Solid state chemical instability of an asparaginyl residue in a model hexapeptide. (1994) (19)
Adenosine-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. (1993) (19)
Purification and characterization of some metabolic effects of S-neplanocylmethionine. (1985) (19)
Pharmaceutical Applications of Cell Culture: An Overview (1991) (19)
Doubly homologated dihalovinyl and acetylene analogues of adenosine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects. (2000) (19)
Elucidation of the mechanism by which homocysteine potentiates the anti-vaccinia virus effects of the S-adenosylhomocysteine hydrolase inhibitor 9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl)-adenine. (1989) (19)
Absorption barriers in the rat intestinal mucosa: 1. Application of an in situ perfusion model to simultaneously assess drug permeation and metabolism. (2010) (19)
The isolation and characterization of the methyl acceptor protein from adrenal chromaffin granules. (1978) (19)
Composition, structure, and age of the Apollo 16 subregolith basement as deduced from the chemistry of post-imbrium melt bombs (1986) (19)
Derivatives of melphalan designed to enhance drug accumulation in cancer cells. (1997) (18)
Assessment of transport barriers using cell and tissue culture systems (1990) (18)
Trypanosoma cruzi: molecular cloning and characterization of the S-adenosylhomocysteine hydrolase. (2003) (18)
Mechanism of action of S-adenosyl-L-homocysteine hydrolase. Measurement of kinetic isotope effects using adenosine-3'-d and S-adenosyl-L-homocysteine-3'-d as substrates (1985) (18)
S-Aristeromycinyl-L-homocysteine, a potent inhibitor of S-adenosylmethionine-dependent transmethylations. (1976) (18)
Intestinal absorption of alpha-methyldopa: in vitro mechanistic studies in rat small intestinal segments. (1987) (18)
Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. (2001) (18)
Phenol sulfotransferase. I. Purification of a rat liver enzyme by affinity chromatography. (1982) (18)
Metabolism of Catecholamine Esters by Cultured Bovine Brain Microvessel Endothelial Cells (1989) (18)
A Comparison of the Bioconversion Rates and the Caco-2 Cell Permeation Characteristics of Coumarin-Based Cyclic Prodrugs and Methylester-Based Linear Prodrugs of RGD Peptidomimetics (1998) (18)
Inhibition of S-Adenosylmethionine-Dependent Transmethylation as an Approach to the Development of Antiviral Agents (1988) (17)
Affinity labeling of histamine N-methyltransferase by 2',3'-dialdehyde derivatives of S-adenosylhomocysteine and S-adenosylmethionine. Kinetics of inactivation. (1978) (17)
Facilitated Intramolecular Conjugate Addition of Amides of 3-(3',6'-Dioxo-2',4'-dimethyl-1',4'-cyclohexadienyl)-3,3-dimethylpropionic Acid. 2. Kinetics of Degradation. (1996) (17)
Structure-affinity relationships of Val-Val and Val-Val-Val stereoisomers with the apical oligopeptide transporter in human intestinal Caco-2 cells. (1998) (17)
Effect of N-1 and N-2 residues on peptide deamidation rate in solution and solid state (2006) (17)
Computational characterization of substrate binding and catalysis in S-adenosylhomocysteine hydrolase. (2001) (17)
Phenol Sulfotransferase: Purification and Characterization of the Rat Brain Enzyme (1981) (17)
Effects of sucrose and mannitol on asparagine deamidation rates of model peptides in solution and in the solid state. (2005) (17)
tert-Butyldimethylsilyl ethers of phenols: Their one-step conversion to benzyl or methyl ethers and utility in regioselective ortho lithiation (1987) (17)
Desilylation of tert-Butyldimethylsilyl Ethers of Phenols (1988) (16)
Catechol O-methyltransferase. 10. 5-Substituted 3-hydroxy-4-methoxybenzoic acids (isovanillic acids) and 5-substituted 3-hydroxy-4-methoxybenzaldehydes (isovanillins) as potential inhibitors. (1982) (16)
Adenosine dialdehyde and neplanocin A: Potent inhibitors of S-adenosylhomocysteine hydrolase in neuroblastoma N2a cells (1987) (16)
Mechanism and products of autoxidation of 5,7-dihydroxytryptamine (1985) (16)
Protein Delivery (2002) (16)
Chemical Pathways of Peptide Degradation. X: Effect of Metal-Catalyzed Oxidation on the Solution Structure of a Histidine-Containing Peptide Fragment of Human Relaxin (2000) (16)
A Comparison of Peptidase Activities and Peptide Metabolism in Cultured Mouse Keratinocytes and Neonatal Mouse Epidermis (2004) (16)
Solution conformation of Leu27 hGRF(1-32)NH2 and its deamidation products by 2D NMR. (2009) (16)
Catechol O-methyltransferase. 9. Mechanism of inactivation by 6-hydroxydopamine. (1976) (16)
Stereopopulation control. V. Facilitation on intramolecular conjugate addition of an aldehyde hydrate and hemiacetal (1973) (15)
Evidence for sulfhydryl groups at the active site of catechol-O-methyltransferase. (1976) (15)
Effects of ligand binding and oxidation on hinge-bending motions in S-adenosyl-L-homocysteine hydrolase. (2006) (15)
Stereoselective Synthesis of Sugar-Modified Enyne Analogues of Adenosine and Uridine. Interaction with S-Adenosyl-L-homocysteine Hydrolase and Antiviral and Cytotoxic Effects (2004) (15)
Cultured bovine brain capillary endothelial cells (BBCEC) - a blood-brain barrier model for studying the binding and internalization of insulin and insulin-like growth factor 1 (1987) (15)
Mechanism of the synergistic antiviral and cytostatic activity of (RS)-3-(adenin-9-yl)-2-hydroxypropanoic acid isobutyl ester and D,L-homocysteine. (1990) (15)
