Daria Hazuda
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US biochemist
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Daria Hazudabiology Degrees
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Biochemistry
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Biology
Daria Hazuda's Degrees
- PhD Biochemistry University of California, Berkeley
- Bachelors Chemistry Stanford University
Why Is Daria Hazuda Influential?
(Suggest an Edit or Addition)According to Wikipedia, Daria J Hazuda is a biochemist known for discovering the first HIV Integrase Strand Transfer Inhibitors and leading the development of the first HIV integrase inhibitor to gain FDA approval, Isentress . Her lab also determined these inhibitors' mechanism of action and ways the virus could develop resistance to them. Hazuda has also performed extensive research and led the development of antivirals for Hepatitis C Virus including Elbasvir and Grazoprevir. She currently serves as Vice President for Infectious Diseases Discovery for Merck and Chief Scientific Officer of their MRL Cambridge Exploratory Science Center.
Daria Hazuda'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
- Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. (2000) (1100)
- The Challenge of Finding a Cure for HIV Infection (2009) (879)
- Genome-scale RNAi screen for host factors required for HIV replication. (2008) (808)
- HIV-1 antiretroviral drug therapy. (2012) (751)
- Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. (2008) (582)
- Raltegravir with optimized background therapy for resistant HIV-1 infection. (2008) (570)
- P-TEFb kinase is required for HIV Tat transcriptional activation in vivo and in vitro. (1997) (544)
- Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. (2008) (544)
- Host Cell Factors in HIV Replication: Meta-Analysis of Genome-Wide Studies (2009) (462)
- Activation of HIV Transcription with Short-Course Vorinostat in HIV-Infected Patients on Suppressive Antiretroviral Therapy (2014) (428)
- Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes (2002) (384)
- Expression of latent HIV induced by the potent HDAC inhibitor suberoylanilide hydroxamic acid. (2009) (358)
- HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. (2000) (328)
- Characterization of Resistance to Non-obligate Chain-terminating Ribonucleoside Analogs That Inhibit Hepatitis C Virus Replication in Vitro* (2003) (319)
- A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. (2004) (314)
- Integrase Inhibitors and Cellular Immunity Suppress Retroviral Replication in Rhesus Macaques (2004) (305)
- Xenopus transcription factor A requires zinc for binding to the 5 S RNA gene. (1983) (277)
- MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants (2012) (234)
- Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. (2003) (233)
- HIV-1 expression within resting CD4+ T cells after multiple doses of vorinostat. (2014) (229)
- A Novel Assay to Measure the Magnitude of the Inducible Viral Reservoir in HIV-infected Individuals (2015) (228)
- A 7-Deaza-Adenosine Analog Is a Potent and Selective Inhibitor of Hepatitis C Virus Replication with Excellent Pharmacokinetic Properties (2004) (223)
- Processing of precursor interleukin 1 beta and inflammatory disease. (1990) (220)
- The kinetics of interleukin 1 secretion from activated monocytes. Differences between interleukin 1 alpha and interleukin 1 beta. (1988) (219)
- c-Myc and Sp1 Contribute to Proviral Latency by Recruiting Histone Deacetylase 1 to the Human Immunodeficiency Virus Type 1 Promoter (2007) (212)
- Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase (2007) (203)
- Latency reversal and viral clearance to cure HIV-1 (2016) (199)
- A Limited Group of Class I Histone Deacetylases Acts To Repress Human Immunodeficiency Virus Type 1 Expression (2009) (198)
- Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial. (2011) (191)
- 4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells. (2000) (189)
- Loss of Raltegravir Susceptibility by Human Immunodeficiency Virus Type 1 Is Conferred via Multiple Nonoverlapping Genetic Pathways (2009) (181)
- Inhibition of cap (m7GpppXm)-dependent endonuclease of influenza virus by 4-substituted 2,4-dioxobutanoic acid compounds (1994) (177)
- Expression of latent human immunodeficiency type 1 is induced by novel and selective histone deacetylase inhibitors (2009) (162)
- Probiotic/prebiotic supplementation of antiretrovirals improves gastrointestinal immunity in SIV-infected macaques. (2013) (157)
- A human monoclonal antibody neutralizes diverse HIV-1 isolates by binding a critical gp41 epitope. (2005) (156)
