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Quantifying biased agonism: understanding the links between affinity and efficacy.

作者信息

Rajagopal Sudarshan

出版信息

Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c1. Epub 2013 May 17.

DOI:10.1038/nrd3954-c1

PMID:23681006

Abstract

摘要

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本文引用的文献

Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15.

A simple method for quantifying functional selectivity and agonist bias.

ACS Chem Neurosci. 2012 Mar 21;3(3):193-203. doi: 10.1021/cn200111m. Epub 2011 Dec 20.

Quantifying ligand bias at seven-transmembrane receptors.

Mol Pharmacol. 2011 Sep;80(3):367-77. doi: 10.1124/mol.111.072801. Epub 2011 May 24.

A modification of receptor theory.

Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.

Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory.

Arch Int Pharmacodyn Ther. 1954 Sep 1;99(1):32-49.

The cubic ternary complex receptor-occupancy model. III. resurrecting efficacy.

J Theor Biol. 1996 Aug 21;181(4):381-97. doi: 10.1006/jtbi.1996.0139.

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

J Biol Chem. 1993 Mar 5;268(7):4625-36.

A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

J Biol Chem. 1980 Aug 10;255(15):7108-17.

Operational models of pharmacological agonism.

Proc R Soc Lond B Biol Sci. 1983 Dec 22;220(1219):141-62. doi: 10.1098/rspb.1983.0093.

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相似文献

Quantifying biased agonism: understanding the links between affinity and efficacy.

Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c1. Epub 2013 May 17.

G Protein-coupled Receptor Biased Agonism.

J Cardiovasc Pharmacol. 2016 Mar;67(3):193-202. doi: 10.1097/FJC.0000000000000356.

Recent updates on GPCR biased agonism.

Pharmacol Res. 2016 Oct;112:49-57. doi: 10.1016/j.phrs.2016.01.031. Epub 2016 Feb 2.

Unravelling intrinsic efficacy and ligand bias at G protein coupled receptors: A practical guide to assessing functional data.

Biochem Pharmacol. 2016 Feb 1;101:1-12. doi: 10.1016/j.bcp.2015.10.011. Epub 2015 Oct 23.

Functional selectivity and biased receptor signaling.

J Pharmacol Exp Ther. 2011 Feb;336(2):296-302. doi: 10.1124/jpet.110.173948. Epub 2010 Oct 28.

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor.

Biochem Pharmacol. 2016 Aug 1;113:70-87. doi: 10.1016/j.bcp.2016.05.014. Epub 2016 Jun 7.

The Effective Application of Biased Signaling to New Drug Discovery.

Mol Pharmacol. 2015 Dec;88(6):1055-61. doi: 10.1124/mol.115.099770. Epub 2015 Jul 2.

What is pharmacological 'affinity'? Relevance to biased agonism and antagonism.

Trends Pharmacol Sci. 2014 Sep;35(9):434-41. doi: 10.1016/j.tips.2014.06.003. Epub 2014 Jul 17.

Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.

Neuropharmacology. 2017 Mar 15;115:60-72. doi: 10.1016/j.neuropharm.2016.07.001. Epub 2016 Jul 5.

Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15.

引用本文的文献

Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response.

Nat Commun. 2019 Sep 9;10(1):4075. doi: 10.1038/s41467-019-11875-6.

An intact model for quantifying functional selectivity.

Sci Rep. 2019 Feb 22;9(1):2557. doi: 10.1038/s41598-019-39000-z.

An evaluation of the operational model when applied to quantify functional selectivity.

Br J Pharmacol. 2018 May;175(10):1654-1668. doi: 10.1111/bph.14171. Epub 2018 Mar 30.

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Nat Rev Drug Discov. 2018 Apr;17(4):243-260. doi: 10.1038/nrd.2017.229. Epub 2018 Jan 5.

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J Mol Endocrinol. 2017 Jul;59(1):R33-R46. doi: 10.1530/JME-17-0042. Epub 2017 Apr 18.

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Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. Epub 2016 Aug 17.

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Sci Rep. 2016 Apr 27;6:25158. doi: 10.1038/srep25158.

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Bioorg Med Chem Lett. 2016 Jan 15;26(2):241-250. doi: 10.1016/j.bmcl.2015.12.024. Epub 2015 Dec 9.

Superagonism at G protein-coupled receptors and beyond.

Br J Pharmacol. 2016 Oct;173(20):3018-27. doi: 10.1111/bph.13278. Epub 2015 Oct 24.

本文引用的文献

Signalling bias in new drug discovery: detection, quantification and therapeutic impact.

Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15.

A simple method for quantifying functional selectivity and agonist bias.

ACS Chem Neurosci. 2012 Mar 21;3(3):193-203. doi: 10.1021/cn200111m. Epub 2011 Dec 20.

Quantifying ligand bias at seven-transmembrane receptors.

Mol Pharmacol. 2011 Sep;80(3):367-77. doi: 10.1124/mol.111.072801. Epub 2011 May 24.

A modification of receptor theory.

Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.

Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory.

Arch Int Pharmacodyn Ther. 1954 Sep 1;99(1):32-49.

The cubic ternary complex receptor-occupancy model. III. resurrecting efficacy.

J Theor Biol. 1996 Aug 21;181(4):381-97. doi: 10.1006/jtbi.1996.0139.

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

J Biol Chem. 1993 Mar 5;268(7):4625-36.

A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.

J Biol Chem. 1980 Aug 10;255(15):7108-17.

Operational models of pharmacological agonism.

Proc R Soc Lond B Biol Sci. 1983 Dec 22;220(1219):141-62. doi: 10.1098/rspb.1983.0093.