Effects of amino acid chirality and the chemical linker on the cell permeation characteristics of cyclic prodrugs of opioid peptides. (2006) (15)
CATECHOL-O-METHYLTRANSFERASE PART 5, STRUCTURE-ACTIVITY RELATIONSHIPS FOR INHIBITION BY FLAVONOIDS (1975) (15)
A conformational study of catecholamine receptor sites. 6. Syntheses of dl-3-amino-2-(3,4-dihydroxyphenyl)-trans-2-decalin hydrochlorides. (1971) (14)
Oxidation of neplanocin A to the corresponding 3'-keto derivative by S-adenosylhomocysteine hydrolase. (1989) (14)
In Vitro Drug Absorption Models. II. Salicylate, Cefoxitin, α-Methyldopa and Theophylline Uptake in Cells and Rings: Correlation with In Vivo Bioavailability (1985) (14)
Mechanisms of inactivation of human S-adenosylhomocysteine hydrolase by 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosines. (2000) (14)
Phenol-sulfotransferase inactivation by 2,3-butanedione and phenylglyoxal: evidence for an active site arginyl residue. (1977) (14)
Importance of the aromatic ring in adrenergic amines. Nonaromatic analoques of phenylethanolamine as substrates for phenylethanolamine N-methyltransferase. (1975) (14)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 7. Role of the ribosyl moiety in enzymatic binding of S-adenosyl-L-homocysteine and S-adenosyl-L-methionine. (1978) (13)
S-adenosylhomocysteine analogues as inhibitors of specific tRNA methylation. (1978) (13)
Integration of Pharmaceutical Discovery and Development (1998) (13)
Significant differences in the disposition of cyclic prodrugs of opioid peptides in rats and guinea pigs following IV administration. (2005) (13)
Formaldehyde production by Tris buffer in peptide formulations at elevated temperature. (2001) (13)
Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatic vs. nonaromatic substrates and inhibitors. (1982) (13)
Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 1. Basic features of the association and dissociation processes. (2007) (13)
Transport Characteristics of Peptidomimetics. Effect of the Pyrrolinone Bioisostere on Transport Across Caco-2 Cell Monolayers (1998) (13)
The delivery of peptides (1989) (13)
4',1'a-Methanocarbocyclic Adenosine Analogues as Potential Inhibitors of S-Adenosylhomocysteine Hydrolase (1995) (13)
Conformational preferences of amphetamine analogues for inhibition of phenylethanolamine N-methyltransferase. Conformationally defined adrenergic agents. 5. (1981) (13)
The effect of beta-turn structure on the passive diffusion of peptides across Caco-2 cell monolayers. (1997) (13)
Affinity labeling of catechol O-methyltransferase by N-haloacetyl derivatives of 3,5-dimethoxy-4-hydroxyphenylethylamine and 3,4-dimethoxy-5-hydroxyphenylethylamine. Kinetics of inactivation. (1975) (13)
Photoaffinity Labeling of Human Placental S-Adenosylhomocysteine Hydrolase with [2-3H]8-Azido-adenosine (*) (1995) (12)
Transport and metabolism of delta sleep-inducing peptide in cultured human intestinal epithelial cell monolayers. (1995) (12)
Ligand-dependent changes in intrinsic fluorescence of S-adenosylhomocysteine hydrolase: implications for the mechanism of inhibitor-induced inhibition. (1993) (12)
Importance of the aromatic ring in adrenergic amines. 6. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of pi-electronic and steric interactions. (1981) (12)
Catechol O-methyltransferase. 3. Mechanism of pyridoxal 5'-phosphate inhibition. (1973) (12)
Molecular dynamics simulations of domain motions of substrate‐free S‐adenosyl‐ L‐homocysteine hydrolase in solution (2008) (12)
The effect of size, charge and cyclization of model peptides on their in vitro release from dl–PLGA microspheres (1997) (12)
Catechol O-methyltransferase. 6. Affinity labeling with N-haloacetyl-3,5-dimethoxy-4-hydroxyphenylalkylamines. (1975) (12)
Facilitated intramolecular conjugate addition of N-(p-methoxyphenyl)-3-(3',6'-dioxo-2',4'-dimethylcyclohexa-1',4'-dienyl)-3,3-diemthylpropionamide. I: Product characterization (1992) (12)
Inactivation of S-adenosyl-L-homocysteine hydrolase by amide and ester derivatives of adenosine-5'-carboxylic acid. (1996) (12)
A molecular model for the active site of S-adenosyl-l-homocysteine hydrolase (1991) (12)
Silica gel assisted reductive cyclization of 2‐nitro‐β‐piperidinostyrenes, derived from 2‐nitrotoluenes, to indoles (1987) (12)
Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. (1994) (12)
S-ADENOSYL-L-METHIONINE-DEPENDENT MACROMOLECULE METHYLTRANSFERASES: POTENTIAL TARGETS FOR THE DESIGN OF CHEMOTHERAPEUTIC AGENTS (1980) (12)
2-Methylpropyl ester of 3-(adenin-9-yl)-2-hydroxypropanoic acid. Mechanism of antiviral action in vaccinia virus-infected L929 cells. (1990) (11)
The Effect of β-Turn Structure on the Permeation of Peptides Across Monolayers of Bovine Brain Microvessel Endothelial Cells (1997) (11)
Rational Approaches to the Design of Mechanism-Based Inhibitors of S-Adenosylhomocysteine Hydrolase (1995) (11)
S-homoadenosyl-L-cysteine and S-homoadenosyl-L-homocysteine. Synthesis and binding studies of hon-hydrolyzed substrate analogues with S-adenosyl-L-homocysteine hydrolase. (2002) (11)
Addition of 1-nitroalkanes to methyl 2,3-O-isopropylidene-β-d-ribo-pentodialdo-1,4-furanoside and N6-benzoyl-2′,3′-O-isopropylideneadenosine-5′-aldehyde (1983) (11)
Effect of stereochemistry on the transport of Aca-linked beta-turn peptidomimetics across a human intestinal cell line. (1997) (11)
