REV-ERB 和 ROR 核受体作为药物靶点。
REV-ERB and ROR nuclear receptors as drug targets.
机构信息
Department of Molecular Therapeutics, The Scripps Research Institute, 130 Scripps Way, Jupiter, Florida 33458, USA.
Department of Pharmacological & Physiological Science, Saint Louis University School of Medicine, 1402 South Grand Blvd, St. Louis, Missouri 63104, USA.
出版信息
Nat Rev Drug Discov. 2014 Mar;13(3):197-216. doi: 10.1038/nrd4100.
Abstract
The nuclear receptors REV-ERB (consisting of REV-ERBα and REV-ERBβ) and retinoic acid receptor-related orphan receptors (RORs; consisting of RORα, RORβ and RORγ) are involved in many physiological processes, including regulation of metabolism, development and immunity as well as the circadian rhythm. The recent characterization of endogenous ligands for these former orphan nuclear receptors has stimulated the development of synthetic ligands and opened up the possibility of targeting these receptors to treat several diseases, including diabetes, atherosclerosis, autoimmunity and cancer. This Review focuses on the latest developments in ROR and REV-ERB pharmacology indicating that these nuclear receptors are druggable targets and that ligands targeting these receptors may be useful in the treatment of several disorders.
摘要
REV-ERB（由 REV-ERBα 和 REV-ERBβ 组成）和视黄酸受体相关孤儿受体（由 RORα、RORβ 和 RORγ 组成）是核受体，参与许多生理过程，包括代谢、发育和免疫以及昼夜节律的调节。这些先前的孤儿核受体的内源性配体的最近特征表明，合成配体的发展和靶向这些受体治疗多种疾病的可能性，包括糖尿病、动脉粥样硬化、自身免疫和癌症。这篇综述重点介绍了 ROR 和 REV-ERB 药理学的最新进展，表明这些核受体是可成药的靶点，靶向这些受体的配体可能对治疗多种疾病有用。
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