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Src Kinases as Therapeutic Targets for Cancer

Lori C Kim, Lanxi Song, Eric B Haura

Nat Rev Clin Oncol. 2009 Oct;6(10):587-95.

PMID: 19787002

Abstract:

Src family kinases (SFKs) have a critical role in cell adhesion, invasion, proliferation, survival, and angiogenesis during tumor development. SFKs comprise nine family members that share similar structure and function. Overexpression or high activation of SFKs occurs frequently in tumor tissues and they are central mediators in multiple signaling pathways that are important in oncogenesis. SFKs can interact with tyrosine kinase receptors, such as EGFR and the VEGF receptor. SFKs can affect cell proliferation via the Ras/ERK/MAPK pathway and can regulate gene expression via transcription factors such as STAT molecules. SFKs can also affect cell adhesion and migration via interaction with integrins, actins, GTPase-activating proteins, scaffold proteins, such as p130(CAS) and paxillin, and kinases such as focal adhesion kinases. Furthermore, SFKs can regulate angiogenesis via gene expression of angiogenic growth factors, such as fibroblast growth factor, VEGF, and interleukin 8. On the basis of these important findings, small-molecule SFK inhibitors have been developed and are undergoing early phase clinical testing. In preclinical studies these agents can suppress tumor growth and metastases. The agents seem to be safe in humans and could add to the therapeutic arsenal against subsets of cancers.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP192705796-A FGF Receptor Tyrosine Kinase Inhibitor - CAS 192705-79-6 FGF Receptor Tyrosine Kinase Inhibitor - CAS 192705-79-6 192705-79-6 Price
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