Arthur Christopoulos
#81,868
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Australian pharmacologist and toxicologist
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#1536
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#12
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Pharmacology
#92
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#119
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Arthur Christopoulos's Degrees
- Masters Toxicology University of Melbourne
- PhD Pharmacology Monash University
Why Is Arthur Christopoulos Influential?
(Suggest an Edit or Addition)According to Wikipedia, Arthur Christopoulos is an Australian Professor of Analytical Pharmacology at Monash University. He is the recipient of numerous national and international awards, including the 2013 John J. Abel Award from the American Society for Pharmacology and Experimental Therapeutics and the Rand Medal from the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists, the 2014 IUPHAR Analytical Pharmacology Lecturer, a 2015 Doctor of Laws from the National and Kapodistrian University of Athens, Greece, the 2016 recipient of the Gaddum Memorial Award from the British Pharmacological Society and the 2016 GSK Award for Research Excellence. Since 2014, Clarivate Analytics has regularly named him a Highly Cited Researcher in Pharmacology and Toxicology. In 2021, Arthur was named a Highly Cited Researcher in both Pharmacology and Toxicology and Biology and Biochemistry categories. In 2017 he was elected a Fellow of the Australian Academy of Health and Medical Sciences and in 2018 he was elected as a Fellow of the British Pharmacological Society. He was a Councillor of the International Union of Basic and Clinical Pharmacology from 2018 to 2022. In 2019 he was appointed Dean of Monash University's Faculty of Pharmacy and Pharmaceutical Sciences and from 2021 to 2023 he served as the inaugural Director of Monash University's Neuromedicines Discovery Centre. He was elected a Fellow of the Australian Academy of Science in 2021.
Arthur Christopoulos'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
- Fitting Models to Biological Data Using Linear and Nonlinear Regression: A Practical Guide to Curve Fitting (2004) (2359)
- Functional Selectivity and Classical Concepts of Quantitative Pharmacology (2007) (1078)
- Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders (2009) (957)
- G Protein-Coupled Receptor Allosterism and Complexing (2002) (892)
- Activation and allosteric modulation of a muscarinic acetylcholine receptor (2013) (773)
- Signalling bias in new drug discovery: detection, quantification and therapeutic impact (2012) (636)
- Allosteric binding sites on cell-surface receptors: novel targets for drug discovery (2002) (617)
- THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein‐coupled receptors (2017) (560)
- THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors (2019) (558)
- International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology (2003) (546)
- Phase-plate cryo-EM structure of a class B GPCR-G protein complex (2017) (400)
- A simple method for quantifying functional selectivity and agonist bias. (2012) (398)
- Emerging paradigms in GPCR allostery: implications for drug discovery (2013) (388)
- Allosteric Modulation of the Cannabinoid CB1 Receptor (2005) (371)
- G-Protein–Coupled Receptor Mas Is a Physiological Antagonist of the Angiotensin II Type 1 Receptor (2005) (362)
- Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs (2013) (350)
- Mechanisms of signalling and biased agonism in G protein-coupled receptors (2018) (343)
- Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. (2007) (327)
- Muscarinic acetylcholine receptors: novel opportunities for drug development (2014) (298)
- THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets (2019) (295)
- Novel Receptor Partners and Function of Receptor Activity-modifying Proteins* (2003) (288)
- Allosteric modulation of G protein-coupled receptors. (2007) (277)
- THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview (2017) (266)
- Allosteric modulation of G protein-coupled receptors: A pharmacological perspective (2011) (257)
- Crystal structures of the M1 and M4 muscarinic acetylcholine receptors (2016) (253)
- Structure of the adenosine-bound human adenosine A1 receptor–Gi complex (2018) (252)
- Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. (2011) (250)
- The role of kinetic context in apparent biased agonism at GPCRs (2016) (245)
- Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex (2018) (232)
- THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors (2021) (212)
- Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia (2008) (208)
- Structural insights into G-protein-coupled receptor allostery (2018) (203)
- Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity (2017) (203)
- Quantification of Ligand Bias for Clinically Relevant β2-Adrenergic Receptor Ligands: Implications for Drug Taxonomy (2014) (200)
