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G Protein-Coupled Receptor Allosterism and Complexing
G protein-coupled receptors (GPCRs) represent the largest family of cell-surface receptors. These receptors are natural allosteric proteins because agonist-mediated signaling by GPCRs requires aExpand
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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules
1 Long chain fatty acids have recently been identified as agonists for the G protein‐coupled receptors GPR40 and GPR120. Here, we present the first description of GW9508, a small‐molecule agonist ofExpand
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Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric systems, affinityExpand
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Signalling bias in new drug discovery: detection, quantification and therapeutic impact
Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors (GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven-transmembrane receptorExpand
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International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology
The recommendations that follow have been updated from the proposals of a Technical Subcommittee set up by the International Union of Pharmacology Committee on Receptor Nomenclature and DrugExpand
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A simple method for quantifying functional selectivity and agonist bias.
Activation of seven-transmembrane (7TM) receptors by agonists does not always lead to uniform activation of all signaling pathways mediated by a given receptor. Relative to other ligands, manyExpand
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Agonist-receptor efficacy. II. Agonist trafficking of receptor signals.
  • T. Kenakin
  • Chemistry, Medicine
  • Trends in pharmacological sciences
  • 1 July 1995
There is evidence to suggest that receptors with seven transmembrane domains can exist in G protein-activating conformations. It is not known how many activated receptor forms exist for eachExpand
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The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitors⃞
4-{[4-({(3R)-1-Butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenyl]oxy}benzoic acid hydrochloride (873140) is a potent noncompetitive allosteric antagonistExpand
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Inverse, protean, and ligand‐selective agonism: matters of receptor conformation
  • T. Kenakin
  • Biology, Medicine
  • FASEB journal : official publication of the…
  • 1 March 2001
Concepts regarding the mechanisms by which drugs activate receptors to produce physiological response have progressed beyond considering the re¬ceptor as a simple on‐off switch. Current evidenceExpand
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Principles: receptor theory in pharmacology.
  • T. Kenakin
  • Biology, Medicine
  • Trends in pharmacological sciences
  • 1 April 2004
Pharmacological receptor theory is discussed with special reference to advances made during the past 25 years. Thus, the operational model has supplanted analysis of drug-receptor interaction inExpand
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