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.
Keywords: Anticancer, antimalaria, farnesyltransferase, FTase inhibitors, FTase inhibitory activity, selectivity.
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