Receptor tyrosine kinases progression

The mutation of certain receptor tyrosine kinase genes can result in the expression of receptors that exist in a constimtively active state (i.e. they are always produced). Such mutated genes may act as oncogenes, genes that contribute to the initiation or progression of cancer. 

Growth factor receptor tyrosine kinases can activate multiple pathways that lead to mitogenesis. There are many examples of growth factor receptor overexpression in tumor cells, and their constitutive activation by various mechanisms is related to tumor formation or progression (Karunagaran et al., 1996 Tsujimura, 1996 Empereur et al., 1997 Borset et al., 1996 Moscatello et al., 1996 Schmidt et al., 1997 Santoro et al., 1995). Many of the above-described MSP-Ron signaling molecules are known to cause cell transformation. For example, Ras genes are mutated in 20-30% of human cancers and the encoded proteins are believed to contribute to the patho-... 

G. Bollag, P.A. Trail, Bay 43-9006 exhibits broad spectrum oral antitumor activity and targets the raf/mek/erk pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis, Cancer Res. 2004, 64(19), 7099-109. 

Ahmad N, Gab H, Javed S, Agarwal R. Skin cancer chemopreventive effects of a flavonoid antioxidant silymarin are mediated via impairment of receptor tyrosine kinase signaling and perturbation in cell cycle progression. Biochem Biophys Res Commiin 1998 247 294-301. 

The c Met receptor tyrosine kinase is one of the RTKs most frequently mutated or abnormally activated in late stage human cancers, and plays a critical role in regulation of tumor progression, invasive growth, and tumor angiogenesis. The triazolopyrazine core was discovered to yield potent... 

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