Mechanism of autoxidation of 5,7-dihydroxytryptamine: effect of fluorine substitution at positions 4 and/or 6. (1990) (11)
The Rationale for Targeting the NAD/NADH Cofactor Binding Site of Parasitic S-Adenosyl-L-Homocysteine Hydrolase for the Design of Anti-Parasitic Drugs (2009) (11)
Secondary structure of a dynamic type I’β-hairpin peptide (2004) (10)
A convenient method for the synthesis of indole-3-acetic acids (1994) (10)
Synthesis and biological evaluation of 4-fluoro-, 7-fluoro-, and 4,7-difluoro-5,6-dihydroxytryptamines. (1990) (10)
Synthesis of Analogues of Neplanocin A: Utilization of Optically Active Dihydroxycyclopentenones Derived from Carbohydrates. (1988) (10)
The Lactonization of 2′‐Hydroxyhydrocinnamic Acid Amides: A Potential Prodrug for Amines. (1991) (10)
Affinity labeling of catechol-O-methyltransferase with N-iodoacetyl-3,5-dimethoxy-4-hydroxyphenylethylamine. (1973) (10)
Conformational study oof catecholamine receptor sites. 7. Syntheses of erythro- and threo-3-amino-2-(3,4-dihydroxyphenyl)-2-butanol hydrochlorides and erythro- and threo-2-amino-3-(3,4-dihydroxyphenyl)butane hydrochlorides. (1971) (10)
Steric hindrance is a key factor in the coupling reaction of (acyloxy) alkyl-α-halides with phenols to make a new promoiety for prodrugs (2002) (10)
Stereopopulation control. VI. Conformational selection of alternative oxidation pathways (1973) (10)
Characteristics of Protein Carboxyl Methylation in the Rat Hypothalamus (1982) (10)
Chemical pathways of peptide degradation i. deamidation of acth (1990) (10)
Synergistic Antiviral Activity of Inhibitors of S-Adenosylhomocysteine Hydrolase and Ribavirin (1993) (10)
Characterization of serotonin uptake in cultured neuroblastoma cells. Difference between differentiated and nondifferentiated cells. (1982) (10)
Characterization of serotonin uptake in cultured pheochromocytoma cells. Comparison with norepinephrine uptake. (1982) (10)
Deamidation of model β-turn cyclic peptides in the solid state (2005) (9)
General principles in the characterization and use of model systems for biopharmaceutical studies. (1996) (9)
Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 2. The role of helix 18 stability. (2008) (9)
Metabolism of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) by bovine brain microvessel endothelial cells (1989) (9)
Aromatic hydroxylation. Hydroxybenzaldehydes from bromobenzaldehydes via reaction of in situ generated, lithiated .alpha.-morpholinobenzyl alkoxides with nitrobenzene (1983) (9)
Deamidation of a model hexapeptide in poly(vinyl alcohol) hydrogels and xerogels. (2000) (9)
Inhibitors of phenylethanolamine-N-methyltransferase. 2. Comparison of nonaromatic analogs of phenylethanolamines, 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline (SKF-64139) and 2,3-dichloro-alpha-methylbenzylamine: effects on rat brain and adrenal catecholamine content and blood pressure. (1982) (9)
Characterization of LLC-PK1 Kidney Epithelial Cells as an in Vitro Model for Studying Renal Tubular Reabsorption of Protein Drugs (1995) (9)
Potential inhibitors of S-adenosylmethionine-dependent methyltransferases. 10. Base- and amino acid modified analogues of S-aristeromycinyl-L-homocysteine. (1985) (9)
Liquid chromatographic analysis of leucine-enkephalin and its metabolites in homogenates of cultured human keratinocytes. (1990) (8)
Purification of bovine liver S-adenosylhomocysteine hydrolase by affinity chromatography on blue dextran-agarose. (1988) (8)
Introduction to the Blood–Brain Barrier: Brain microvessel endothelial cell culture systems (1998) (8)
The mechanism of inhibition of Alcaligenes faecalis S-adenosylhomocysteine hydrolase by neplanocin A. (1987) (8)
Metabolism, Uptake, and Transepithelial Transport of the Stereoisomers of Val-Val-Val in the Human Intestinal Cell Line, Caco-2 (2004) (8)
Cultured human colon carcinoma cells (Caco-2) as a model to study the mechanism by which palmitoyl-DL-carnitine enhances intestinal permeability of drugs (1993) (8)
Caco-2 cell monolayers as a model for studies of drug transport across human intestinal epithelium (2002) (8)
Rational Delivery Strategies for the Design of Peptides with Enhanced Oral Delivery (1994) (8)
Synthesis of 5'-functionalized nucleosides: S-Adenosylhomocysteine analogues with the carbon-5' and sulfur atoms replaced by a vinyl or halovinyl unit. (2008) (8)
Synthesis of homologated halovinyl derivatives from aristeromycin and their inhibition of human placental S-adenosyl-L-homocysteine hydrolase. (1998) (8)
Are Graduate Programs Training Pharmaceutical Scientists to Function Effectively in the New, Highly Integrated and Globalized Pharmaceutical Industry? (1997) (8)
Aristeromycin-5'-carboxaldehyde: a potent inhibitor of S-adenosyl-L-homocysteine hydrolase. (1996) (8)
Inhibitors of phenylethanolamine N-methyltransferase. 1. Effects of 2-cycloocytyl-2-hydroxyethylamine on rat brain and adrenal catecholamine content and blood pressure. (1982) (8)
Synthesis and evaluation of 4′-5′-dehydro-5′-fluoroaristeromycins as S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitors (1992) (7)
Catechol O-methyltransferase. 8. Structure-activity relationships for inhibition by 8-hydroxyquinolines (1976) (7)
Histamine N-methyltransferase. Inhibition and potentiation by trans- and cis-1,5-diphenyl-3-dimethylaminopyrrolidine. (1974) (7)
