Binding mutant kinases

The Signalchem human kinase panel consists of 273 wt kinases (including some lipid kinases), 3 mutant kinases and 17 kinases with special binding partners or constructs. For more information, see http //www.signalchem.com/ disco very.php type= l catfiler= 12. 

A crystal structure of the mutant T790M kinase is available that shows the new gatekeeper methionine able to move to accommodate a bound inhibitor. This is consistent with the observed binding of inhibitors to mutant and double mutant kinases containing this mutation.74... 

Petruzzelli L, Herrera R, Arenas-Garcia R, Fernandez R, Bimbaum MJ, Rosen OM 1986 Isolation of a Drosophila genomic sequence homologous to the kinase domain of the human insulin receptor and detection of the phosphorylated Drosophila receptor with an anti-peptide antibody. Proc Natl Acad Sci USA 83 4710-4714 Podskalny J, McElduff A, Gorden P 1984 Insulin receptors on Chinese hamster ovary (CHO) cells altered insulin binding to glycosylation mutants. Biochem Biophys Res Commun 125 70-75... 

Receptor t5n osine kinases are involved in a myriad of signaling pathways, and active mutants promote oncogenesis in animals and in human [reviewed in (Blume-Jensen and Hunter 2001)]. All RTKs are characterized by an extracellular ligand-binding domain, a single transmembrane domain. 

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