title: Targeting protein kinases in cancer therapy.
abstract: Over the years, many different tyrosine and serine/threonine protein kinases have been selected as candidates for drug discovery activities in oncology research, based either on their overexpression and/or dysfunction in a particular organ or tissue, or through their association in deregulated signal transduction/cell cycle pathways. This review summarises current preclinical and clinical knowledge of ATP-competitive, small molecule kinase inhibitors, and receptor or ligand-competitive antibodies of selected protein kinases in which drug discovery and development activities have advanced with some success.
authors.affiliation: Oncology Research, Novartis Pharma AG, CH-4002 Basel, Switzerland. doriano.fabbro@pharma.novartis.com
authors.forename: Doriano
authors.initials: D
authors.lastname: Fabbro
authors.forename: Carlos
authors.initials: C
authors.lastname: García-Echeverría
mesh_terms: D000255:Adenosine Triphosphate / Q000494:pharmacology; D000818:Animals; D000911:Antibodies, Monoclonal / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001549:Benzamides; D002467:Cell Nucleus / Q000187:drug effects / Q000201:enzymology; D003593:Cytoplasm / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D015316:Genetic Therapy; D006801:Humans; D000068877:Imatinib Mesylate; D008565:Membrane Proteins / Q000037:antagonists & inhibitors; D010879:Piperazines / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases / Q000235:genetics; D011743:Pyrimidines / Q000627:therapeutic use; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors; D017978:Receptors, Growth Factor / Q000037:antagonists & inhibitors; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors
chemical_list: D000911:Antibodies, Monoclonal; D000970:Antineoplastic Agents; D001549:Benzamides; D004791:Enzyme Inhibitors; D008565:Membrane Proteins; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D017978:Receptors, Growth Factor; C084881:flt3 ligand protein; D000068877:Imatinib Mesylate; D000255:Adenosine Triphosphate; D011494:Protein Kinases; D066246:ErbB Receptors; D020794:Receptor Protein-Tyrosine Kinases; D040262:Receptors, Vascular Endothelial Growth Factor