title: The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents.
abstract: Cancer is a serious disease characterized by the uncontrolled growth division of cells, and nowadays it remains a significant challenge for the medical field. Malaria is an infectious disease in the similar situation to cancer. Almost 40% people in the world live in areas with malaria risk and each year there are about 2 to 3 million people dying from malaria. Farnesyltransferase (FTase) that belongs to isoprenyltransferase family can catalyze the initial step of Ras-processing and is identified as a promising target for the treatment of cancer and malaria. During the past decade years, a large number of FTase inhibitors with anticancer or antimalarial activity have been reported and some of them are undergoing clinical development. This review mainly introduces the FTase inhibitors as anticancer and antimalarial agents, with focus on their enzyme inhibitory activity, stability and enzyme selectivity, etc. In particular, the promising new FTase inhibitors among them will be discussed in detail and the inspirations for their design will be highlighted.
authors.forename: Yan
authors.initials: Y
authors.lastname: Shen
authors.forename: Shengsheng
authors.initials: S
authors.lastname: Qiang
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China. mashutao@sdu.edu.cn.
authors.forename: Shutao
authors.initials: S
authors.lastname: Ma
mesh_terms: D000962:Antimalarials / Q000737:chemistry* / Q000378:metabolism; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism; D001555:Benzene Derivatives / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D010963:Plasmodium falciparum / Q000187:drug effects; D011485:Protein Binding; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000970:Antineoplastic Agents; D001555:Benzene Derivatives; D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D015800:Protozoan Proteins; D051231:Farnesyltranstransferase