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促肾上腺皮质激素释放因子受体:从分子生物学到药物设计

Corticotrophin-releasing factor receptors: from molecular biology to drug design.

作者信息

Chalmers D T, Lovenberg T W, Grigoriadis D E, Behan D P, De Souza E B

机构信息

Neurocrine Biosciences, San Diego, CA 92121, USA.

出版信息

Trends Pharmacol Sci. 1996 Apr;17(4):166-72. doi: 10.1016/0165-6147(96)81594-x.

DOI:10.1016/0165-6147(96)81594-x
PMID:8984745
Abstract

Corticotrophin-releasing factor (CRF) acts within both the brain and the periphery to coordinate the overall response of the body to stress. The involvement of the CRF systems in a variety of both CNS and peripheral disease states has stimulated great interest in this peptide as a potential site of therapeutic intervention. The recent cloning of multiple CRF receptor subtypes has precipitated a new era in CRF research that has allowed precise molecular, pharmacological and anatomical examination of mammalian CRF receptors. In this article, Derek Chalmers and colleagues highlight the major differences between the two classes of CRF receptors, CRF1 and CRF2, and a functionally related CRF-binding protein, and discuss the relevance of these sites to the ongoing development of CRF-based therapeutics.

摘要

促肾上腺皮质激素释放因子(CRF)在大脑和外周均发挥作用,以协调身体对应激的整体反应。CRF系统参与多种中枢神经系统和外周疾病状态,这激发了人们对这种肽作为潜在治疗干预靶点的极大兴趣。多种CRF受体亚型的近期克隆开启了CRF研究的新时代,使得对哺乳动物CRF受体进行精确的分子、药理学和解剖学研究成为可能。在本文中,德里克·查尔默斯及其同事着重介绍了两类CRF受体(CRF1和CRF2)以及一种功能相关的CRF结合蛋白之间的主要差异,并讨论了这些靶点与基于CRF的治疗药物正在进行的研发之间的相关性。

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