Src-family tyrosine kinase (SFK) (SFK)

The Src-family tyrosine kinases (SFKs) are a group of non-receptor protein tyrosine kinases that play a critical role in regulating signal transduction pathways associated with cell growth, differentiation, motility, and survival (UniProt P12931). The family includes members such as Src, Fyn, Yes, Lck, Lyn, Hck, Fgr, and Blk, with Src being the most extensively studied. In various malignancies, including ovarian and lung cancers, SFKs are frequently overexpressed or hyperactivated, promoting tumor progression, metastasis, and resistance to standard chemotherapy (PubMed PMID: 22964666). Dasatinib is a small-molecule inhibitor that targets these kinases, and its use in combination with chemotherapy agents like paclitaxel and carboplatin is intended to sensitize tumor cells to apoptosis and overcome drug resistance (NCI Drug Dictionary). By inhibiting SFK activity, dasatinib disrupts the oncogenic signaling cascades, such as the PI3K/Akt and MAPK pathways, that contribute to the aggressive phenotype of cancer cells. This combination approach has been explored in clinical trials to improve outcomes in patients with advanced solid tumors where SFK signaling is a known driver of malignancy.

Other names

c-Srcp60-SrcProto-oncogene c-SrcSRC1pp60c-src

Dasatinib acts as a potent, ATP-competitive inhibitor of the Src family kinases, binding to the active and inactive conformations of the kinase domain to block downstream signaling pathways involved in cell survival and proliferation (PubChem CID 10635).