Directed Drug Delivery: A Multidisciplinary Problem (1985) (7)
Adenosine dialdehyde: A potent inhibitor of S-adenosylhomocysteine hydrolase (1982) (7)
The effect of beta-turn structure on the permeation of peptides across monolayers of bovine brain microvessel endothelial cells. (1997) (7)
STEREOPOPULATION CONTROL PART 4, FACILITATION OF INTRAMOLECULAR CONJUGATE ADDITION OF THE HYDROXYL GROUP (1974) (7)
Targeting 5′‐Epoxy‐5′‐(methylthio)adenosine Phosphorylase by 5′‐Haloalkyl Analogues of 5′‐Deoxy‐5′‐(methylthio)adenosine. (1992) (7)
A simple diffusion device to study transport across cells cultured on microporous membranes (1990) (7)
Factors that restrict the intestinal cell permeation of cyclic prodrugs of an opioid peptide (DADLE): Part I. Role of efflux transporters in the intestinal mucosa. (2009) (7)
Effects of selected vasoactive substances on adenylate cyclase activity in brain, isolated brain microvessels, and primary cultures of brain microvessel endothelial cells (1992) (7)
Factors that restrict intestinal cell permeation of cyclic prodrugs of an opioid peptide (DADLE): Part II. Role of metabolic enzymes in the intestinal mucosa. (2009) (7)
Elucidation of the Mechanism by Which 9-(Trans-2′, Trans-3′-Dihydroxycyclopent-4′-enyl)-Adenine Lnactivates S-Adenosylhomocysteine Hydrolase and Elevates Cellular Levels of Sadenosylhomocysteinew (1989) (7)
S-adenosylmethionine, S-adenosylhomocysteine and S-adenosylhomocysteine hydrolase variations during differentiation of Dictyostelium discoideum. (1988) (7)
A new side-by-side diffusion cell for studying transport across epithelial cell monolayers (1992) (7)
Limited proteolysis of S-adenosylhomocysteine hydrolase: implications for the three-dimensional structure. (1995) (7)
Factors that restrict the cell permeation of cyclic prodrugs of an opioid peptide, part 3: Synthesis of analogs designed to have improved stability to oxidative metabolism. (2012) (6)
Crystallization and preliminary X-ray analysis of human placental S-adenosylhomocysteine hydrolase. (1997) (6)
Adenosine 5'-diphosphate dialdehyde: an affinity labeling reagent for phenol-sulfotransferase. (1978) (6)
Selected-ion monitoring gas chromatographic-mass spectrometric analysis of catecholamines: enhancement of sensitivity by a simple clean-up step on Sephadex G-10. (1988) (6)
S-adenosyl-L-homocysteine dialdehyde: an affinity labeling reagent for histamine-N-methyltransferase. (1977) (6)
The mechanism of inactivation of human placental S-adenosylhomocysteine hydrolase by (E)-4',5'-didehydro-5'-methoxyadenosine and adenosine 5'-carboxaldehyde oxime. (1997) (6)
PERMEABILITY CHARACTERISTICS OF CULTURED MOUSE KERATINOCYTES COMPARED TO HAIRLESS MOUSE SKIN (1991) (6)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. 6. TRUCTURAL MODIFICATIONS OF S-ADENOSYLMETHIONINE (1976) (6)
Identification and quantitation of tetrapeptide deamidation products by mass spectrometry. (1992) (6)
Release of endogenous brain epinephrine by the calcium ionophores X537A and A23187 (1985) (6)
Potential inhibitor of S-adenosylmethionine-dependent methyltransferases. 2. Modification of the base portion of S-adenosylhomocysteine. (1974) (6)
Peptidyl dipeptidase A-catalyzed metabolism of delta sleep-inducing peptide in bovine brain microvessel endothelial cells: a cell culture model of the blood brain barrier. (1995) (5)
Adenosine-Derived 5′-α-Halo Thioether, Sulfoxide, Sulfone, and (5′-Halo)Methylene Analogues. Inhibition of S-Adenosyl-L-Homocysteine Hydrolase (1993) (5)
Efficient synthesis of 3,5-dihydroxy-4-methylbenzoic acid (1981) (5)
Selective fluorogenic derivatization of a peptide nucleic acid trimer with naphthalene-2,3-dicarboxaldehyde. (1997) (5)
Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and alpha-methylbenzylamine. (1982) (5)
Effects of ascorbic acid on the uptake of serotonin in differentiated neuroblastoma cells. (1982) (5)
Cultured brain microvessel endothelial cells as in vitro models of the blood-brain barrier. (1992) (5)
Comparison of separation and detection techniques for human growth hormone releasing factor (hGRF) and the products derived from deamidation. (1993) (5)
Thalictrum alkaloids. 8. The isolation, structural elucidation, and synthesis of dehydrothalicarpine. (1968) (5)
Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase? (2005) (5)
Immobilization of ascorbic acid oxidase (1982) (5)
Effects of phenylethanolamine N-methyltransferase inhibitors on rat brain catecholamine levels and body temperature. (1982) (5)
Directional probes of the hydrophobic component of the aromatic ring binding site of norepinephrine N-methyltransferase. (1982) (5)
Properties of phenol sulphotransferase from brain of the monkey Rhesus macaca. (1992) (4)
Solution and Solid‐State Chemical Instabilities of Asparaginyl and Aspartyl Residues in Model Peptides. (1995) (4)
Mechanism of autoxidation of 5,7-dihydroxytryptamine: singlet oxygen-18 is incorporated on C-4 during oxidation with molecular oxygen-18 (1989) (4)
Evaluation of NAD(H) Analogues as Selective Inhibitors for Trypanosoma Cruzi S-Adenosylhomocysteine Hydrolase (2009) (4)
Importance of the aromatic ring in adrenergic amines. 8. 2-(Aminomethyl)-trans-2-decalols as inhibitors of norepinephrine N-methyltransferase. (1982) (4)
Catechol O-methyltransferase. 11. Inactivation by 5-hydroxy-3-mercapto-4-methoxybenzoic acid. (1982) (4)
Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using an acyloxyalkoxy promoiety. (1999) (4)
Independent synthesis of 5-hydroxytryptamine-4,7-dione - the neurocytotoxic product of autoxidation of 5,7-dihydroxytryptamine (1988) (4)
Phenol sulphotransferase: purification and characterization of the rat kidney and stomach enzymes. (1985) (4)
Substrate specificity of phenol sulfotransferase from primary cultures of bovine brain microvessel endothelium (1989) (4)
Academic pharmaceutics: The challenge of excellence (1990) (3)
Biotechnology : Pharmaceutical Aspects (2008) (3)
It is equally important to mention that the journal's impact as judged by "usage metrics" (i.e., article downloads) continued to grow significantly in 2010. (2011) (3)
Synthesis of an esterase-sensitive cyclic prodrug of a model hexapeptide having enhanced membrane permeability and enzymatic stability using a 3-(2'-hydroxy-4',6'-dimethylphenyl)-3,3-dimethyl propionic Acid promoiety. (1999) (3)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. 4. URTHER MODIFICATIONS OF THE AMINO ACID AND BASE PORTIONS F S-ADENOSYL-L-HOMOCYSTEINE (1976) (3)
Neplanocin A inhibition of S-adenosylhomocysteine hydrolase in Alcaligenes faecalis has no effect on growth of the microorganism. (1987) (3)
Targeted Drug Delivery (1991) (3)
Biochemistry of S-adenosylmethionine and related compounds : proceedings of a conference held at the Lake of the Ozarks (Missouri) on October 26-29, 1981 (1982) (3)
Stratigraphy and Evolution of the Upper Highland Crust Near North Ray, Apollo 16 (1981) (3)
Comparative kinetics of cofactor association and dissociation for the human and trypanosomal S-adenosylhomocysteine hydrolases. 3. Role of lysyl and tyrosyl residues of the C-terminal extension. (2010) (3)
Design and Biological Evaluation of New Mechanismbased Inhibitors of S-Adenosyl-L-homocysteine Hydrolase (1999) (3)
Precursor lithologies and metamorphic history of granulitic breccias from north ray crater, station 11, Apollo 16 (1987) (3)
SELECTIVE RING C-METHYLATION OF HYDROXYBENZALDEHYDES VIA THEIR MANNICH BASES (1983) (3)
Biotechnology : Pharmaceutical Aspects (2008) (3)
IMPORTANCE OF THE AROMATIC RING IN ADRENERGIC AMINES. PART 6. NONAROMATIC ANALOGUES OF PHENYLETHANOLAMINE AS INHIBITORS OF PHENYLETHANOLAMINE N-METHYLTRANSFERASE: ROLE OF Π-ELECTRONIC AND STERIC INTERACTIONS (1981) (3)
Neutral amino acid transport across brain microvessel endothelial cell monolayers (1986) (3)
Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of hydrophobic and steric interactions. (1981) (3)
Chair Report of the Research and Graduate Affairs Committee 1 (1996) (3)
An Efficient In Vitro Assay for Acetylcholinesterase Reactivators Using Immobilized Enzyme (1984) (3)
Selective Ring Omethylation of Hydroxybenzaldehydes Via Their Mannich Bases (1983) (3)
Simultaneous assay for mRNA (guanine-7-)-methyltransferase and mRNA(2'-O-nucleoside)methyltransferase of purified vaccinia (WR) virions. (1978) (3)
Rat kidney histamine N-methyltransferase: purification and partial characterization. (1985) (3)
Conformational aspects of systems related to acetylcholine. 4. The syntheses of the dl-2-dimethylamino-trans-decalin methiodides. (1972) (3)
A facilitated cyclic ether formation and its potential application in solid-phase peptide and organic synthesis. (2000) (3)
A conformational study of catecholamine receptor sites. 5. Syntheses of dl-3-amino-2-(3,4-dihydroxyphenyl)-trans-2-decalol hydrochlorides. (1971) (3)
Quantitation of S-adenosylhomocysteine hydrolase in mouse L929 cells using the inhibitor neplanocin A. (1985) (3)
POTENTIAL INHIBITORS OF S‐ADENOSYLMETHIONINE‐DEPENDENT METHYLTRANSFERASES PART 1, MODIFICATION OF THE AMINO ACID PORTION OF S‐ADENOSYLHOMOCYSTEINE (1974) (2)
Sulfate conjugation of catecholamines and their derivatives in monkey brain (1995) (2)
Mechanism of Action of S-Adenosyl-L-homocysteine Hydrolase. Measurement of Kinetic Isotope Effects Using Adenosine-3′-d and S-Adenosyl-L-homocysteine-3′-d as Substrates (1986) (2)
General methods for the preparation of α and/OR β deuterium labelled 6‐hydroxydopamine derivatives (1982) (2)
“Trimethyl lock” facilitated spirocyclizations: A structural analysis (1996) (2)
Novel esterase-sensitive cyclic prodrugs of a model hexapeptide having enhanced membrane permeability and enzymatic stability (1997) (2)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. PART 7. ROLE OF THE RIBOSYL MOIETY IN ENZYMATIC BINDING OF S-ADENOSYL-L-HOMOCYSTEINE AND S-ADENOSYL-L-METHIONINE (1979) (2)
Sulfation of catecholamines, hypertensive and hypotensive drugs by monkey brain cortex enzymes. (1993) (2)
Silica gel‐assisted reduction of nitrostyrenes to 2‐aryl‐2‐[2H]‐1‐nitroethanes with sodium borodeuteride (1983) (2)
Effects of phenylethanolamine N-methyltransferase inhibitors on uptake and release of norepinephrine and dopamine from rat brain. (1985) (2)
Synthesis of coumarin-based, esterase-sensitive cyclic prodrugs of opioid peptides with enhanced membrane permeability and enzymatic stability. (1999) (2)
Inhibitors of phenylethanolamine-N-methyltransferase: effects on brain catecholamine content and blood pressure in DOCA-salt hypertensive rats. (1984) (2)
An Efficient Method for the Conversion of Phenolic Mannich Bases to C-Methylated Phenols. Synthesis of 3,6-Dimethylcatechol (1983) (2)
Application of Cell Culture Systems to the Study of Drug Transport and Metabolism (1995) (2)