- Presenilin-1 and Presenilin-2 Exhibit Distinct yet Overlapping γ-Secretase Activities* (2003) (146)
- Inhibition of HIV-1 Ribonuclease H by a Novel Diketo Acid, 4-[5-(Benzoylamino)thien-2-yl]-2,4-dioxobutanoic Acid* (2003) (144)
- Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase (1998) (135)
- Replication Fitness and NS5B Drug Sensitivity of Diverse Hepatitis C Virus Isolates Characterized by Using a Transient Replication Assay (2005) (127)
- MK-7009, a Potent and Selective Inhibitor of Hepatitis C Virus NS3/4A Protease (2009) (126)
- PD-1 blockade potentiates HIV latency reversal ex vivo in CD4+ T cells from ART-suppressed individuals (2019) (125)
- SARS-CoV-2 tropism, entry, replication, and propagation: Considerations for drug discovery and development. (2021) (121)
- PD-1 Blockade in Rhesus Macaques: Impact on Chronic Infection and Prophylactic Vaccination (2009) (118)
- Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties. (2005) (114)
- A novel assay for the DNA strand-transfer reaction of HIV-1 integrase. (1994) (111)
- First Demonstration of Cerebrospinal Fluid and Plasma Aβ Lowering with Oral Administration of a β-Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates (2009) (109)
- A deep learning genome-mining strategy for biosynthetic gene cluster prediction (2019) (108)
- X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform. (2000) (108)
- HIV-1 Reverse Transcriptase Plus-strand Initiation Exhibits Preferential Sensitivity to Non-nucleoside Reverse Transcriptase Inhibitors in Vitro* (2007) (105)
- LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease (2006) (101)
- Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase (1997) (97)
- Natural Polymorphisms of Human Immunodeficiency Virus Type 1 Integrase and Inherent Susceptibilities to a Panel of Integrase Inhibitors (2009) (93)
- Robust Antiviral Efficacy upon Administration of a Nucleoside Analog to Hepatitis C Virus-Infected Chimpanzees (2008) (92)
- CD32 is expressed on cells with transcriptionally active HIV but does not enrich for HIV DNA in resting T cells (2018) (89)
- Structural Basis for the Inhibition of RNase H Activity of HIV-1 Reverse Transcriptase by RNase H Active Site-Directed Inhibitors (2010) (89)
- Identification of Novel Mutations Responsible for Resistance to MK-2048, a Second-Generation HIV-1 Integrase Inhibitor (2010) (87)
- In Vitro Characterization of MK-1439, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor (2013) (86)
- Isolation and Characterization of Novel Human Immunodeficiency Virus Integrase Inhibitors from Fungal Metabolites (1999) (84)
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes. (2001) (83)
- Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites (2003) (82)
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes. (2001) (82)
- Emerging pharmacology: inhibitors of human immunodeficiency virus integration. (2009) (81)
- Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1). (2006) (79)
- Macrocyclic Inhibitors of β-Secretase: Functional Activity in an Animal Model. (2006) (79)
- In Vitro Resistance Selection with Doravirine (MK-1439), a Novel Nonnucleoside Reverse Transcriptase Inhibitor with Distinct Mutation Development Pathways (2014) (77)
- Analysis of boceprevir resistance associated amino acid variants (RAVs) in two phase 3 boceprevir clinical studies. (2013) (75)
- Recommendations for measuring HIV reservoir size in cure-directed clinical trials (2020) (74)
- Dissecting the effects of DNA polymerase and ribonuclease H inhibitor combinations on HIV-1 reverse-transcriptase activities. (2005) (74)
- Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors. (2007) (72)
- Host-cell positive transcription elongation factor b kinase activity is essential and limiting for HIV type 1 replication. (1999) (72)
- Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities. (2003) (71)
- Ultra-long-acting tunable biodegradable and removable controlled release implants for drug delivery (2019) (70)
- Doravirine Suppresses Common Nonnucleoside Reverse Transcriptase Inhibitor-Associated Mutants at Clinically Relevant Concentrations (2016) (69)
- Modified mRNA/lipid nanoparticle-based vaccines expressing respiratory syncytial virus F protein variants are immunogenic and protective in rodent models of RSV infection (2020) (68)
- Human interleukin 1 beta is not secreted from hamster fibroblasts when expressed constitutively from a transfected cDNA (1988) (68)
- Structure-function mapping of interleukin 1 precursors. Cleavage leads to a conformational change in the mature protein. (1991) (66)
