title: Ten things you should know about protein kinases: IUPHAR Review 14.
abstract: Many human malignancies are associated with aberrant regulation of protein or lipid kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein and lipid kinases represent an important target class for treating human disorders. This review focus on 'the 10 things you should know about protein kinases and their inhibitors', including a short introduction on the history of protein kinases and their inhibitors and ending with a perspective on kinase drug discovery. Although the '10 things' have been, to a certain extent, chosen arbitrarily, they cover in a comprehensive way the past and present efforts in kinase drug discovery and summarize the status quo of the current kinase inhibitors as well as knowledge about kinase structure and binding modes. Besides describing the potentials of protein kinase inhibitors as drugs, this review also focus on their limitations, particularly on how to circumvent emerging resistance against kinase inhibitors in oncological indications.
authors: PIQUR Therapeutics, Basel, Switzerland.
authors: Doriano
authors: D
authors: Fabbro
authors: Novartis Institutes of Biomedical Research, Basel, Switzerland.
authors: Sandra W
authors: SW
authors: Cowan-Jacob
authors: Novartis Institutes of Biomedical Research, Basel, Switzerland.
authors: Henrik
authors: H
authors: Moebitz
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D055808:Drug Discovery; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011494:Protein Kinases / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases
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