Allostery in Drug Development

doi:10.1007/978-981-13-8719-7_1

	Allostery in Drug Development
	Cheng, Xi; Jiang, Hualiang
刊名	PROTEIN ALLOSTERY IN DRUG DISCOVERY
	2019
卷号	1163 页码:1-23
关键词	Allosteric perturbation Biased agonists Conformational changes Protein dynamics Rational drug design
ISSN号	0065-2598
DOI	10.1007/978-981-13-8719-7_1
通讯作者	Jiang, Hualiang(hljiang@simm.ac.cn)
英文摘要	Allosteric regulation is a ubiquitous strategy employed in nature to control cellular processes by regulating the affinities of biomolecules. Allosteric modulators are able to tune the protein/substrate affinity in a highly predictable way, suggesting that such modulators may represent safe drugs. Tremendous advances have been made in the development of allosteric modulators and the characterization of their therapeutic targets. Here, we briefly introduce several representative allosteric modulators of important drug targets, such as the G protein-coupled receptor family. We also review the state-of-the-art experimental and computational approaches used in allosteric drug development. The accumulated knowledge of allosteric regulation and the technical progress made in drug development will lead to an explosion of promising allosteric drugs in the near future.
WOS关键词	MARKOV STATE MODELS ; MU-OPIOID RECEPTOR ; LIGAND-BINDING SITES ; DRUGGABLE HOT-SPOTS ; BETA-ARRESTIN ; SMALL-MOLECULE ; DISORDERED PROTEIN ; BIASED AGONISM ; DOUBLE-BLIND ; GPCR
WOS研究方向	Research & Experimental Medicine ; Pharmacology & Pharmacy
语种	英语
出版者	SPRINGER INTERNATIONAL PUBLISHING AG
WOS记录号	WOS:000514080400002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/281419]
专题	中国科学院上海药物研究所
通讯作者	Jiang, Hualiang
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Cheng, Xi,Jiang, Hualiang. Allostery in Drug Development[J]. PROTEIN ALLOSTERY IN DRUG DISCOVERY,2019,1163:1-23.
APA	Cheng, Xi,&Jiang, Hualiang.(2019).Allostery in Drug Development.PROTEIN ALLOSTERY IN DRUG DISCOVERY,1163,1-23.
MLA	Cheng, Xi,et al."Allostery in Drug Development".PROTEIN ALLOSTERY IN DRUG DISCOVERY 1163(2019):1-23.