- Inhibition of human immunodeficiency virus integrase by bis-catechols (1995) (64)
- β-Secretase Cleavage at Amino Acid Residue 34 in the Amyloid β Peptide Is Dependent upon γ-Secretase Activity* (2003) (61)
- Structure and absolute stereochemistry of HIV-1 integrase inhibitor integric acid. A novel eremophilane sesquiterpenoid produced by a Xylaria sp. (1999) (60)
- The role of manganese in promoting multimerization and assembly of human immunodeficiency virus type 1 integrase as a catalytically active complex on immobilized long terminal repeat substrates (1996) (59)
- Altering Expression Levels of Human Immunodeficiency Virus Type 1 gp120-gp41 Affects Efficiency but Not Kinetics of Cell-Cell Fusion (2002) (59)
- Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integrase. (2002) (57)
- Combined approaches for HIV cure (2013) (57)
- 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity. (2001) (56)
- Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones. (2007) (56)
- HDAC inhibition induces HIV-1 protein and enables immune-based clearance following latency reversal. (2017) (55)
- Sustained Viral Response in a Hepatitis C Virus-Infected Chimpanzee via a Combination of Direct-Acting Antiviral Agents (2010) (55)
- HIV integrase as a target for antiretroviral therapy (2012) (55)
- A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells. (2005) (55)
- Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase. (2008) (55)
- Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold. (2010) (54)
- Analysis of Low-Frequency Mutations Associated with Drug Resistance to Raltegravir before Antiretroviral Treatment (2010) (54)
- Differentiation into an Effector Memory Phenotype Potentiates HIV-1 Latency Reversal in CD4+ T Cells (2019) (54)
- Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes. (2001) (54)
- The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons (2016) (51)
- BACE-1 inhibition by a series of ψ[CH2NH] reduced amide isosteres (2006) (51)
- In vivo analysis of the effect of panobinostat on cell-associated HIV RNA and DNA levels and latent HIV infection (2016) (49)
- Raltegravir: the first HIV‐1 integrase strand transfer inhibitor in the HIV armamentarium (2011) (48)
- siRNA Screening of a Targeted Library of DNA Repair Factors in HIV Infection Reveals a Role for Base Excision Repair in HIV Integration (2011) (47)
- Viral long terminal repeat substrate binding characteristics of the human immunodeficiency virus type 1 integrase. (1994) (47)
- Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors. (2007) (44)
- Postexposure Protection of Macaques from Vaginal SHIV Infection by Topical Integrase Inhibitors (2014) (44)
- HIV resistance to the fusion inhibitor enfuvirtide: mechanisms and clinical implications. (2004) (44)
- Inhibition of Human Immunodeficiency Virus Type 1 Concerted Integration by Strand Transfer Inhibitors Which Recognize a Transient Structural Intermediate (2007) (44)
- Biochemical and cell-based assays for characterization of BACE-1 inhibitors. (2005) (44)
- Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection. (2001) (43)
- Generation of SARS-CoV-2 reporter replicon for high-throughput antiviral screening and testing (2021) (42)
- Purification and characterization of human recombinant precursor interleukin 1 beta. (1989) (42)
- Distinct Mutation Pathways of Non-Subtype B HIV-1 during In Vitro Resistance Selection with Nonnucleoside Reverse Transcriptase Inhibitors (2010) (41)
- Effect of Suberoylanilide Hydroxamic Acid (SAHA) Administration on the Residual Virus Pool in a Model of Combination Antiretroviral Therapy-Mediated Suppression in SIVmac239-Infected Indian Rhesus Macaques (2014) (41)
- Cooperative interactions between replication origin-bound molecules of herpes simplex virus origin-binding protein are mediated via the amino terminus of the protein. (1992) (40)
- Compounds That Bind APP and Inhibit Aβ Processing in Vitro Suggest a Novel Approach to Alzheimer Disease Therapeutics* (2005) (40)
- Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection. (2001) (39)
- 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains. (2003) (38)
- A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors. (2006) (38)
- Potential new therapies for the treatment of HIV-1 infection. (2002) (37)
- The Base Excision Repair Pathway Is Required for Efficient Lentivirus Integration (2011) (37)
- Four novel bis-(naphtho-γ-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase (2003) (37)
- Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity. (2000) (37)