3-Substituted-4-methoxy-5-hydroxybenzaldehydes and benzoic acids as inhibitors of catechol-O-methyltransferase (1981) (2)
Metabolism of catecholamine esters by cultured bovine brain microvessel endothelial cells. (1989) (2)
Adenosine‐5′‐carboxaldehyde: A Potent Inhibitor of S‐Adenosyl‐L‐ homocysteine Hydrolase. (1994) (2)
Stereocontrolled Synthesis of Diene and Enyne Sugar-Modified Nucleosides and Their Interaction with S-Adenosyl-L-homocysteine Hydrolase (2003) (2)
Transmethylation : proceedings of the Conference on Transmethylation, Bethesda, Maryland, U.S.A., on October 16-19, 1978 (1979) (2)
Mechanism of inhibition of pineal hydroxyindole-O-methyltransferase by pyridoxal 5'-phosphate. (1978) (2)
Prodrug Strategies to Improve the Oral Absorption of Peptides and Peptide Mimetics (2000) (2)
Catechol O-methyltransferase. 9. Mechanism of inactivation by 6-hydroxydopamine (1977) (1)
Desilylation of tert‐Butyldimethylsilyl Ethers of Phenols. (1989) (1)
STEREOPOPULATION CONTROL PART 5, FACILITATION OF INTRAMOLECULAR CONJUGATE ADDITION OF AN ALDEHYDE HYDRATE AND HEMIACETAL (1974) (1)
IMPORTANCE OF THE AROMATIC RING IN ADRENERGIC AMINES. 7. COMPARISON OF THE STEREOSELECTIVITY OF NOREPINEPHRINE N-METHYLTRANSFERASE FOR AROMATICS. NONAROMATIC SUBSTRATES AND INHIBITORS (1983) (1)
ISOLATION AND CHARACTERIZATION OF THE METHYL ACCEPTOR PROTEIN FROM ADRENAL CHROMAFFIN GRANULES (1979) (1)
Educational and Communication Issues Related to Profiling Compounds for Their Drug‐Like Properties (2007) (1)
Accessory Minerals in North Ray Crater Breccias, Apollo 16 (1981) (1)
SILICA GEL ASSISTED REDUCTIVE CYCLIZATION OF ALKOXY-2, β-DINITROSTYRENES TO ALKOXYINDOLES (1984) (1)
Characterization of the unstirred water layer in cultured brain microvessel endothelial cells (1993) (1)
Facilitated Intramolecular Conjugate Addition of N‐(p‐Methoxyphenyl)‐3‐ (3′,6′‐dioxo‐2′,4′‐dimethylcyclohexa‐1′,4′‐dienyl)‐3,3‐ dimethylpropionamide. Part 1. Product Characterization. (1993) (1)
Effect of limited proteolysis on the stability and enzymatic activity of human placental S‐adenosylhomocysteine hydrolase (1997) (1)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. 10. ASE- AND AMINO ACID MODIFIED ANALOGS OF S-ARISTEROMYCINYL-L-HOMOCYSTEINE (1985) (1)
Value of Pharmaceutical Sciences (1997) (1)
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects. (2004) (1)
Synthesis of an Esterase‐Sensitive Cyclic Prodrug of a Model Hexapeptide Having Enhanced Membrane Permeability and Enzymic Stability Using a 3‐(2′‐Hydroxy‐4′,6′‐dimethylphenyl)‐3,3‐Dimethylpropionic Acid Promoiety (2000) (1)
Compounds for enzyme inhibition of proteasome. (2005) (1)
Carnosine as a substrate for the peptide carrier in Caco-2 cells (1993) (1)
Deamidation of model beta-turn cyclic peptides in the solid state. (2005) (1)
Mechanism of drug action. Edited by Thomas P. Singer, Tag E. Mansour, and Raul N. Ondarza. Academic Press, Inc., Orlando, FL 32887. 1983. 405 pp. 15.5 × 23 cm. $45.00 (1985) (1)
Mechanism and Products of Autoxidation of 5,7-Dihydroxytryptamine. (1986) (1)
Nucleic Acid Related Compounds. Part 80. Synthesis of 5′‐S‐(Alkyl and aryl)‐5′‐fluoro‐5′‐thioadenosines with Xenon Difluoride or ( Diethylamido)sulfur Trifluoride, Hydrolysis in Aqueous Buffer, and inhibition of S‐Adenosyl‐L‐homocysteine Hydrolase by Derived “ Adenosine 5′‐Aldehyde” Species. (1994) (1)
Sulfation of hypertensive and hypotensive drugs by monkey brain phenol sulfotransferase (1993) (1)
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. (1999) (1)
Can Metal Segregation Remove Siderophiles from Lunar Impact Melts (1982) (1)
Nucleic Acid Related Compounds. Part 99. Synthesis of Homologated Halovinyl Derivatives from Aristeromycin and Their Inhibition of Human Placental S-Adenosyl-L-homocysteine Hydrolase. (1998) (1)
Inhibition of Rous, sarcoma virus medicated cellular transformation by analogues of S-adenosyl-L-homocysteine (1982) (1)
Value of pharmaceutical sciences. (1998) (1)
Synthesis of methyl 5-O-acetyl-7-deoxy-2,3-O-isopropylidene-heptofuranosid-6-uloses☆ (1983) (1)
Editorial. (2015) (1)
Effect of ibopamine and the active metabolite epinine on the catecholamine content of rat hypothalamus and brainstem in vitro. (1988) (1)
Silica Gel-assisted Reduction of Nitrostyrenes to 2-Aryl-1-nitroalkanes with Sodium Borohydride. (1983) (1)
Carrier-Mediated Transport of Bile Acids and Amino Acids in Caco-2 Cells (1991) (1)
Regioselective syntheses of deuterium labelled 6‐hydroxydopamines (1983) (1)
Editorial: JPharmSci annually recognizes peer reviewers (2014). (2015) (1)
THE EFFECTS OF NONIONIC SURFACTANTS ON THE PERMEATION OF SOLUTES ACROSS CACO-2 CELL MONOLAYERS (1999) (1)
Biological Models to Assess Drug Bioavailability (2007) (1)
Synthesis of Hydroxylated Cyclohexenyl- and Cyclohexanyladenines as Potential Inhibitors of S-Adenosylhomocysteine Hydrolase. (1993) (1)
Efficient Enantioselective Syntheses of Carbocyclic Nucleoside and Prostaglandin Synthons. (1990) (1)
STRUCTURE OF HUMAN PLACENTAL S-ADENOSYLHOMOCYSTEINE HYDROLASE: DETERMINATION OF A 30 SELENIUM ATOM SUBSTRUCTURE FROM DATA AT A SINGLE WAVELENGTH (1999) (0)
Design and Synthesis of Amide Isosteres of Phe-Gly: Potential Peptidomimetic Ligands for the Intestinal Oligopeptide Transporter PepT1 (2001) (0)
Editorial. (2020) (0)
