期刊
EXPERT OPINION ON THERAPEUTIC PATENTS
卷 28, 期 2, 页码 139-145出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2018.1414183
关键词
Anticancer agents; cancer therapy; focal adhesion kinase (FAK); non-receptor tyrosine kinase; small molecule FAK inhibitors
资金
- China Major Projects on Control and Rectification of Water Body Pollution [2017ZX07602-002]
Introduction: Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes at sites of cell adhesion to the extracellular matrix (ECM) and mediates signalling events downstream of integrin engagement of the ECM. FAK is known to regulate cell survival, proliferation and migration. Areas covered: FAK expression has also been shown to be up-regulated in many cancer types. Previous study also indicates that FAK-mediated signaling and functions are intrinsically involved in the progression of tumor aggressiveness, suggesting that FAK is a promising target for anticancer therapies. Small molecule FAK inhibitors have been developed and are being tested in clinical phase trials. Expert Opinion: These inhibitors have demonstrated to be effective by inducing tumor cell apoptosis in addition to reducing metastasis and angiogenesis. In this review, we give updates on the design, synthesis and structure-activity relationship analysis of small molecule FAK inhibitors discovered from 2015 until now. We also review the FAK inhibitors that are in clinical development and highlight the future prospects.
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