- Characterization of the herpes simplex virus origin binding protein interaction with OriS. (1991) (37)
- Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase. (2002) (37)
- Integrastatins: structure and HIV-1 integrase inhibitory activities of two novel racemic tetracyclic aromatic heterocycles produced by two fungal species (2002) (36)
- Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains. (2004) (35)
- Antiviral Activity of MK-4965, a Novel Nonnucleoside Reverse Transcriptase Inhibitor (2009) (34)
- The DNA binding domain of herpes simplex virus type 1 origin binding protein is a transdominant inhibitor of virus replication. (1993) (34)
- Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment. (2004) (34)
- Combinatorial synthesis of CCR5 antagonists. (2001) (33)
- Rational design and synthesis of selective BACE-1 inhibitors. (2004) (33)
- Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds. (2004) (33)
- 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV. (2002) (33)
- Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp. (2003) (32)
- A presenilin‐independent aspartyl protease prefers the γ‐42 site cleavage (2006) (32)
- 8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors. (2007) (31)
- Isolation, Structure, and HIV‐1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum. (2004) (31)
- Resistance to HIV integrase strand transfer inhibitors: in vitro findings and clinical consequences. (2014) (29)
- CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines. (2002) (28)
- A potent and orally active HIV-1 integrase inhibitor. (2007) (28)
- Long-acting formulations for the treatment of latent tuberculous infection: opportunities and challenges. (2018) (27)
- Resistance-Associated Amino Acid Variants Associated with Boceprevir plus Pegylated Interferon-α2B and Ribavirin in Patients with Chronic Hepatitis C in the Sprint-1 Trial (2013) (26)
- Report of the National Institutes of Health SARS-CoV-2 Antiviral Therapeutics Summit (2021) (26)
- Resistance to inhibitors of the human immunodeficiency virus type 1 integration. (2010) (25)
- Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors. (2007) (25)
- Novel mutations introduced at the β-site of amyloid β protein precursor enhance the production of amyloid β peptide by BACE1 in vitro and in cells (2005) (25)
- A long-acting formulation of the integrase inhibitor raltegravir protects humanized BLT mice from repeated high-dose vaginal HIV challenges. (2016) (25)
- Human Immunodeficiency Virus Type 1 (HIV-1) Integration: a Potential Target for Microbicides To Prevent Cell-Free or Cell-Associated HIV-1 Infection (2008) (25)
- Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp. (2003) (25)
- Isolation, Structure, and HIV‐1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum (2003) (24)
- Processing of Precursor Interleukin 18 and Inflammatory Disease * (2001) (24)
- 1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains. (2003) (24)
- A genome wide analysis of ubiquitin ligases in APP processing identifies a novel regulator of BACE1 mRNA levels (2006) (24)
- Modified mRNA/lipid nanoparticle-based vaccines expressing respiratory syncytial virus F protein variants are immunogenic and protective in rodent models of RSV infection (2020) (23)
- Discovery, structure and HIV-1 integrase inhibitory activities of integracins, novel dimeric alkyl aromatics from Cytonaema sp. (2002) (23)
- Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide. (2004) (23)
- Title: Once-weekly Oral Dosing of MK-8591 Protects Male Rhesus Macaques from Intrarectal SHIV109CP3 Challenge. (2020) (23)
- Characterization of a soluble stable human cytomegalovirus protease and inhibition by M-site peptide mimics (1996) (22)
- SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition. (2010) (22)
- New antiretroviral agents: looking beyond protease and reverse transcriptase. (2001) (21)
- Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors. (2010) (20)
- Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane. (2005) (20)
- Immunogenicity generated by mRNA vaccine encoding VZV gE antigen is comparable to adjuvanted subunit vaccine and better than live attenuated vaccine in nonhuman primates. (2020) (20)
- Gene expression profiling of rat liver reveals a mechanistic basis for ritonavir-induced hyperlipidemia. (2007) (20)
- Follicular T cells optimize the germinal center response to SARS-CoV-2 protein vaccination in mice (2022) (20)
- Equivalent inhibition of half-site and full-site retroviral strand transfer reactions by structurally diverse compounds (1997) (20)
