Department of Pharmacy, University of Genova, Viale Benedetto XV, 3, 16132 Genova, Italy.
Int J Mol Sci. 2022 Jun 7;23(12):6381. doi: 10.3390/ijms23126381.
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor development and metastasis formation. To date, studies on the role of FAK and FAK inhibitors are of great interest for both pharmaceutical companies and academia. This review is focused on compounds able to block FAK with different potencies and with different mechanisms of action, that have appeared in the literature since 2017. Furthermore, new emerging PROTAC molecules have appeared in the literature. This summary could improve knowledge of new FAK inhibitors and provide information for future investigations, in particular, from a medicinal chemistry point of view.
黏着斑激酶（FAK）在不同的实体瘤中过度表达，是一种非受体酪氨酸激酶。近年来，FAK 已被认为是抗肿瘤药物开发的新靶点，有助于对抗肿瘤的发展和转移形成。迄今为止，FAK 及其抑制剂的研究对于制药公司和学术界都具有重要意义。本文综述了 2017 年以来文献中出现的具有不同效力和不同作用机制的能阻断 FAK 的化合物。此外，文献中还出现了新的新兴的 PROTAC 分子。这一综述可以提高对新型 FAK 抑制剂的认识，并为未来的研究提供信息，特别是从药物化学的角度。
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