SOME NEW INHIBITORS OF EPINEPHRINE BIOSYNTHESIS. IMPORTANCE OF THE AROMATIC RING IN ADRENERGIC AMINES. 4. (Ref. 1) (1979) (0)
Labeling of catechol-O-methyltransferase with N-haloacetyl derivatives. (1977) (0)
Abstracts of lectures symposium disposition and delivery of peptide drugs (1988) (0)
CATECHOL O-METHYLTRANSFERASE. 7. AFFINITY LABELING WITH THE OXIDATION PRODUCTS OF 6-AMINODOPAMINE (1976) (0)
Human S-adenosylhomocysteine hydrolase complexed with neplanocin (2003) (0)
Synthesis of Coumarin‐Based, Esterase‐Sensitive Cyclic Prodrugs of Opioid Peptides with Enhanced Membrane Permeability and Enzymic Stability (2010) (0)
CATECHOL O‐METHYLTRANSFERASE PART 6, AFFINITY LABELING WITH N‐HALOACETYL‐3,5‐DIMETHOXY‐4‐HYDROXYPHENYLALKYLAMINES (1975) (0)
Compounds for proteasome inhibition of enzymes (2005) (0)
Silica Gel Assisted Reductive Cyclization of 2-Nitro-β-piperidinostyrenes (III), Derived from 2-Nitrotoluenes (I), to Indoles (IV). (1988) (0)
Composes d'inhibition enzymatique proteasome (2005) (0)
Abstracts of Dutch doctoral theses (2005) (0)
CATECHOL O-METHYLTRANSFERASE. 12. AFFINITY LABELING THE ACTIVE SITE WITH THE OXIDATION PRODUCTS OF 5,6-DIHYDROXYINDOLE (1982) (0)
Steric Hindrance is a Key Factor in the Coupling Reaction of (Acyloxy) Alkyl‐α‐halides with Phenols to Make a New Promoiety for Prodrugs. (2002) (0)
Protein Chemistry: Protein Methylation . Woon Ki Paik and Sangduk Kim. Wiley-Interscience, New York, 1980. xviii, 282 pp., illus. $27.50. Biochemistry, vol. 1. (1980) (0)
Mechanism of Autoxidation of 5,7‐Dihydroxytryptamine: Effect of Fluorine Substitution at Positions 4 and/or 6. (1991) (0)
AAPS Update (2006) (0)
-3-Deazaadenine: Analogs ofNeplanocin A WhichRetain Potent Antiviral Activity butExhibit ReducedCytotoxicity (1987) (0)
Editorial Invitation to Become a Reviewer for the Journal of Pharmaceutical Sciences. (2018) (0)
Protein transport through cultured brain microvessel endothelial cells, a model of the blood-brain barrier☆ (1990) (0)
In vitro cell culture systems to evaluate the enzymatic degradation of peptides and proteins (1994) (0)
Compounds for proteasomenzyminhibering (2005) (0)
AAPS Update (2005) (0)
Composes d'inhibition enzymatique (2005) (0)
Design and Biological Evaluation of New Mechanism-Based Inhibitors of S-Adenosyl-L-homocysteine Hydrolase (1999) (0)
Enantiospecific Syntheses of Aristeromycin and Neplanocin A. (2010) (0)
SYNTHESIS OF METHYL 5-O-ACETYL-7-DEOXY-2,3-O-ISOPROPYLIDENE-6-HEPTULO-1,4-FURANOSIDES (1984) (0)
IMPORTANCE OF THE AROMATIC RING IN ADRENERGIC AMINES. 8. 2-(AMINOMETHYL)-TRANS-2-DECALOLS AS INHIBITORS OF NOREPINEPHRINE N-METHYLTRANSFERASE (1983) (0)
Enzyme Chemistry: Impact and Applications (1986) (0)
NEW APPROACHES TO CONTROLLING THE ACTIVITY OF PHENYLETHANOLAMINE N-METHYLTRANSFERASE IN STRESS (1976) (0)
At the time, Dr. Middaugh was a senior scientist in pharmaceutical research and vaccine development at Merck and Company. (2014) (0)
Development of a Novel Redox-Sensitive Protecting Group for Amines Which Utilizes a Facilitated Lactonization Reaction. (1995) (0)
Textural and modal analysis of Apollo 16 and 17 highland breccias (1980) (0)
Impact of Journal of Pharmaceutical Sciences. (2008) (0)
Delivering peptides and peptidomimetics across membrane barriers: A prodrug approach (2002) (0)
Journal of Pharmaceutical Sciences. Editorial. (2010) (0)
The term of these individuals will expire on December 31, 2013. (2014) (0)
Protein chemistry. (1980) (0)
Role of brain epinephrine neurons in the regulation of serum prolactin and luteinizing hormone release in female rats. (1985) (0)
MOLECULAR MECHANISM OF ACTION OF 5,6-DIHYDROXYTRYPTAMINE. SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-METHYL-, 7-METHYL- AND 4,7-DIMETHYL-5,6-DIHYDROXYTRYPTAMINES (1985) (0)
Secondary structure of a dynamic type I'beta-hairpin peptide. (2004) (0)
Enzymatic compounds for proteasome inhibition (2005) (0)
Acid Related Compounds . 84 . Synthesis of 6 ’ 4 E and 2 )-Halohomovinyl Derivatives of Adenosine , Inactivation of S-Adenosyl-L-homocysteine Hydrolase , and Correlation of Anticancer and Antiviral Potencies with Enzyme Inhibition 1 (2001) (0)
Serotonin uptake in neuroblastoma and phenochromocytoma cells. Abstr. (1981) (0)
The "Ten Most Highly Cited Articles" and the "Ten Most Frequently Downloaded Articles" in the Journal of Pharmaceutical Sciences. (2012) (0)
Professor Benet is considered by his peers to be one of the “founding fathers” of the modern pharmaceutical sciences. (2012) (0)
Rational strategies to enhance the intestinal permeability of peptides (1994) (0)
AAPS Update (2005) (0)
CATECHOL O-METHYLTRANSFERASE. 10. 5-SUBSTITUTED, 3-HYDROXY-4-METHOXYBENZOIC ACIDS (ISOVANILLIC ACIDS) AND 5-SUBSTITUTED, 3-HYDROXY-4-METHOXYBENZALDEHYDES (ISOVANILLINS) AS POTENTIAL INHIBITORS (1982) (0)
The Design, Synthesis and Screening of Potential Pyridinium Oxime Prodrugs. (1985) (0)
Nature of the Apollo 16 Subregolith Basement as Deduced from the Composition of Large Impact Glass Samples (1982) (0)
A Convenient Method for the Synthesis of Indole‐3‐acetic Acids. (1994) (0)
An analytical method for simultaneously assessing biological and physical barriers of the rat intestinal mucosa (2006) (0)
Catechol O-methyltransferase. 8. Structure-activity relationships for inhibtion by 8-hydroxyquinolines. (1976) (0)
Combined Modulation of 5-AdenosyImethionine Biosynthesis and 5-Adenosylhomocysteine Metabolism Enhances Inhibition of Nucleic Acid Methylation and LI 210 Cell Growth1 (2006) (0)
