Title: Molecular Targeting of Protein Kinases to Optimize Selectivity and Resistance Profiles of Kinase Inhibitors
Volume: 7
Issue: 14
Author(s): Liao Jie-Lou Jeffrey
Affiliation:
Keywords:
Protein kinase, protein kinase inhibitor, selectivity, imatinib, CML, drug-resistant mutation, systematic structural analysis
Abstract: This article reviews several important observations in the field of protein kinase drug discovery, exemplified mainly by targeting c-Abl for the treatment of CML. Structure-based strategy and insight are provided for the optimization of the selectivity and resistant mutation profiles of protein kinase inhibitors.