Work

FAK: A Potential Target for Cancer Therapy

Year: 2025

Type: editorial

Abstract: Focal adhesion kinase (FAK) is a nonreceptor tyrosine kinase with enzymatic and scaffolding functions, composed of a FERM domain, kinase domain, proline-rich regions, and a FAT domain. It interacts with over 50 proteins and plays a key role in cancer progression, metastasis, and recurrence. Although eight FAK inhibitors have entered clinical trials, they primarily block kinase activity and fail to disrupt scaffolding functions. PROTAC technology offers a novel strategy by degrading the entire FAK protein, eliminating both functions. Several FAK-targeting PROTACs have been developed with promising results. Given FAK's critical role in tumor malignancy, combination therapiessuch as dual-target degradation or inhibitor-degrader strategiesmay provide enhanced anticancer efficacy.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/acsmedchemlett.5c00184

Authors: Chao Zhang, Yu Rao

Institutions: Changping Laboratory, State Key Laboratory of Molecular Oncology, Tsinghua University

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funders: Beijing Frontier Research Center for Biological Structure, Tsinghua University, Beijing Outstanding Young Talents, National Natural Science Foundation of China, National Key Research and Development Program of China