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Tyrosine Kinase Mechanisms and Pathways
Author(s) -
Cole Philip
Publication year - 2009
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.23.1_supplement.198.1
Subject(s) - proto oncogene tyrosine protein kinase src , tyrosine kinase , tyrosine , receptor tyrosine kinase , kinase , enzyme , chemistry , signal transduction , biochemistry , computational biology , microbiology and biotechnology , biology
Protein tyrosine kinases (PTKs) are critical signaling enzymes and their dysregulation in disease states has made them attractive targets for pharmacologic inhibition. We will highlight several of the chemical approaches that we have taken to analyze PTK catalytic mechanisms, substrate selection, and regulation. In particular we will describe how designed bisubstrate analog inhibitors of PTKs and chemical rescue of mutation have both been useful when combined with crystallographic and mass spec analysis. Representative tyrosine kinase examples to be discussed include: Src, Abl, and EGFR.