- Emergence of resistance-associated variants after failed triple therapy with vaniprevir in treatment-experienced non-cirrhotic patients with hepatitis C-genotype 1 infection: a population and clonal analysis. (2013) (20)
- MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants (2014) (19)
- Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors. (2015) (19)
- Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. (2006) (19)
- Discovery of natural product inhibitors of HIV-1 integrase at Merck (2005) (19)
- Monitoring the development of non-nucleoside reverse transcriptase inhibitor-associated resistant HIV-1 using an electrochemiluminescence-based reverse transcriptase polymerase assay. (2008) (19)
- Discovery and analysis of inhibitors of the human immunodeficiency integrase. (1997) (18)
- A genotype 2b NS5B polymerase with novel substitutions supports replication of a chimeric HCV 1b:2b replicon containing a genotype 1b NS3-5A background. (2006) (18)
- Mechanisms of Human Immunodeficiency Virus Type 1 Concerted Integration Related to Strand Transfer Inhibition and Drug Resistance (2008) (18)
- Effects of Treatment with Suppressive Combination Antiretroviral Drug Therapy and the Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid; (SAHA) on SIV-Infected Chinese Rhesus Macaques (2014) (18)
- The application potential of machine learning and genomics for understanding natural product diversity, chemistry, and therapeutic translatability. (2020) (17)
- Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors. (2008) (17)
- 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity. (2002) (17)
- Isolation, structure and HIV-1 integrase inhibitory activity of exophillic acid, a novel fungal metabolite from Exophiala pisciphila. (2003) (17)
- A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage. (2006) (16)
- Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products. (2003) (16)
- [791] HCV ANTIVIRAL ACTIVITY AND RESISTANCE ANALYSIS IN CHRONICALLY INFECTED CHIMPANZEES TREATED WITH NS3/4A PROTEASE AND NS5B POLYMERASE INHIBITORS (2007) (16)
- Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor. (2004) (16)
- Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase. (2008) (16)
- Active evolution of memory B-cells specific to viral gH/gL/pUL128/130/131 pentameric complex in healthy subjects with silent human cytomegalovirus infection. (2017) (15)
- Innovation and greater probability of success in drug discovery and development -- from target to biomarkers. (2005) (15)
- Mechanistic Study of Common Non-Nucleoside Reverse Transcriptase Inhibitor-Resistant Mutations with K103N and Y181C Substitutions (2016) (15)
- Total synthesis, characterization, and conformational analysis of the naturally occurring hexadecapeptide integramide A and a diastereomer. (2010) (15)
- Derivatives of Mesoxalic Acid Block Translocation of HIV-1 Reverse Transcriptase* (2014) (13)
- Scintillation proximity assays for mechanistic and pharmacological analyses of HIV-1 integration. (2009) (13)
- Assessment of the susceptibility of mutant HIV-1 to antiviral agents. (2010) (12)
- A human monoclonal antibody neutralizes diverse HIV-1 isolates by binding a critical gp 41 epitope (2005) (12)
- Pharmacodynamic Analysis of a Serine Protease Inhibitor, MK-4519, against Hepatitis C Virus Using a Novel In Vitro Pharmacodynamic System (2011) (12)
- Identification of proximal biomarkers of PKC agonism and evaluation of their role in HIV reactivation (2017) (12)
- CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity. (2003) (12)
- Detection of Cell-Cell Interactions via Photocatalytic Cell Tagging (2021) (12)
- 10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants. (2008) (12)
- Antiviral Activity and In Vitro Mutation Development Pathways of MK-6186, a Novel Nonnucleoside Reverse Transcriptase Inhibitor (2012) (11)
- Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists. (2004) (11)
- BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres. (2006) (11)
- Xenopus transcription factor A promotes DNA reassociation. (1985) (11)
- Novel mutations introduced at the beta-site of amyloid beta protein precursor enhance the production of amyloid beta peptide by BACE1 in vitro and in cells. (2005) (11)
- Development of boceprevir: a first‐in‐class direct antiviral treatment for chronic hepatitis C infection (2013) (10)
- Rational Design of Doravirine: From Bench to Patients. (2020) (10)
- Analysis of Resistance to the HIV-1 Integrase Inhibitor Raltegravir: Results from the Benchmrk 1 and 2 (2008) (10)
- Inhibitors of human immunodeficiency virus integration (2003) (10)
- MK-8591 Potency and PK Provide High Inhibitory Quotients at Low Doses QD and QW (10)
