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14-September-2008 18:02:40 - kinase inhibitor A protein kinase inhibitor is a type of enzyme inhibitor which specifically blocks the action of protein kinase. Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinase.1 They can interfere with the repair of DNA double-strand breaks.2 Examples Currently there are several drugs launched that target protein kinases and the receptors that activate them: Name Target Company Class Bevacizumab VEGF Genentech Monoclonal antibody BIBW 2992 EGFR and Erb2 Boehringer Ingelheim Small molecule Cetuximab Erb1 Imclone/BMS Monoclonal antibody Imatinib Bcr-Abl Novartis Small molecule Trastuzumab Erb2 Genentech/Roche Monoclonal antibody Gefitinib EGFR AstraZeneca Small molecule Ranibizumab VEGF Genentech Monoclonal antibody Pegaptanib VEGF OSI/Pfizer Small molecule Sorafenib multiple targets Onyx/Bayer Small molecule Dasatinib multiple targets BMS Small molecule Sunitinib multiple targets Pfizer Small molecule Erlotinib Erb1 Genentech/Roche Small molecule Nilotinib Bcl-Abr Novartis Small molecule Lapatinib Erb1/Erb2 GSK Small molecule Panitumumab EGFR Amgen Monoclonal antibody References ^ Definition of tyrosine kinase inhibitor - NCI Dictionary of Cancer Terms. ^ Zhao Y, Thomas HD, Batey MA, et al May 2006. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 66 10: 5354-62. doi:10.1158/0008-5472.CAN-05-4275. PMID 16707462. External links MeSH Protein+kinase+inhibitors IC50 values for common inhibitors KinaseCentral.com v d e Pharmacology: enzyme inhibition Class Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition Substrate Oxidoreductase EC 1: Aromatase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors - COX-2 inhibitor Transferase EC 2: Integrase inhibitor - Protein kinase inhibitors - Reverse transcriptase inhibitors - COMT inhibitors Hydrolase EC 3: Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors ACE inhibitor, Trypsin inhibitor - Histone deacetylase inhibitor Lyase EC 4: Carbonic anhydrase inhibitors v d e Chemotherapeutic agents/Antineoplastic agents L01 Purine+pyrimidine/ Ribonucleotides/ Deoxyribonucleotides Antimetabolites Folic acid Aminopterin, Methotrexate, Pemetrexed, Raltitrexed Purine Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine Pyrimidine Cytarabine, Decitabine, Fluorouracil/Capecitabine, Floxuridine, Gemcitabine, Enocitabine, Sapacitabine DNA Alkylating/alkylating-like Nitrogen mustards Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan, Bendamustine, Trofosfamide, Uramustine Nitrosoureas Carmustine, Fotemustine, Lomustine, Nimustine, Prednimustine, Ranimustine, Semustine, Streptozocin Platinum alkylating-like Carboplatin, Cisplatin, Nedaplatin, Oxaliplatin, Triplatin tetranitrate, Satraplatin Alkyl sulfonates Busulfan, Mannosulfan, Treosulfan Hydrazines Procarbazine Triazenes Dacarbazine, Temozolomide Aziridines Carboquone, ThioTEPA, Triaziquone, Triethylenemelamine Spindle poisons/mitotic inhibitors Taxanes Docetaxel, Larotaxel, Ortataxel, Paclitaxel, Tesetaxel · Vinca alkaloids Vinblastine, Vincristine, Vinflunine, Vindesine, Vinorelbine · Ixabepilone Cytotoxic/antitumor antibiotics Anthracyclines Aclarubicin, Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Amrubicin, Pirarubicin, Valrubicin, Zorubicin Anthracenediones Mitoxantrone, Pixantrone Streptomyces Actinomycin, Bleomycin, Mitomycin, Plicamycin · Hydroxyurea Topoisomerase inhibitors Camptotheca Camptothecin, Topotecan, Irinotecan, Rubitecan, Belotecan · Podophyllum Etoposide, Teniposide Other Altretamine · Amsacrine · Bexarotene · Estramustine · Irofulven · Trabectedin Cellular CI monoclonal antibodies Receptor tyrosine kinase Cetuximab, Panitumumab, Trastuzumab · CD20 Rituximab, Tositumomab · other Alemtuzumab, Bevacizumab, Edrecolomab, Gemtuzumab Tyrosine kinase inhibitors Axitinib · Bosutinib · Cediranib · Dasatinib · Erlotinib · Gefitinib · Imatinib · Lapatinib · Lestaurtinib · Nilotinib · Semaxanib · Sorafenib · Sunitinib · Vandetanib Cyclin-dependent kinase inhibitors Alvocidib · Seliciclib Other Fusion protein Aflibercept · Denileukin diftitox Other/ungrouped Photosensitizers Aminolevulinic acid/Methyl aminolevulinate · Efaproxiral · Porphyrin derivatives Porfimer sodium, Talaporfin, Temoporfin, Verteporfin Other Retinoids Alitretinoin, Tretinoin · Anagrelide · Arsenic trioxide · Asparaginase/Pegaspargase · Atrasentan · Bortezomib · Carmofur · Celecoxib · Demecolcine · Elesclomol · Elsamitrucin · Etoglucid · Lonidamine · Lucanthone · Masoprocol · Mitobronitol · Mitoguazone · Mitotane · Oblimersen · Omacetaxine · Sitimagene ceradenovec · Tegafur · Testolactone · Tiazofurine · Tipifarnib · Vorinostat This biochemistry article is a stub. Retrieved from http://en..org/wiki/Protein_kinase_inhibitor Categories: Biochemistry stubs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch This page was last modified on 24 August 2008, at 19:20
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