title: Design strategies for protein kinase inhibitors.
abstract: Deregulation of protein kinases due to mutation or overexpression is a hallmark of several diseases, for example, cancer, diabetes, inflammation and cardiovascular disorders. Consequently, there has been a growing interest in the discovery of protein kinase inhibitors as novel drugs. Here, we focus on key milestones and advances in protein kinase inhibitor drug discovery over the last year, with an emphasis on novel strategies such as targeting of single and multiple binding sites, inactive conformations of kinases, allosteric sites, regulatory domains and heat shock proteins. We will highlight recent developments for specific inhibitors in clinical studies for growth factor receptors, non-receptor tyrosine kinases and serine/threonine kinases.
authors.affiliation: University of Rhode Island, Department of Biomedical and Pharmaceutical Sciences, Kingston, RI 02881, USA. kparang@uri.edu
authors.forename: Keykavous
authors.initials: K
authors.lastname: Parang
authors.forename: Gongqin
authors.initials: G
authors.lastname: Sun
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods* / Q000639:trends; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D017978:Receptors, Growth Factor
chemical_list: D047428:Protein Kinase Inhibitors; D017978:Receptors, Growth Factor; D020794:Receptor Protein-Tyrosine Kinases