Pharmacologic activation of p53 by small-molecule MDM2 antagonists.

Pharmacologic activation of p53 by small-molecule MDM2 antagonists.
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DOI:
10.2174/138161211795222603
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发表时间:
2011
影响因子:
3.1
通讯作者:
Maki CG
Maki CG
中科院分区:
医学4区
文献类型:
--
作者:
Shen H;Maki CG

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通过抑制 p53 和 MDM2 之间的相互作用来恢复 p53 活性是一种有吸引力的癌症治疗方法。为此,在过去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小分子 MDM2 拮抗剂,在临床前研究中显示出巨大的前景。本综述将重点介绍小分子 MDM2 拮抗剂作为潜在癌症治疗药物的最新进展,特别是 Nutlin-3。
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.
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