- Allosteric Ligands of the Glucagon-Like Peptide 1 Receptor (GLP-1R) Differentially Modulate Endogenous and Exogenous Peptide Responses in a Pathway-Selective Manner: Implications for Drug Screening (2010) (197)
- Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. (2012) (196)
- Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations (2013) (186)
- Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes (2005) (185)
- International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands (2014) (183)
- Advances in G Protein-Coupled Receptor Allostery: From Function to Structure (2014) (179)
- Assessing the distribution of parameters in models of ligand-receptor interaction: to log or not to log. (1998) (172)
- Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor (2018) (169)
- A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity (2008) (167)
- Novel Allosteric Modulators of G Protein-coupled Receptors* (2015) (165)
- Microglial activation and progressive brain changes in schizophrenia (2016) (158)
- The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors. (2012) (155)
- Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties (2010) (153)
- Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation (2016) (150)
- RNA editing of the serotonin 5HT2C receptor and its effects on cell signalling, pharmacology and brain function. (2008) (149)
- Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor. (2012) (147)
- Identification of Orthosteric and Allosteric Site Mutations in M2 Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias* (2010) (143)
- Bridging the gap: bitopic ligands of G-protein-coupled receptors. (2013) (142)
- Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor Ligands* (2007) (141)
- Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity (2009) (141)
- Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. (2013) (130)
- The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism (2016) (122)
- Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors. (2008) (117)
- Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. (2006) (115)
- Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects (2012) (114)
- Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor (2015) (112)
- Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes. (2009) (111)
- New Insights into the Function of M4 Muscarinic Acetylcholine Receptors Gained Using a Novel Allosteric Modulator and a DREADD (Designer Receptor Exclusively Activated by a Designer Drug) (2008) (110)
- A kinetic view of GPCR allostery and biased agonism. (2017) (110)
- Allosteric modulation as a unifying mechanism for receptor function and regulation (2017) (110)
- A Monod-Wyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) Allosteric Modulation* (2011) (110)
- A new mechanism of allostery in a G protein-coupled receptor dimer (2014) (109)
- Endogenous Allosteric Modulators of G Protein–Coupled Receptors (2015) (109)
- Structure-Function Studies of Allosteric Agonism at M2 Muscarinic Acetylcholine Receptors (2007) (107)
- Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy (2016) (105)
- Probing the Molecular Mechanism of Interaction between 4-n-Butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the Muscarinic M1 Receptor: Direct Pharmacological Evidence That AC-42 Is an Allosteric Agonist (2006) (102)
- DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo (2018) (102)
- ALLOSTERIC INTERACTIONS AT MUSCARINIC CHOLINOCEPTORS (1998) (102)
- ‘Ins and outs’ of seven-transmembrane receptor signalling to ERK (2005) (97)
- Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs (2007) (97)
- Characterization of serotonin 5‐HT2C receptor signaling to extracellular signal‐regulated kinases 1 and 2 (2005) (95)
- Cellular Signaling Mechanisms for Muscarinic Acetylcholine Receptors (2003) (93)
- Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice (2017) (93)
- Activation of the GLP-1 receptor by a non-peptidic agonist (2020) (93)
- Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective (2014) (93)
- Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist (2014) (87)
- Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor (2015) (87)
- Polymorphism and Ligand Dependent Changes in Human Glucagon-Like Peptide-1 Receptor (GLP-1R) Function: Allosteric Rescue of Loss of Function Mutation (2011) (87)
- Reversible and Specific Extracellular Antagonism of Receptor-Histidine Kinase Signaling* (2002) (85)
- Second Extracellular Loop of Human Glucagon-like Peptide-1 Receptor (GLP-1R) Has a Critical Role in GLP-1 Peptide Binding and Receptor Activation* (2011) (84)
- RAMPs: 5 years on, where to now? (2003) (83)
- A structure-activity analysis of biased agonism at the dopamine D2 receptor. (2013) (82)
- Sustainable Pharmacy Education in the Time of COVID-19 (2020) (82)
- Allosteric Modulation of Muscarinic Acetylcholine Receptors (2007) (82)
- Allosteric modulators of G-protein-coupled receptors. (2003) (81)
- Allostery and Biased Agonism at Class B G Protein-Coupled Receptors. (2017) (81)
- Determinants of 1-Piperidinecarboxamide, N-[2-[[5-Amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) Affinity for Calcitonin Gene-Related Peptide and Amylin Receptors—The Role of Rec (2006) (81)
