Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
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DOI：
10.1039/c2md20299a
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发表时间：
2013-03
期刊：
影响因子：
--
通讯作者：
Distefano MD
中科院分区：
文献类型：
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作者：
Ochocki JD;Distefano MD
蛋白质异戊烯化的翻译后修饰是底物蛋白C-末端上的共价脂质修饰，其用于增强膜亲和力。致癌蛋白如Ras具有这种修饰，并且已经投入大量精力开发用于临床治疗的异戊烯基转移酶的抑制剂。除了癌症治疗，异戊烯基转移酶抑制剂已经开始在其他疾病中发现重要的治疗用途，包括早衰症、丙型肝炎和丁型肝炎、寄生虫感染和其他疾病。这篇综述将追踪异戊烯基转移酶抑制剂从最初作为癌症治疗药物到其在其他疾病中的扩展应用的演变。
The posttranslational modification of protein prenylation is a covalent lipid modification on the C-terminus of substrate proteins that serves to enhance membrane affinity. Oncogenic proteins such as Ras have this modification and significant effort has been placed into developing inhibitors of the prenyltransferase enzymes for clinical therapy. In addition to cancer therapy, prenyltransferase inhibitors have begun to find important therapeutic uses in other diseases, including progeria, hepatitis C and D, parasitic infections, and other maladies. This review will trace the evolution of prenyltransferase inhibitors from their initial use as cancer therapeutics to their expanded applications for other diseases.