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FTase inhibitors and cancer: prospects for use in targeted therapies

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Abstract

Farnesyltransferase (FTase) is a key enzyme that catalyzes the farnesylation of Ras protein. It is used to bind RAS protein to plasma membrane to complete signal transduction. Ras has been shown to be closely related to the development of many cancers. In recent years, FTase has been studied more deeply as an anticancer target. And more and more novel FTase inhibitors have been reported for the treatment of pancreatic cancer, lung cancer, colon cancer, HGPS, PL and so on. This review summarizes the structural features and biological activities of various novel FTase inhibitors reported since 2013. The reported novel FTase inhibitors were reclassified from the perspective of structure, their current tumor antagonism potential was summarized, and their current challenges and future development trends were further analyzed.

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Acknowledgements

This work was supported by the National Natural Science Foundation of China (No.82204210), the Hebei Natural Science Foundation (NO. H2022406062), the Funded by Science and Technology Project of Hebei Education Department (NO. QN2022161), the 2022 Research Start‐up Fund for High‐level Talents of Chengde Medical University (NO. 202207), and the Chengde Medical University basic research funds special project (NO. KY202315).

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  1. These authors contributed equally: Ming-tao Xia, Ling Yu

Authors and Affiliations

  1. Key Laboratory of Traditional Chinese Medicine Research and Development of Hebei Province, Hebei Key Laboratory of Nerve Injury and Repair, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde, 067000, P. R. China

    Ming-tao Xia, Zhi-wei Yan, You-de Wang, Li-ying Zhang, Guang-xin Miao & Shuai Li

  2. Department of Pharmacy, Anorectal Hospital of Chengde Medical University, Chengde, 067000, P. R. China

    Ling Yu

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Xia, Mt., Yu, L., Yan, Zw. et al. FTase inhibitors and cancer: prospects for use in targeted therapies. Med Chem Res 33, 21–35 (2024). https://doi.org/10.1007/s00044-023-03171-2

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