Isoprenoid modification and plasma membrane association: critical factors for ras oncogenicity.
Isoprenoid modification and plasma membrane association: critical factors for ras oncogenicity.
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发表时间：
1991-09
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通讯作者：
C. Der;A. Cox
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作者：
C. Der;A. Cox
ras蛋白与质膜的结合是其转化活性的关键。这种关联是由一系列翻译后修饰促进的，这些修饰由所有ras蛋白中存在的共有C-末端CAAX基序发出信号。最近的发现，一个15-碳类异戊二烯（法呢基）组，来自胆固醇生物合成中的一个重要中间体，被共价连接到ras蛋白刺激了相当大的兴趣，并提出了几个重要的新方向的ras研究。特别是，一个有前途的药理学方法拮抗致癌ras活性在人类恶性肿瘤将设计特定的抑制剂的酶催化ras加工，从而干扰ras蛋白与质膜。
Association of ras protein with the plasma membrane is critical for its transforming activity. This association is promoted by a series of post-translational modifications that are signaled by the consensus C-terminal CAAX motif present in all ras proteins. The recent discovery that a 15-carbon isoprenoid (farnesyl) group, derived from an essential intermediate in cholesterol biosynthesis, is attached covalently to ras proteins has stimulated considerable interest and has suggested several important new directions for ras studies. In particular, one promising pharmacologic approach for antagonizing oncogenic ras activity in human malignancies would be to design specific inhibitors of the enzymes that catalyze ras processing and thereby interfere with ras protein association with the plasma membrane.