- Amylin receptors: molecular composition and pharmacology. (2004) (79)
- Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators. (2013) (79)
- Allosteric targeting of receptor tyrosine kinases (2014) (78)
- Interaction of ebeinone, an alkaloid from Fritillaria imperialis, at two muscarinic acetylcholine receptor subtypes. (1997) (78)
- Quantification of Functional Selectivity at the Human α1A-Adrenoceptor (2011) (78)
- Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor. (2012) (77)
- Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor (2016) (75)
- THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets (2021) (75)
- Differential Activation and Modulation of the Glucagon-Like Peptide-1 Receptor by Small Molecule Ligands (2013) (75)
- Rules of Engagement: GPCRs and G Proteins. (2018) (75)
- Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs. (2009) (75)
- Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor (2016) (74)
- Allosteric modulation of the calcium-sensing receptor by gamma-glutamyl peptides: inhibition of PTH secretion, suppression of intracellular cAMP levels, and a common mechanism of action with L-amino acids. (2011) (72)
- Allosteric Modulation of Endogenous Metabolites as an Avenue for Drug Discovery (2012) (71)
- Prolonged Calcitonin Receptor Signaling by Salmon, but Not Human Calcitonin, Reveals Ligand Bias (2014) (71)
- Modulation of the Glucagon-Like Peptide-1 Receptor Signaling by Naturally Occurring and Synthetic Flavonoids (2011) (71)
- Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery (2012) (69)
- Dominant Negative G Proteins Enhance Formation and Purification of Agonist-GPCR-G Protein Complexes for Structure Determination. (2018) (69)
- Structural Determinants of Allosteric Agonism and Modulation at the M4 Muscarinic Acetylcholine Receptor (2010) (68)
- Identification of N-Terminal Receptor Activity-Modifying Protein Residues Important for Calcitonin Gene-Related Peptide, Adrenomedullin, and Amylin Receptor Function (2008) (68)
- Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors (2011) (68)
- Allosteric modulation of G protein-coupled receptors. (2004) (68)
- Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation. (2020) (67)
- Orthosteric and Allosteric Modes of Interaction of Novel Selective Agonists of the M1 Muscarinic Acetylcholine Receptor (2010) (66)
- Cellular signaling mechanisms for muscarinic acetylcholine receptors. (2003) (65)
- Allostery in GPCRs: 'MWC' revisited. (2011) (65)
- The assessment of antagonist potency under conditions of transient response kinetics. (1999) (65)
- Structural basis of receptor sulfotyrosine recognition by a CC chemokine: the N-terminal region of CCR3 bound to CCL11/eotaxin-1. (2014) (65)
- Tyrosine Sulfation of Chemokine Receptor CCR2 Enhances Interactions with Both Monomeric and Dimeric Forms of the Chemokine Monocyte Chemoattractant Protein-1 (MCP-1)* (2013) (65)
- Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics (2015) (63)
- Measurements of ligand bias and functional affinity (2013) (62)
- Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits. (2013) (61)
- On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor. (1998) (60)
- Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs. (2006) (60)
- Procalcitonin has bioactivity at calcitonin receptor family complexes: Potential mediator implications in sepsis* (2008) (59)
- Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function. (2013) (59)
- Structure and Dynamics of Adrenomedullin Receptors AM1 and AM2 Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins. (2020) (59)
- Impact of species variability and ‘probe‐dependence’ on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor (2011) (58)
- Distinct Receptor Activity-Modifying Protein Domains Differentially Modulate Interaction with Calcitonin Receptors (2006) (58)
- Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. (2013) (57)
- Novel GPCR paradigms at the μ‐opioid receptor (2015) (56)
- G-protein-coupled receptor allosterism: the promise and the problem(s). (2004) (56)
- Modulating receptor function through RAMPs: can they represent drug targets in themselves? (2009) (56)
- Modulation of cannabinoid agonist binding by 5‐HT in the rat cerebellum (2002) (55)
- Qualitative and quantitative assessment of relative agonist efficacy. (1999) (54)
- Comparison of Receptor Binding Characteristics of Commonly Used Muscarinic Antagonists in Human Bladder Detrusor and Mucosa (2009) (53)
- Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D₂ receptor. (2014) (53)
- A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal Structures (2016) (52)
- Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors (2016) (52)
- Determination of Adenosine A1 Receptor Agonist and Antagonist Pharmacology Using Saccharomyces cerevisiae: Implications for Ligand Screening and Functional Selectivity (2009) (51)
- The generation of nitric oxide by G protein-coupled receptors. (1998) (51)
- Molecular Determinants of Allosteric Modulation at the M1 Muscarinic Acetylcholine Receptor* (2014) (51)