- Active evolution of memory B-cells specific to viral gH/gL/pUL128/130/131 pentameric complex in healthy subjects with silent human cytomegalovirus infection (2017) (9)
- Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV. (2017) (9)
- DNA-activated ATPase activity associated with Xenopus transcription factor A. (1986) (9)
- Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase. (2003) (9)
- Complete Absolute Configuration of Integramide A, a Natural, 16‐mer Peptide Inhibitor of HIV‐1 Integrase, Elucidated by Total Synthesis (2009) (9)
- Discovery, Structure and HIV‐1 Integrase Inhibitory Activities of Integracins, Novel Dimeric Alkyl Aromatics from Cytonaema sp. (2002) (9)
- Evolution of the D-ribose operon on Escherichia coli B/r (1982) (9)
- Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development (2020) (9)
- Purification of untagged HIV-1 reverse transcriptase by affinity chromatography. (2010) (8)
- Inhibitors of human immunodeficiency virus type I integration (2006) (8)
- Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain. (1999) (8)
- Failure of AZT: A molecular perspective (1997) (8)
- Improved Detection of HIV Gag p24 Protein Using a Combined Immunoprecipitation and Digital ELISA Method (2021) (8)
- Dissecting Tn5 transposition using HIV-1 integrase diketoacid inhibitors. (2007) (7)
- Differentiation to an effector memory phenotype potentiates HIV-l latency reversal in CD4+ T cells (2019) (7)
- Interleukin-10 contributes to reservoir establishment and persistence in SIV-infected macaques treated with antiretroviral therapy (2022) (7)
- Four Novel Bis‐(naphtho‐γ‐pyrones) Isolated from Fusarium Species as Inhibitors of HIV‐1 Integrase. (2003) (6)
- Correction to Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors. (2016) (6)
- Gag p24 is a Marker of HIV Expression in Tissues and Correlates with Immune Response. (2021) (6)
- Developing and applying ultrasensitive p24 protein immunoassay for HIV latency (2015) (6)
- 1208 EVALUATION OF NS3 AMINO ACID VARIANTS IN A PHASE 1B STUDY OF GENOTYPE 1 (GT1) AND GT3 INFECTED PATIENTS WITH THE HCV PROTEASE INHIBITOR, MK-5172 (2012) (6)
- 433 FREQUENCIES OF RESISTANCE-ASSOCIATED AMINO ACID VARIANTS DETECTED BY 454-SEQUENCING DURING COMBINATION TREATMENT WITH BOCEPREVIR PLUS PEGINTRON (PEGINTERFERON ALFA-2B)/RIBAVIRIN IN HCV (GT1)-INFECTED PATIENTS (2011) (6)
- 39 MK-5172: A NOVEL HCV NS3/4A PROTEASE INHIBITOR WITH POTENT ACTIVITY AGAINST KNOWN RESISTANCE MUTANTS (2010) (5)
- Design of a Multiuse Photoreactor To Enable Visible‐Light Photocatalytic Chemical Transformations and Labeling in Live Cells (2020) (5)
- Identification of novel bifunctional HIV-1 reverse transcriptase inhibitors (2018) (5)
- Effect of SAHA administration on the residual virus pool in a model of combination (2014) (5)
- IL-10 driven memory T cell survival and Tfh differentiation promote HIV persistence (2021) (5)
- 543. Molnupiravir Maintains Antiviral Activity Against SARS-CoV-2 Variants In Vitro and in Early Clinical Studies (2021) (5)
- O6 Single doses as low as 0.5 mg of the novel NRTTI MK-8591 suppress HIV for at least 7 days (2017) (4)
- Impact of HIV-1 Resistance-Associated Mutations on Susceptibility to Doravirine: Analysis of Real-World Clinical Isolates (2021) (4)
- Structure, Stereochemistry, and Biological Activity of Integramycin, a Novel Hexacyclic Natural Product Produced by Actinoplanes sp. that Inhibits HIV‐1 Integrase. (2002) (4)
- Preliminary Acceptability of a Home-Based Peripheral Blood Collection Device for Viral Load Testing in the Context of Analytical Treatment Interruptions in HIV Cure Trials: Results from a Nationwide Survey in the United States (2022) (4)
- Frequencies of Resistance-Associated Amino Acid Variants Detected by 454 Sequencing During Combination Treatment With Boceprevir Plus Pegintron (Peginterferon Alfa-2B)/Ribavirin in HCV (G1)-Infected Patients (2011) (4)
- Primer ID Ultra-Deep Sequencing Reveals Dynamics of drug Resistance-Associated Variants in Breakthrough Hepatitis C Viruses: Relevance to Treatment Outcome and Resistance Screening (2016) (4)
- Cellular Gene Modulation of HIV-Infected CD4 T Cells in Response to Serial Treatment with the Histone Deacetylase Inhibitor Vorinostat (2020) (4)
- Triple Hyp→Pro replacement in integramide A, a peptaib inhibitor of HIV‐1 integrase: Effect on conformation and bioactivity (2011) (3)
- The chemical biology of coronavirus host–cell interactions (2020) (3)
- Radiosynthesis of the HIV integrase inhibitor [18F]MK‐0518 (Isentress) (2010) (3)
