孤儿核受体雌激素相关受体α选择性反向激动剂的鉴定
Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha.
作者信息
Busch Brett B, Stevens William C, Martin Richard, Ordentlich Peter, Zhou Sihong, Sapp Douglas W, Horlick Robert A, Mohan Raju
机构信息
Department of Medicinal Chemistry, X-Ceptor Therapeutics, Inc., 4757 Nexus Center Drive, San Diego, California 92121, USA.
出版信息
J Med Chem. 2004 Nov 4;47(23):5593-6. doi: 10.1021/jm049334f.
The estrogen-related receptor alpha (ERRalpha) is an orphan receptor belonging to the nuclear receptor superfamily. The physiological role of ERRalpha has yet to be established primarily because of lack of a natural ligand. Herein, we describe the discovery of the first potent and selective inverse agonist of ERRalpha. Through in vitro and in vivo studies, these ligands will elucidate the endocrine signaling pathways mediated by ERRalpha including association with human disease states.
雌激素相关受体α（ERRα）是一种属于核受体超家族的孤儿受体。ERRα的生理作用尚未完全明确，主要原因是缺乏天然配体。在此，我们描述了首个强效且选择性的ERRα反向激动剂的发现。通过体外和体内研究，这些配体将阐明由ERRα介导的内分泌信号通路，包括与人类疾病状态的关联。
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