- Application of a Kinetic Model to the Apparently Complex Behavior of Negative and Positive Allosteric Modulators of Muscarinic Acetylcholine Receptors (2004) (50)
- The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling (2010) (50)
- Functional Importance of a Structurally Distinct Homodimeric Complex of the Family B G Protein-Coupled Secretin Receptor (2009) (50)
- On the Mechanism of Interaction of Potent Surmountable and Insurmountable Antagonists with the Prostaglandin D2 Receptor CRTH2 (2006) (50)
- M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss (2016) (50)
- Small Molecule Allosteric Modulation of the Glucagon-Like Peptide-1 Receptor Enhances the Insulinotropic Effect of Oxyntomodulin (2012) (49)
- 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. (2008) (49)
- Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants (2016) (49)
- Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. (2015) (49)
- Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation (2016) (48)
- A Critical Role for the Short Intracellular C Terminus in Receptor Activity-Modifying Protein Function (2006) (48)
- Recent advances in the determination of G protein-coupled receptor structures. (2018) (47)
- Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery. (2016) (47)
- Molecular Mechanisms of Bitopic Ligand Engagement with the M1 Muscarinic Acetylcholine Receptor* (2014) (47)
- Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A1 Receptor (2018) (46)
- Design and Receptor Interactions of Obligate Dimeric Mutant of Chemokine Monocyte Chemoattractant Protein-1 (MCP-1)* (2012) (46)
- Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor (2018) (46)
- Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy (2016) (46)
- Engendering biased signalling from the calcium‐sensing receptor for the pharmacotherapy of diverse disorders (2014) (46)
- Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia (2021) (46)
- Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor. (2016) (45)
- Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists. (2001) (45)
- Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists. (2020) (45)
- Consequences of splice variation on Secretin family G protein‐coupled receptor function (2012) (45)
- Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor* (2014) (44)
- Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand. (2015) (44)
- Investigation of the Interaction of a Putative Allosteric Modulator, N-(2,3-Diphenyl-1,2,4-thiadiazole-5-(2H)-ylidene) Methanamine Hydrobromide (SCH-202676), with M1 Muscarinic Acetylcholine Receptors (2004) (43)
- Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias. (2015) (42)
- Overview of receptor allosterism. (2000) (42)
- Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors. (1999) (42)
- Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery (2017) (42)
- Characterization of the Novel Positive Allosteric Modulator, LY2119620, at the Muscarinic M2 and M4 Receptors (2014) (42)
- Dynamic mechanisms of non-classical antagonism by competitive AT(1) receptor antagonists. (2000) (41)
- Evidence for Pleiotropic Signaling at the Mouse β3-Adrenoceptor Revealed by SR59230A [3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol Oxalate] (2005) (41)
- Effect of the Calcimimetic R-568 [3-(2-Chlorophenyl)-N-((1R)-1-(3-methoxyphenyl)ethyl)-1-propanamine] on Correcting Inactivating Mutations in the Human Calcium-Sensing Receptor (2009) (41)
- Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity (2016) (41)
- Interaction of anandamide with the M1 and M4 muscarinic acetylcholine receptors (2001) (40)
- Pharmacological analysis of cannabinoid receptor activity in the rat vas deferens (2001) (40)
- Crystal structure of the M5 muscarinic acetylcholine receptor (2019) (39)
- Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor (2016) (39)
- Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor. (2012) (38)
- Functional and structural perspectives on allosteric modulation of GPCRs. (2014) (38)
- Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs (2019) (38)
- Delineating the Mode of Action of Adenosine A1 Receptor Allosteric Modulators (2010) (38)
- Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism (2018) (37)
- New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism (2018) (37)
- Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors. (2006) (36)
- Structure and dynamics of the CGRP receptor in apo and peptide-bound forms (2021) (35)
- Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor (2016) (35)
- Regulation of M2 Muscarinic Acetylcholine Receptor Expression and Signaling by Prolonged Exposure to Allosteric Modulators (2005) (35)
- Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism (2017) (35)
- Glucagon‐like peptide‐1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists (2018) (35)
- Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor. (2015) (35)
- H2 Relaxin Is a Biased Ligand Relative to H3 Relaxin at the Relaxin Family Peptide Receptor 3 (RXFP3) (2010) (34)
