1. FAK inhibitors in cancer, a patent review - an update on progress.
- Author
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Ye YX, Cao YY, Xu LS, Wang HC, Liu XH, and Zhu HL
- Subjects
- Animals, Humans, Chemistry, Pharmaceutical, Drug Development, Molecular Targeted Therapy, Structure-Activity Relationship, Antineoplastic Agents pharmacology, Antineoplastic Agents chemistry, Drug Design, Focal Adhesion Protein-Tyrosine Kinases antagonists & inhibitors, Focal Adhesion Protein-Tyrosine Kinases metabolism, Neoplasms drug therapy, Neoplasms pathology, Neoplasms enzymology, Patents as Topic, Protein Kinase Inhibitors pharmacology, Protein Kinase Inhibitors chemistry
- Abstract
Introduction: Focal adhesion kinase (FAK) is a cytoplasmic non-receptor tyrosine kinase over-expressed in various malignancies which is related to various cellular functions such as adhesion, metastasis and proliferation., Areas Covered: There is growing evidence that FAK is a promising therapeutic target for designing inhibitors by regulating the downstream pathways of FAK. Some potential FAK inhibitors have entered clinical phase research., Expert Opinion: FAK could be an effective target in medicinal chemistry research and there were a variety of FAKIs have been patented recently. Here, we updated an overview of design, synthesis and structure-activity relationship of chemotherapeutic FAK inhibitors (FAKIs) from 2017 until now based on our previous work. We hope our efforts can broaden the understanding of FAKIs and provide new ideas and insights for future cancer treatment from medicinal chemistry point of view.
- Published
- 2024
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