异戊烯基转移酶抑制剂：治疗从癌症到寄生虫感染的人类疾病。
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
作者信息
Ochocki Joshua D, Distefano Mark D
机构信息
Department of Chemistry, University of Minnesota, Minneapolis, MN 55455 (USA).
出版信息
Medchemcomm. 2013 Mar;4(3):476-492. doi: 10.1039/C2MD20299A.
Abstract
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.
摘要
蛋白质异戊二烯化的翻译后修饰是在底物蛋白C末端进行的共价脂质修饰，用于增强膜亲和力。诸如Ras等致癌蛋白具有这种修饰，并且已经投入了大量努力来开发用于临床治疗的异戊二烯基转移酶抑制剂。除癌症治疗外，异戊二烯基转移酶抑制剂已开始在其他疾病中找到重要的治疗用途，包括早衰症、丙型和丁型肝炎、寄生虫感染及其他疾病。本综述将追溯异戊二烯基转移酶抑制剂从最初用作癌症治疗药物到其在其他疾病中的扩展应用的演变过程。
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