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Prenyl-binding domains: potential targets for Ras inhibitors and anti-cancer drugs.

机译:异戊二烯结合域:Ras抑制剂和抗癌药物的潜在靶标。

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摘要

Ras and Rho GTPases are prominent participants in malignant transformation. They possess an essential prenyl group (farnesyl or geranylgeranyl) that endows them with membrane-tethering ability and functional specificity. Accumulating evidence suggests that prenyl groups are involved primarily in lipid-protein interactions, and recent experiments point to prenyl-binding hydrophobic pockets in proteins regulating Ras and Rho in normal cells and cancer cells. This review presents the evidence for such prenyl-binding domains as significant players in the control of Ras-like GTPases, and the emerging concept of prenyl-binding domains as potential targets for Ras inhibitors and anti-cancer drugs.
机译:Ras和Rho GTPases是恶性转化的重要参与者。它们具有必需的异戊二烯基(法呢基或香叶基香叶基),赋予它们膜束缚能力和功能特异性。越来越多的证据表明,异戊二烯基团主要参与脂质-蛋白质的相互作用,最近的实验表明,正常细胞和癌细胞中调节Ras和Rho的蛋白质中异戊二烯基结合的疏水口袋。这篇综述提供了这样的证据,即异戊烯基结合结构域是控制Ras样GTPases的重要角色,而新兴的异戊二烯结合域概念也可能成为Ras抑制剂和抗癌药物的潜在靶标。

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