小分子 MDM2 拮抗剂对 p53 的药理学激活。
Pharmacologic activation of p53 by small-molecule MDM2 antagonists.
机构信息
Department of Anatomy and Cell Biology Rush University Medical Center 1750 W Harrison Ave Jelke Building, Room 1306, USA.
出版信息
Curr Pharm Des. 2011;17(6):560-8. doi: 10.2174/138161211795222603.
Abstract
Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2 binding inhibitors have been developed during the past several years. Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on Nutlin-3.
摘要
通过抑制 p53 与 MDM2 之间的相互作用来恢复 p53 的活性，这代表了癌症治疗的一种有吸引力的方法。为此，在过去的几年中，已经开发了许多小分子 p53-MDM2 结合抑制剂。Nutlin-3 是一种有效的、选择性的小分子 MDM2 拮抗剂，在临床前研究中显示出了很大的潜力。这篇综述将重点介绍小分子 MDM2 拮抗剂作为潜在癌症治疗剂的最新进展，特别强调 Nutlin-3。
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