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【Clin Cancer Res】靶向MDM2 与p53 相互作用的癌症治

Targeting the MDM2-p53 Interaction for Cancer Therapy

Abstract

p53 is a powerful tumor suppressor and is an attractive cancer therapeutic target because it can be functionally activated to eradicate tumors. The gene encoding p53 protein is mutated or deleted in half of human cancers, which inactivates its tumor suppressor activity. In the remaining cancers with wild-type p53 status, its function is effectively inhibited through direct interaction with the human murine double minute 2 (MDM2) oncoprotein. Blocking the MDM2-p53 interaction to reactivate the p53 function is a promising cancer therapeutic strategy. This review will highlight the advances in the design and development of small-molecule inhibitors of the MDM2-p53 interaction as a cancer therapeutic approach.

http://clincancerres.aacrjournals.org/cgi/content/abstract/14/17/5318 由于p53在功能上能被激活用于消灭肿瘤,它成为强大肿瘤抑制剂用于肿瘤治疗靶标。半数人类癌症患者都是编码p53蛋白的基因突变或丢失,抑制肿瘤抑制剂活化。剩余患者携带野生型p53基因,它的功能是通过直接作用于人类MDM2抑癌蛋白而有效抑制p53的抑癌作用。所以阻抑MDM2-p53 相互作用也是一个有力的癌症治疗策略。这是一篇综述:强调抑制MDM2-p53 交互作用的小分子抑制剂的设计和发展。 能看到全文吗?楼主有的话给我发一份,多谢!
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作者:admin@医学,生命科学    2011-06-15 17:11
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