文献类型：期刊文献

英文题名：New tricks for human farnesyltransferase inhibitor: cancer and beyond

作者：Wang, Jingyuan[1];Yao, Xue[1];Huang, Jin[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, 130 Mei Long Rd, Shanghai 200237, Peoples R China

年份：2017

卷号：8

期号：5

起止页码：841

外文期刊名：MEDCHEMCOMM

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000402049300003)】；

基金：This work was supported by grants from the Shanghai Committee of Science and Technology (grants 15431902000).

语种：英文

摘要：Human protein farnesyltransferase (FTase) catalyzes the addition of a C-15-farnesyl lipid group to the cysteine residue located in the COOH-terminal tetrapeptide motif of a variety of important substrate proteins, including well-known Ras protein superfamily. The farnesylation of Ras protein is required both for its normal physiological function, and for the transforming capacity of its oncogenic mutants. Over the last several decades, FTase inhibitors (FTIs) were developed to disrupt the farnesylation of oncogenic Ras as anticancer agents, and some of them have entered cancer clinical investigation. On the other hand, some substrates of FTase were demonstrated to be related with other human diseases, including Hutchinson-Gilford progeria syndrome, chronic hepatitis D, and cardiovascular diseases. In this review, we summarize the roles of FTase in malignant transformation, proliferation, apoptosis, angiogenesis, and metastasis of tumor cells, and the recently anticancer clinical research advances of FTIs. The therapeutic prospect of FTIs on several other human diseases is also discussed.