Facilitated Intramolecular Conjugate Addition of Amides of 3‐(3′,6′‐ Dioxo‐2′,4′‐dimethyl‐1′,4′‐cyclohexadienyl)‐3,3‐dimethylpropionic Acid. Part 2. Kinetics of Degradation. (1997) (0)
SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2- AND 4-SUBSTITUTED 6,7-DIHYDROXY-1,2,3,4-TETRAHYDROISOQUINOLINES (1976) (0)
Journal of Pharmaceutical Sciences. Editorial. (2010) (0)
Editorial. (2019) (0)
Evaluation of a Vitamin‐Cloaking Strategy for Oligopeptide Therapeutics: Biotinylated HIV‐1 Protease Inhibitors. (1994) (0)
tert-Butyldimethylsilyl Ethers of Phenols: Their One-Step Conversion to Benzyl or Methyl Ethers and Utility in Regioselective ortho Lithiation. (1988) (0)
4354 Antiviral Action (2001) (0)
Short Communication (1' R,2'5,3'R)-9-(2',3' -Dihydroxycyclopentan-1'-yl)-ade nine and -3-deaza-adenine: analogues of aristeromycin which exhibit potent antiviral activity with reduced cytotoxicity (1993) (0)
United States Patent ( 19 ) Hider et al . ( 54 ) NOVEL 3-HYDROXYPYRID-2-ONES AND 3-HYDROXYPRD-4-ONES USEFUL IN TREATING PATENTS HAVING ATOXC CONCENTRATION OF IRON (2017) (0)
Editorial: 10 most accessed and the 10 most cited papers. (2015) (0)
Editorial. (2020) (0)
A possible involvement of mRNA-methyltransferases in the initiation of RNA synthesis by cytoplasmic polyhedrosis virus of Bombyx mori. (1980) (0)
Editorial. Gordon L. Amidon Dedicated Issue. (2014) (0)
Professor Benet’s contributions to the pharmaceutical sciences. (2013) (0)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. 9. ′,3′-DIALDEHYDE DERIVATIVES OF CARBOCYCLIC PURINE NUCLEOSIDES AS INHIBITO S OF S-ADENOSYLHOMOCYSTEINE HYDROLASE (1985) (0)
The 2013 Ebert Prize was presented to Professor Benet and his coauthor Dr. Reyes. (2013) (0)
Synthesis and Antiviral Activity of [2-[[4-[3-[(1-Methylethyl)amino]-2-Pyridyl]-1-Piperazinyl]Carbonyl]-1H-Indol-5-yl] (BHAP) Acylsphingosine HIV Reverse Transcriptase Inhibitors (1995) (0)
Editorial: Marcus E. Brewster. (2014) (0)
DIRECTIONAL PROBES OF THE HYDROPHOBIC COMPONENT OF THE AROMATIC RING BINDING SITE OF NOREPINEPHRINE N-METHYLTRANSFERASE (1983) (0)
CONVENIENT PREPARATION OF S-ADENOSYLHOMOCYSTEINE AND RELATED COMPOUNDS (1976) (0)
Phosphate prodrugs of amines which utilize a fast hydroxy-amide lactonization Structural specificity for alkaline phosphatase (1995) (0)
This honor is being bestowed on Professor Stella because of his numerous and significant contributions to research, teaching, and service in the pharmaceutical sciences. (2011) (0)
HISTAMINE N-METHYLTRANSFERASE. INHIBITION AND POTENTIATION BY TRANS- AND CIS-1,5-DIPHENYLAMINOPYRROLIDINE (1974) (0)
Docking strategies: binding of substrate and inhibitors to S-adenoslyhomocysteine hydrolase - a case study (2001) (0)
POTENTIAL INHIBITORS OF S-ADENOSYLMETHIONINE-DEPENDENT METHYLTRANSFERASES. 8. OLECULAR DISSECTIONS OF CARBOCYCLIC 3-DEAZAADENOSINE AS INHIBITORS F S-ADENOSYLHOMOCYSTEINE HYDROLASE (1985) (0)
Synthesis of an Esterase‐Sensitive Cyclic Prodrug of a Model Hexapeptide Having Enhanced Membrane Permeability and Enzymatic Stability Using an Acyloxyalkoxy Promoiety (2000) (0)
2009 Ebert Prize. Editorial. (2009) (0)
Composes pour l'inhibition enzymatique (2005) (0)
Compounds for proteasomenzymhemmung (2005) (0)
The Ebert Prize was established in 1873 and it is the oldest pharmacy award in existence in the United States. (2014) (0)
Editorial. (2019) (0)
A 9-Step Enantiospecific Synthesis of (-)-Aristeromycin (II) from D-Ribonic Acid γ-Lactone (I). (1989) (0)
Synthesis and Biological Evaluation of 4-Fluoro-, 7-Fluoro-, and 4,7- Difluoro-5,6-dihydroxytryptamines. (1991) (0)
PROBES OF THE ACTIVE SITE OF NOREPINEPHRINE N-METHYLTRANSFERASE: EFFECT OF HYDROPHOBIC AND HYDROPHILIC INTERACTIONS ON SIDE-CHAIN BINDING OF AMPHETAMINE AND α-METHYLBENZYLAMINE (1983) (0)
Editorial: the ten most highly cited articles. (2014) (0)
, Thomas P. Singer, Tag E. Mansour, Raul N. Ondarza (Eds.). Academic Press, Inc., Orlando (1983), 405, , cm. $45.00 (1985) (0)
Interview with a Distinguished Pharmaceutical Scientist: Ronald T. Borchardt, Ph.D., Recipient of the 1997 AAPS Distinguished Pharmaceutical Scientist Award (1997) (0)
DIFFERENT ISOTOPE EFFECTS FOR PARALLEL PATHWAYS OF ENZYME-CATALYZED TRANSMETHYLATION (1984) (0)
A comprehensive analysis of the scientific scope of the papers. (2013) (0)
Independent Synthesis of 5-Hydroxytryptamine-4,7-dione (XIX). The Neurocytotoxic Product of Autoxidation of 5,7-Dihydroxytryptamine. (1989) (0)
Enzymatic degradation of delta-sleep inducing peptide in an epithelial cell culture model (1994) (0)
Provenance of the Apollo 16 Feldspathic Fragmental Breccias at North Ray Crater (1981) (0)
Editorial Invitation to Become a Reviewer for the Journal of Pharmaceutical Sciences. (2018) (0)
STEREOPOPULATION CONTROL PART 6, CONFORMATIONAL SELECTION OF ALTERNATIVE OXIDATION PATHWAYS (1974) (0)
Prodrug strategies to enhance the permeation of peptides through the intestinal mucosa (2002) (0)
Synthesis and Evaluation of Novel Coumarin-Based Esterase-Sensitive Cyclic Prodrugs of Peptidomimetic RGD Analogues with Improved Membrane Permeability. (1999) (0)
The use of phenylethanolamine N-methyltransferase inhibitors in elucidating the role of brain epinephrine in the control of cardiovascular function (1982) (0)

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