Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors

doi:10.1038/aps.2011.170

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物靶标结构与功能中心

	Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors
	Pal, Kuntal 1; Melcher, Karsten 1; Xu, H. Eric1,2
刊名	ACTA PHARMACOLOGICA SINICA
	2012-03
卷号	33 期号:3 页码:300-311
关键词	G-protein-coupled receptor (GPCR) parathyroid hormone glucagon calcitonin crystal structure
ISSN号	1671-4083
DOI	10.1038/aps.2011.170
文献子类	Review
英文摘要	Class B G-protein-coupled receptors (GPCRs) are receptors for peptide hormones that include glucagon, parathyroid hormone, and calcitonin. These receptors are involved in a wide spectrum of physiological activities, from metabolic regulation and stress control to development and maintenance of the skeletal system. As such, they are important drug targets for the treatment of diabetes, osteoporosis, and stress related disorders. Class B GPCRs are organized into two modular domains: an extracellular domain (ECD) and a helical bundle that contains seven transmembrane helices (TM domain). The ECD is responsible for the high affinity and specificity of hormone binding, and the TM domain is required for receptor activation and signal coupling to downstream G-proteins. Although the structure of the full-length receptor remains unknown, the ECD structures have been well characterized for a number of Class B GPCRs, revealing a common fold for ligand recognition. This review summarizes the general structural principles that guide hormone binding by Class B ECDs and their implications in the design of peptide hormone analogs for therapeutic purposes.
资助项目	Jay and Betty Van Andel Foundation[00000000] ; National Institute of Health[GM087413]
WOS关键词	CORTICOTROPIN-RELEASING-FACTOR ; GLUCAGON-LIKE PEPTIDE-1 ; VASOACTIVE INTESTINAL POLYPEPTIDE ; CYCLASE-ACTIVATING POLYPEPTIDE ; EXTRACELLULAR DOMAIN ; PARATHYROID-HORMONE ; CRYSTAL-STRUCTURE ; MOLECULAR RECOGNITION ; METABOLIC STABILITY ; INTERNATIONAL UNION
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000301187300003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278166]
专题	药物靶标结构与功能中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Melcher, Karsten
作者单位	1.Van Andel Res Inst, Lab Struct Sci, Grand Rapids, MI 49503 USA; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Struct & Funct Drug Targets, VARI SIMM Ctr,State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Pal, Kuntal,Melcher, Karsten,Xu, H. Eric. Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors[J]. ACTA PHARMACOLOGICA SINICA,2012,33(3):300-311.
APA	Pal, Kuntal,Melcher, Karsten,&Xu, H. Eric.(2012).Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors.ACTA PHARMACOLOGICA SINICA,33(3),300-311.
MLA	Pal, Kuntal,et al."Structure and mechanism for recognition of peptide hormones by Class B G-protein-coupled receptors".ACTA PHARMACOLOGICA SINICA 33.3(2012):300-311.