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垂体腺苷酸环化酶激活多肽（PACAP）1型受体（PAC1-R）酰肼类拮抗剂的发现与构效关系研究

Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).

作者信息

Beebe Xenia, Darczak Daria, Davis-Taber Rachel A, Uchic Marie E, Scott Victoria E, Jarvis Michael F, Stewart Andrew O

机构信息

Neuroscience Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-1066, USA.

出版信息

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2162-6. doi: 10.1016/j.bmcl.2008.01.052. Epub 2008 Jan 18.

DOI:10.1016/j.bmcl.2008.01.052
PMID:18272364
Abstract

Potent small molecule antagonists for the PAC(1)-R have been discovered. Previously known antagonists for the PAC(1)-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.

摘要

已发现针对PAC(1)-R的强效小分子拮抗剂。此前已知的PAC(1)-R拮抗剂是略有截短的肽配体。本文报道的酰肼是首次报道的针对这类B类GPCR的小分子拮抗剂。

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