Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy
| Autor: | Yin-Ru Li, Yan-Bing Zhang, Xin-Yi Tian, Cheng-Yun Jin, Yuan Liu, Xiao-Jing Pang, Xiu-Juan Liu, Sai-Yang Zhang, Jian Song, Wen-Bo Liu, Guang-Xi Yu |
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| Rok vydání: | 2021 |
| Předmět: |
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Molecular Pharmaceutical Science Organic chemistry Antineoplastic Agents Review Analytical Chemistry Focal adhesion 03 medical and health sciences PROTAC 0302 clinical medicine QD241-441 Neoplasms Drug Discovery Animals Molecular Targeted Therapy Physical and Theoretical Chemistry Cell adhesion Protein Kinase Inhibitors 030304 developmental biology 0303 health sciences Chemistry Drug discovery Proteolysis targeting chimera focal adhesion kinase Small molecule anticancer activity Chemistry (miscellaneous) Cell culture diaminopyrimidines 030220 oncology & carcinogenesis Focal Adhesion Protein-Tyrosine Kinases Cancer research Molecular Medicine triazine biological phenomena cell phenomena and immunity Tyrosine kinase Intracellular |
| Zdroj: | Molecules Molecules, Vol 26, Iss 4250, p 4250 (2021) |
| ISSN: | 1420-3049 |
| Popis: | FAK is a nonreceptor intracellular tyrosine kinase which plays an important biological function. Many studies have found that FAK is overexpressed in many human cancer cell lines, which promotes tumor cell growth by controlling cell adhesion, migration, proliferation, and survival. Therefore, targeting FAK is considered to be a promising cancer therapy with small molecules. Many FAK inhibitors have been reported as anticancer agents with various mechanisms. Currently, six FAK inhibitors, including GSK-2256098 (Phase I), VS-6063 (Phase II), CEP-37440 (Phase I), VS-6062 (Phase I), VS-4718 (Phase I), and BI-853520 (Phase I) are undergoing clinical trials in different phases. Up to now, there have been many novel FAK inhibitors with anticancer activity reported by different research groups. In addition, FAK degraders have been successfully developed through “proteolysis targeting chimera” (PROTAC) technology, opening up a new way for FAK-targeted therapy. In this paper, the structure and biological function of FAK are reviewed, and we summarize the design, chemical types, and activity of FAK inhibitors according to the development of FAK drugs, which provided the reference for the discovery of new anticancer agents. |
| Databáze: | OpenAIRE |
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