Imatinib mesylate enzyme inhibition

Protein kinases can be classified according to the amino acid residue that is phosphorylated in the cellular process. Consequently, there are tyrosine-specific kinases and serine/threonine kinases. Tyrosine kinases are a family of tightly regulated enzymes, and the aberrant activation of various members of this family is one of the hallmarks of cancer. Tyrosine phosphorylation has been linked to multiple cell growth and differentiation pathways. Imatinib mesylate (1) is a tyrosine kinase inhibitor (TKI). An important characteristic of imatinib mesylate (1) is that it is an ATP-competitive inhibitor. It binds at the ATP binding site and blocks ATP binding thereby inhibiting kinase activities. [Pg.31]

Imatinib mesylate (Gleevec , Novartis) is a small-molecule compound that inhibits a specific tyrosine kinase enzyme, the Bcr-Abl fusion oncoprotein. It is used for gastrointestinal stromal tumor and chronic myeloid leukemia. [Pg.50]