Inhibitors of Ras farnesyltransferases.

Inhibitors of Ras farnesyltransferases.
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DOI:
10.1016/0968-0004(93)90072-u
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发表时间:
1993-09
影响因子:
13.8
通讯作者:
Fuyuhiko Tamanoi
Fuyuhiko Tamanoi
中科院分区:
生物学1区
文献类型:
--
作者:
Fuyuhiko Tamanoi

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法尼基转移酶催化胆固醇前体法尼基焦磷酸对蛋白质的翻译后修饰。这种酶的底物之一是癌基因的产物。最近,法尼基转移酶的抑制剂已经通过两种不同的方法确定:天然化合物的微生物筛选和底物类似物。这些抑制剂可用于阻断Ras蛋白的作用,进一步表征蛋白质异戊二烯基转移酶,并阐明胆固醇代谢的调节。
Farnesyltransferase catalyses the post-translational modification of proteins by a cholesterol precursor, farnesylpyrophosphate. One of the substrates of this enzyme is the product of therasoncogene. Recently, inhibitors of farnesyltransferase have been identified through two different approaches: microbial screens for natural compounds, and substrate analogues. These inhibitors may be useful in blocking the action of Ras proteins, in further characterizing protein prenyltransferases, and in elucidating the regulation of cholesterol metabolism.