- Complexing Receptor Pharmacology (2006) (34)
- Three allosteric modulators act at a common site, distinct from that of competitive antagonists, at muscarinic acetylcholine M2 receptors. (1997) (33)
- Attention-Deficit and Disruptive Behavior Disorders (2014) (33)
- Reverse Engineering of the Selective Agonist TBPB Unveils Both Orthosteric and Allosteric Modes of Action at the M1 Muscarinic Acetylcholine Receptor (2013) (33)
- Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery. (2013) (33)
- The Role of Transmembrane Domain 3 in the Actions of Orthosteric, Allosteric, and Atypical Agonists of the M4 Muscarinic Acetylcholine Receptor (2011) (33)
- Differential GLP-1R binding and activation by peptide and non-peptide agonists (2020) (32)
- Subtype (2020) (32)
- Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells. (2013) (31)
- Assessment of the allosteric interactions of the bisquaternary heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at M1 and M2 muscarine receptors. (1994) (31)
- The Molecular Control of Calcitonin Receptor Signaling. (2019) (31)
- Structure and dynamics of the active Gs-coupled human secretin receptor (2020) (31)
- Interaction Studies of Multiple Binding Sites on M4 Muscarinic Acetylcholine Receptors (2006) (31)
- Analytical pharmacology: the impact of numbers on pharmacology. (2011) (30)
- A Positive Allosteric Modulator of the Adenosine A1 Receptor Selectively Inhibits Primary Afferent Synaptic Transmission in a Neuropathic Pain Model (2015) (30)
- 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. (2009) (30)
- 4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor. (2016) (29)
- Structure-Function Studies of Allosteric Agonism at M 2 Muscarinic Acetylcholine Receptors (2007) (29)
- Second Extracellular Loop of Human Glucagon-like Peptide-1 Receptor (GLP-1R) Differentially Regulates Orthosteric but Not Allosteric Agonist Binding and Function* (2011) (29)
- Stimulus Bias Provides Evidence for Conformational Constraints in the Structure of a G Protein-coupled Receptor* (2012) (29)
- Involvement of the sigma1 (σ1) receptor in the anti‐amnesic, but not antidepressant‐like, effects of the aminotetrahydrofuran derivative ANAVEX1‐41 (2007) (29)
- Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform. (2010) (29)
- Quantification of Allosteric Interactions at G Protein–Coupled Receptors Using Radioligand Binding Assays (2000) (28)
- Neurological, neuropsychiatric and neurodevelopmental complications of COVID-19 (2020) (28)
- Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs (2020) (28)
- Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite (2013) (28)
- Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators (2016) (27)
- The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. (2016) (27)
- Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity (2021) (27)
- Pharmacological analysis of the novel mode of interaction between xanomeline and the M1 muscarinic acetylcholine receptor. (1999) (27)
- Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an "infinite dilution" procedure. (1997) (27)
- Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors. (1996) (27)
- Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking* (2014) (26)
- Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors (2018) (25)
- Muscarinic M5 receptors modulate ethanol seeking in rats (2018) (25)
- Allosteric Modulation of a Chemogenetically Modified G Protein-Coupled Receptor (2013) (25)
- Receptor expression modulates calcium-sensing receptor mediated intracellular Ca2+ mobilization. (2015) (25)
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- Acetylcholine receptors (muscarinic) in GtoPdb v.2021.3 (2021) (0)
- Activities of Daily Living (2021) (0)
- Muscarinic Acetylcholine Receptor 1 Structure-Function Relationships at the M Mechanistic Insights into Allosteric (2014) (0)
- Predictive Validity (2022) (0)
- ALDH (2020) (0)
- The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ-Opioid Receptor. (2022) (0)
- Subcellular Trafficking Acetylcholine Receptor Internalization and Muscarinic 1 Allosteric Modulation of M Signal Transduction : (2014) (0)
- SNP (2020) (0)
- Erratum: Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecular ligands (Molecular Pharmacology (2013) 83 (822-834)) (2013) (0)
- Non-classical modes of signaling by 5HT(2C) receptors (2006) (0)
- Erratum: Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an 'infinite dilution' procedure (Biochemical Pharmacology (1997) 53 (795-800)) (1997) (0)
- Binding and functional characterisation of allosteric agonists at M2 muscarinic acetylcholine receptors (2008) (0)
- Novel Adenosine A2B Receptor Signalling in Cardiac Fibroblasts: Uncovering Context-Specific Biased Agonism (2018) (0)
- Concordance between two methods for estimating heterotropic cooperativity at muscarine receptors (1995) (0)
- Allosteric Ligands of Metabotropic Glutamate Receptor 5 Have Biased Agonism and Cooperativity (2015) (0)
- Response from Non-sumountable antagonism: transcending steady steady state (2001) (0)
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