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Measurements of ligand bias and functional affinity.

作者信息

Kenakin Terry, Christopoulos Arthur

出版信息

Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c2. Epub 2013 May 17.

DOI:10.1038/nrd3954-c2
PMID:23681003
Abstract
摘要

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Measurements of ligand bias and functional affinity.配体偏向性和功能亲和力的测量。
Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c2. Epub 2013 May 17.
2
Dynamic bias and its implications for GPCR drug discovery.动态偏向及其对G蛋白偶联受体药物发现的影响。
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3
Signalling bias in new drug discovery: detection, quantification and therapeutic impact.新药发现中的信号偏倚：检测、定量和治疗影响。
Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15.
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Quantifying biased agonism: understanding the links between affinity and efficacy.量化偏向性激动作用：理解亲和力与效能之间的联系。
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Is the Quest for Signaling Bias Worth the Effort?是否值得追求信号偏倚？
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The Effective Application of Biased Signaling to New Drug Discovery.偏向性信号传导在新药研发中的有效应用
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7
Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy.定量分析临床相关β2-肾上腺素能受体配体的配体偏向：对药物分类学的影响。
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Practical guide for calculating and representing biased signaling by GPCR ligands: A stepwise approach.GPCR配体计算和表示偏向性信号传导的实用指南：逐步方法
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Unravelling intrinsic efficacy and ligand bias at G protein coupled receptors: A practical guide to assessing functional data.解析G蛋白偶联受体的内在活性和配体偏向性：评估功能数据实用指南
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Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity.利用酿酒酵母测定腺苷A1受体激动剂和拮抗剂药理学：对配体筛选和功能选择性的影响。
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Ligand bias underlies differential signaling of multiple FGFs via FGFR1.配体偏向是多种 FGF 通过 FGFR1 进行差异化信号传递的基础。

本文引用的文献

1
Quantifying biased agonism: understanding the links between affinity and efficacy.量化偏向性激动作用：理解亲和力与效能之间的联系。
Nat Rev Drug Discov. 2013 Jun;12(6):483. doi: 10.1038/nrd3954-c1. Epub 2013 May 17.
2
Signalling bias in new drug discovery: detection, quantification and therapeutic impact.新药发现中的信号偏倚：检测、定量和治疗影响。
Nat Rev Drug Discov. 2013 Mar;12(3):205-16. doi: 10.1038/nrd3954. Epub 2012 Feb 15.
3
Crystal structure of the β2 adrenergic receptor-Gs protein complex.β2 肾上腺素能受体-Gs 蛋白复合物的晶体结构。
Elife. 2024 Apr 3;12:RP88144. doi: 10.7554/eLife.88144.
4
Quantitative assessment of ligand bias from bias plots: The bias coefficient "kappa".从偏倚图定量评估配体偏倚：偏倚系数“kappa”。
Biochim Biophys Acta Gen Subj. 2023 Oct;1867(10):130428. doi: 10.1016/j.bbagen.2023.130428. Epub 2023 Jul 23.
5
Agonist efficiency links binding and gating in a nicotinic receptor.激动剂效率将烟碱型乙酰胆碱受体的结合和门控联系起来。
Elife. 2023 Jul 3;12:e86496. doi: 10.7554/eLife.86496.
6
Tyrosine 7.43 is important for mu-opioid receptor downstream signaling pathways activated by fentanyl.酪氨酸7.43对于芬太尼激活的μ-阿片受体下游信号通路很重要。
Front Pharmacol. 2022 Sep 2;13:919325. doi: 10.3389/fphar.2022.919325. eCollection 2022.
7
Functional Characterization of Sodium Channel Inhibitors at the Delta-Opioid Receptor.δ-阿片受体上钠通道抑制剂的功能特性
ACS Omega. 2022 May 12;7(20):16939-16951. doi: 10.1021/acsomega.1c07226. eCollection 2022 May 24.
8
Place of the partial dopamine receptor agonist aripiprazole in the management of schizophrenia in adults: a Delphi consensus study.部分多巴胺受体激动剂阿立哌唑在成人精神分裂症治疗中的地位：德尔菲共识研究。
BMC Psychiatry. 2022 May 28;22(1):364. doi: 10.1186/s12888-022-04008-9.
9
From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.从结构到临床：设计一种具有治疗阿尔茨海默病潜力的毒蕈碱 M1 受体激动剂。
Cell. 2021 Nov 24;184(24):5886-5901.e22. doi: 10.1016/j.cell.2021.11.001.
10
The Guts of the Opioid Crisis.阿片类药物危机的核心问题
Physiology (Bethesda). 2021 Sep 1;36(5):315-323. doi: 10.1152/physiol.00014.2021.
Nature. 2011 Jul 19;477(7366):549-55. doi: 10.1038/nature10361.
4
Divergent agonist selectivity in activating β1- and β2-adrenoceptors for G-protein and arrestin coupling.激动剂在激活β1-和β2-肾上腺素能受体与 G 蛋白和阻滞蛋白偶联的偏性。
Biochem J. 2011 Aug 15;438(1):191-202. doi: 10.1042/BJ20110374.
5
Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.β2 肾上腺素能受体的纳米体稳定的活性状态结构。
Nature. 2011 Jan 13;469(7329):175-80. doi: 10.1038/nature09648.
6
Galpha-subunits differentially alter the conformation and agonist affinity of kappa-opioid receptors.Gα亚基以不同方式改变κ-阿片受体的构象和激动剂亲和力。
Biochemistry. 2008 Feb 12;47(6):1567-78. doi: 10.1021/bi701476b. Epub 2008 Jan 19.
7
Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.G蛋白偶联受体激动剂活性的评估：通过Gi/o、Gs和G15对M2毒蕈碱受体信号传导的分析
J Pharmacol Exp Ther. 2007 Jun;321(3):1193-207. doi: 10.1124/jpet.107.120857. Epub 2007 Mar 28.
8
Operational models of pharmacological agonism.药理学激动作用的操作模型。
Proc R Soc Lond B Biol Sci. 1983 Dec 22;220(1219):141-62. doi: 10.1098/rspb.1983.0093.
9
An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation.一种药理学激动作用的操作模型：E/[A]曲线形状对激动剂解离常数估计的影响。
Br J Pharmacol. 1985 Feb;84(2):561-71. doi: 10.1111/j.1476-5381.1985.tb12941.x.