从发现到临床：靶向泛素系统。
From Discovery to Bedside: Targeting the Ubiquitin System.
机构信息
Departments of Molecular Oncology and Early Discovery Biochemistry, Genentech, Inc., South San Francisco, CA 94008, USA.
Department of Discovery Chemistry, Genentech, Inc., South San Francisco, CA 94008, USA.
出版信息
Cell Chem Biol. 2019 Feb 21;26(2):156-177. doi: 10.1016/j.chembiol.2018.10.022. Epub 2018 Dec 13.
The ubiquitin/proteasome system is a primary conduit for selective intracellular protein degradation. Since its discovery over 30 years ago, this highly regulated system continues to be an active research area for drug discovery that is exemplified by several approved drugs. Here we review compounds in preclinical testing, clinical trials, and approved drugs, with the aim of highlighting innovative discoveries and breakthrough therapies that target the ubiquitin system.
泛素/蛋白酶体系统是细胞内选择性蛋白降解的主要途径。自 30 多年前发现以来，这个高度调控的系统一直是药物发现的活跃研究领域，有几种已批准的药物就是例证。在此，我们对处于临床前试验、临床试验和已批准药物阶段的化合物进行综述，旨在突出靶向泛素系统的创新发现和突破性疗法。
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