The Development of FAK Inhibitors: A Five-Year Update

• Published in: International journal of molecular sciences Vol. 23; no. 12; p. 6381
• Main Authors: Spallarossa, Andrea, Tasso, Bruno, Russo, Eleonora, Villa, Carla, Brullo, Chiara
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 07-06-2022; MDPI
• Subjects: anticancer compounds; Apoptosis; Binding sites; Cell adhesion & migration; Cell growth; Competition; Drug dosages; FAK inhibitors; Focal adhesion kinase; Growth factors; Kinases; medicinal chemistry; Melanoma; Metastases; Ovarian cancer; Pharmaceutical industry; Phosphorylation; PROTAC; Protein-tyrosine kinase receptors; Proteins; pyrimidines; Review; Thyroid gland; Tumors; Tyrosine
• ISSN: 1422-0067; 1661-6596; 1422-0067
• 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.