- Safety, immune and anti-viral effects of pegylated interferon alpha 2b administration in ART-suppressed individuals: Results of pilot clinical trial. (2020) (3)
- Next generation therapeutics. (2013) (3)
- Immunomodulation by the Commensal Microbiome During Immune-Targeted Interventions: Focus on Cancer Immune Checkpoint Inhibitor Therapy and Vaccination (2021) (3)
- Evaluation of MK-7009, A Novel Macrocyclic Inhibitor of NS3/4A Protease, in the Chimpanzee Model of Chronic Hepatitis C Virus Infection (2008) (3)
- PD-1 blockade potentiates HIV latency reversal ex vivo in CD4+ T cells from ART-suppressed individuals (2019) (3)
- Microbiome and Metabolome driven differentiation of TGF-β producing Tregs leads to Senescence and HIV latency (2020) (3)
- 844 IN VITRO CHARACTERIZATION OF THE PAN-GENOTYPE ACTIVITY OF THE HCV NS3/4A PROTEASE INHIBITORS BOCEPREVIR AND TELAPREVIR (2012) (3)
- Microbiome And Metabolome Driven Differentiation Of TGF-β Producing Tregs Leads to Senescence and HIV Latency (2021) (3)
- Generation of a SARS-CoV-2 Replicon as a Model System to Dissect Virus Replication and Antiviral Inhibition (2020) (2)
- Supplementary material : Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial (2011) (2)
- Inhibitors of human immunodeficiency virus type I (2006) (2)
- Structure-Function Mapping of Interleukin 1 Precursors (2001) (2)
- A Deep Learning Genome-Mining Strategy Improves Biosynthetic Gene Cluster Prediction (2018) (2)
- Primary Human Dendritic Cells and Whole-Blood Based Assays to Evaluate Immuno-Modulatory Properties of Heat-Killed Commensal Bacteria (2021) (2)
- In a 5-Day Monotherapy Trial, MK-8408 Demonstrates Potent Antiviral Activity and Improved Resistance Profile in HCV Patients with Genotypes 1, 2, and 3 Infections (2016) (2)
- 1198 RESISTANCE ANALYSIS OF CIRRHOTIC TREATMENT-EXPERIENCED GENOTYPE 1 PATIENTS IN A STUDY OF MK-7009 IN COMBINATION WITH PEGYLATED INTERFERON/RIBAVIRIN (2013) (2)
- Integrastatins: Structure and HIV-1 Integrase Inhibitory Activities of Two Novel Racemic Tetracyclic Aromatic Heterocycles Produced by Two Fungal Species. (2002) (2)
- P4-418 Inhibition of APP processing by substrate-binding compounds: a novel approach to amyloid lowering (2004) (1)
- Isolation, Structure and HIV‐1 Integrase Inhibitory Activity of Exophillic Acid, a Novel Fungal Metabolite from Exophiala pisciphila. (2004) (1)
- 545. Rational Design of Doravirine (DOR): A Review of Development From Bench to Patients (2018) (1)
- Participant experiences using novel home-based blood collection device for viral load testing in the HIV cure trials with analytical treatment interruptions (2022) (1)
- Discovery and X-ray Crystallographic Analysis of a Iminohydantoin Inhibitor of beta-Secretase (2008) (1)
- Resistance to Inhibitors of Human Immunodeficiency Virus Type I Integration (2009) (1)
- MK-5172, a Novel Macrocyclic Inhibitor of NS3/4a Protease Demonstrates Efficacy Against Viral Resistance in the Chimpanzee Model of Chronic Hepatitis C Virus Infection (2010) (1)
- with oral administration of a BACE1 inhibitor in nonhuman primates (2008) (1)
- The role of zinc in transcriptional control of xenopus 5S RNA gene (1983) (1)
- Peptides : Breaking Away Proceedings of the Twenty-First American Peptide Symposium (2009) (1)
- Activity profile-based siRNA screen to explore the functional genomics of Alzheimer's disease (2007) (1)
- P2-066 A genetically engineered mouse model with an enhanced beta-secretase substrate exhibits increased amyloid generation (2004) (1)
- 1198 HCV NS3/4A PROTEASE RESISTANCE-ASSOCIATED VARIANTS (RAVS) IDENTIFIED IN GENOTYPE 1A PATIENTS EXHIBIT DIFFERENCES IN PHENOTYPIC RESISTANCE TO BOCEPREVIR AND TELAPREVIR IN GENOTYPE 1A REPLICON CELLS (2012) (1)
- Potent targeted activator of cell kill molecules eliminate cells expressing HIV-1 (2023) (1)
- Treatment of SHIV-infected, ART-suppressed rhesus macaques with bispecific HIVxCD3 DART® molecules (2019) (1)
- Total Synthesis , Characterization , and Conformational Analysis of the Naturally-Occurring Hexadecapeptide Integramide A and Its Diastereomer at Positions 14 and 15 (2009) (1)
- “We are looking at the future right now”: community acceptability of a home-based viral load test device in the context of HIV cure-related research with analytical treatment interruptions in the United States (2022) (1)
- Track A Basic Science (2012) (1)
- A-108 The Contribution of memory CD4+ T cell subset phenotype to latency reversal efficiency (2018) (0)
- 805 RIBAVIRIN NEITHER ENHANCES NOR ANTAGONIZES THE IN VIVO ACTIVITY OF VANIPREVIR IN THE CHIMPANZEE MODEL OF CHRONIC HCV INFECTION (2011) (0)
