title: Molecular targeting of protein kinases to optimize selectivity and resistance profiles of kinase inhibitors.
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.
authors: TransTech Pharma Inc., 4170 Mendenhall Oaks Pkwy, High Point, NC 27265, USA. jliao@ttpharma.com
authors: Jeffrey Jie-Lou
authors: JJ
authors: Liao
mesh_terms: D001665:Binding Sites; D019008:Drug Resistance, Neoplasm; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy*; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000627:therapeutic use; D011494:Protein Kinases / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011494:Protein Kinases