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Inc. The evaluate concludes with a conversation on the application of modern techniques and knowledge of the kinome as means to gear up the tyrosine kinase drug discovery process. Gene Mutation Disease EGFRvIII Extracellular domain name Glioblastoma, Ovarian tumor, Non small cell lung carcinoma FGFR3 Extracellular domain name Multiple myeloma BCR-ABL Translocation t(9:22) Chronic myeloid leukemia Acute lymphocytic leukemia TEl-ABL Translocation t(9:12) Itgav Acute lymphocytic leukemia TEL-PDGF Translocation t(5:12) Chronic myeloid monocytic leukemia EGFR and EGF, TGF Autocrine-paracrine loop Non small cell lung carcinoma Bladder malignancy Glioblastoma multiforme PDGFR and PDGF Autocrine-paracrine loop Glioma IGFR and IGF I and II Autocrine-paracrine loop Breast cancer Open in a separate window Table 2 Protein kinase inhibitors in clinical trials Inhibitor Target kinase(s) MAC glucuronide α-hydroxy lactone-linked SN-38 Company Malignancy Status Ref. /th /thead Small molecule inhibitors STI-571 Abl, c-kit, PDGFR Novartis CML, GIST launched 39 ZD1839 EGFR AstraZeneca NSCLC, SCC launched 40 OSI-774 EGFR OSI/Genetech SCC, BC, LC Phase III 75 PKI-166 EGFR, Her-2 Novartis general malignancy Phase II 76 PTK-787 VEGFR Novartis CR malignancy Phase III 77 SU5416 VEGFR Sugen solid tumor Phase III Monoclonal antibody Herceptin Her-2/neu Genetech BC FDA approved 46 MDX-H210 Her-2/neu Madarex BC Phase I 78 2C4 Her-2/neu Genetech BC, PC, OC Phase II – C225 EGFR Imclone Pan.C, BC, RenC Phase III – Antisense ISIS 3521 PKC- ISIS NSCLC, BC, Pan.C Phase II 79 GEM 231 PKA Hybridon CR, Pan.C, LC Phase I 80Immunotoxins Anti-Tac (Fv)-PE38 CD25 – MAC glucuronide α-hydroxy lactone-linked SN-38 B, T cell leukemia Phase I 81 DAB389IL2 IL-2R – CTCL, HD, B-NHL Phase III 82Hsp90 inhibitors Geldanamycin Hsp90 Conforma. Inc. Thyroid malignancy Phase I 83 17-AAG Hsp90 – BC MAC glucuronide α-hydroxy lactone-linked SN-38 Phase I Phase I 84 Open in a separate window BC- Breast malignancy, LC- Lung malignancy, NSCLC- Non small cell lung malignancy, SSC- squamous cell carcinoma, CR- Colorectal malignancy, CML- Chronic myeloid leukemia, GIST- Gastrointestinial stromal tumor, CTCL-Cutaneous T cell lymphoma, NHL- Non Hodgkins lymphoma, HD- Hodgkins disease, Pan.C C Pancreatic malignancy, Ren.C- Renal malignancy, KHK- Kyowa Hakko Kogyo Ltd. Glossary ABBREVIATIONSAML acute myeloid leukemiaALL acute lymphocytic leukemiaCML chronic myeloid leukemiaCMML chronic myelomonocytic leukemiaEGF epidermal growth factorFGF fibroblast growth factorFGFR fibroblast growth factor receptorGIST gastrointestinal stromal tumorIGF insulin like growth factorIGFR insulin like growth factor receptorMAPK mitogen activated protein kinasePDGFR platelet-derived growth factor receptorPDGF platelet-derived growth factorPI3K phosphatidyl inositol kinaseSH2 Src homology 2IR insulin receptormTOR mammalian target of rapamycin MAC glucuronide α-hydroxy lactone-linked SN-38 Biographies ?? Anup K. Mukhopadhyay is an Associate Professor of the Department of Biotechnology, National Institute of Pharmaceutical Education and Research, Punjab, India-160062. His research interest is in the area of mitochondrial bioenergetics of malignancy cell of haemato-oncologic diseases. His research interest also includes kinetics of electron transfer enzyme and reactive oxygen species. ?? Manash K. Paul is usually a PhD student of the Department of Biotechnology, National Institute of Pharmaceutical Education and Research, Punjab, India-160062. his current research includes target enzymes in malignancy therapeutics and mitochondrial bioenergetics in malignancy leukocyte..