- Iconographies supplémentaires de l'article : Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial (2011) (0)
- Robust Antiviral Efficacy upon Administration of a Nucleoside Analog to Hepatitis C Virus-Infected Chimpanzees (cid:1) (2009) (0)
- P-A3 Identification of proximal biomarkers of PKC agonist activity in HIV-1 latently infected cells (2016) (0)
- Evaluation of IAP/SMAC mimetics as latency reversal agents in primary cells and cytokine induction in in vivo models predictive of cytokine release (2019) (0)
- First Demonstration of Cerebrospinal Fluid and Plasma A (cid:1) Lowering with Oral Administration of a (cid:1) -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates □ S (2008) (0)
- Analyzing the effects of sub‐optimal doses of raltegravir on HIV‐1 integration (2013) (0)
- CCDC 619397: Experimental Crystal Structure Determination (2007) (0)
- Doravirine and Islatravir Have Complementary Resistance Profiles and Create a Combination with a High Barrier to Resistance (2022) (0)
- 153. Molnupiravir Exhibits a High Barrier to the Development of SARS-CoV-2 Resistance in vitro (2022) (0)
- Structure-function relationships of a Xenopus transcription factor specific for 5S RNA genes (1985) (0)
- In Vitro Dose Ranging Studies for Serine Protease Inhibitor, MK-4519, Against a Hepatitis C Virus (HCV) Replicon using the Bellocell System (2010) (0)
- SIV INTEGRASE (CATALYTIC DOMAIN + DNA BIDING DOMAIN COMPRISING RESIDUES 50-293) MUTANT WITH PHE 185 REPLACED BY HIS (F185H) (2000) (0)
- In Vitro Pharmacokinetic/Pharmacodynamic Modeling of HIV Latency Reversal by Novel HDAC Inhibitors Using an Automated Platform (2021) (0)
- Integrase Inhibitors Postexposure Protection of Macaques from Vaginal SHIV Infection by (2014) (0)
- Call for Papers: Drug Resistance in Infectious Diseases and Beyond. (2022) (0)
- The Biology and Biochemistry of Integration as a Target for Chemotherapeuric Intervention (2021) (0)
- Vaccine Hyporesponse Induced by Individual Antibiotic Treatment in Mice and Non-Human Primates Is Diminished upon Recovery of the Gut Microbiome (2021) (0)
- P2-137 Secretase inhibitors reduce amyloid production in primary neurons from novel MWP HUAPP KI mice (2004) (0)
- Novel mutations introduced at the β-site of amyloid β protein precursor enhance the productio no famyloi d βpeptid eb yBACE 1in vitr oan di ncells (2005) (0)
- In vivo analysis of the effect of panobinostat on cell-associated HIV RNA and DNA levels and latent HIV infection (2016) (0)
- Role of triple Hyp ? Pro substitution on conformation and bioactivity of integramide A (2010) (0)
- Puri®cation, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain (1999) (0)
- Identification of a Novel HIV-1 Neutralizing Antibody Using Synthetic Peptides that Mimic a GP41 Fusion Intermediate (2006) (0)
- Xenopus Transcription RNA Gene* Factor A Requires Zinc for Binding to the 5 s (2001) (0)
- High resolution photocatalytic mapping of SARS-CoV-2 Spike protein-host cell membrane interactions (2022) (0)
- TGF-β associated senescence and impaired metabolism in central memory CD4 T cells promotes HIV persistence (2021) (0)
- Presence of Baseline Boceprevir (Boc) Resistance-Associated Variants (Ravs) Appears Not to Influence Treatment Outcomes in the Majority of Patients Following Boc/PR Treatment (2011) (0)
- Comparable HIV suppression by pegylated-IFN-α2a or pegylated-IFN-α2b during a 4-week analytical treatment interruption. (2021) (0)
- P1-359 Identification of genes that regulate the processing of the β-amyloid precursor protein and are candidates for association with late-onset Alzheimer’s disease by a genome-wide siRNA screen (2006) (0)
- Vaccine Hyporesponse Induced by Individual Antibiotic Treatment in Mice and Non-Human Primates Is Diminished upon Recovery of the Gut Microbiome (2021) (0)
- Single cell multi-omic reference atlases of non-human primate immune tissues reveals CD102 as a biomarker for long-lived plasma cells (2022) (0)
- Emerging Pharmacology: Inhibitors of Human (2009) (0)
- Recommendations for measuring HIV reservoir size in cure-directed clinical trials (2020) (0)
- Equisetin (I) and a Novel Opposite Stereochemical Homolog Phomasetin (II), Two Fungal Metabolites as Inhibitors of HIV-1 Integrase. (1998) (0)
- Inhibition ofCap(m7GpppXm)-Dependent Endonuclease ofInfluenza Virus by4-Substituted 2,4-Dioxobutanoic AcidCompounds (1994) (0)
- Vaccinationon Chronic Infection and Prophylactic PD-1 Blockade in Rhesus Macaques: Impact (2008) (0)
- Sequence within the HIV-1 LTR required for strand transfer by integrase in vitro (1995) (0)
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