Profiling the kinome for drug discovery

Drug Discovery Today: Technologies - Tập 3 - Trang 269-276 - 2006
S. Frank Yan1, Frederick J. King2,3, Yingyao Zhou1, Markus Warmuth4, Gang Xia4
1Cheminformatics, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA
2Lead Discovery, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA
3Developmental and Molecular Pathways, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, MA, 02139, USA
4Kinase Drug Discovery, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA

Tài liệu tham khảo

Bimbo, 2005, Systematic deletion analysis of fission yeast protein kinases, Eukaryot. Cell, 4, 799, 10.1128/EC.4.4.799-813.2005 Manning, 2002, The protein kinase complement of the human genome, Science, 298, 1912, 10.1126/science.1075762 Hopkins, 2002, The druggable genome, Nat. Rev. Drug Discov., 1, 727, 10.1038/nrd892 Stoughton, 2005, How molecular profiling could revolutionize drug discovery, Nat. Rev. Drug Discov., 4, 345, 10.1038/nrd1696 Ley, 2003, A pilot study of high-throughput, sequence-based mutational profiling of primary human acute myeloid leukemia cell genomes, Proc. Natl. Acad. Sci. U S A, 100, 14275, 10.1073/pnas.2335924100 Schnittger, 2006, D324N single-nucleotide polymorphism in the FLT3 gene is associated with higher risk of myeloid leukemias, Genes Chromosomes Cancer, 45, 332, 10.1002/gcc.20294 Lynch, 2004, Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib, N. Engl. J. Med., 350, 2129, 10.1056/NEJMoa040938 Bardelli, 2003, Mutational analysis of the tyrosine kinome in colorectal cancers, Science, 300, 949, 10.1126/science.1082596 Kling, 2005, The search for a sequencing thoroughbred, Nat. Biotechnol., 23, 1333, 10.1038/nbt1105-1333 Carr, 2005, Mapping posttranslational modifications of proteins by MS-based selective detection: application to phosphoproteomics, Methods Enzymol., 405, 82, 10.1016/S0076-6879(05)05005-6 Corthals, 2005, Identification of phosphorylation sites using microimmobilized metal affinity chromatography, Methods Enzymol., 405, 66, 10.1016/S0076-6879(05)05004-4 Bose, 2006, Phosphoproteomic analysis of Her2/neu signaling and inhibition, Proc. Natl. Acad. Sci. U S A, 103, 9773, 10.1073/pnas.0603948103 Echeverri, 2006, High-throughput RNAi screening in cultured cells: a user's guide, Nat. Rev. Genet., 7, 373, 10.1038/nrg1836 Moffat, 2006, Building mammalian signalling pathways with RNAi screens, Nat. Rev. Mol. Cell. Biol., 7, 177, 10.1038/nrm1860 Fitzgerald, 2005, RNAi versus small molecules: different mechanisms and specificities can lead to different outcomes, Curr. Opin. Drug Discov. Devel., 8, 557 Yan, S.F. et al. Learning from the data: mining of large high-throughput screening databases. J. Chem. Inf. Model., doi:10.1021/ci060102u Fabian, 2005, A small molecule-kinase interaction map for clinical kinase inhibitors, Nat. Biotechnol., 23, 329, 10.1038/nbt1068 Vieth, 2005, Kinomics: characterizing the therapeutically validated kinase space, Drug Discov. Today, 10, 839, 10.1016/S1359-6446(05)03477-X Melnick, 2006, An efficient rapid system for profiling the cellular activities of molecular libraries, Proc. Natl. Acad. Sci. U S A, 103, 3153, 10.1073/pnas.0511292103 Vieth, 2004, Kinomics-structural biology and chemogenomics of kinase inhibitors and targets, Biochim. Biophys. Acta, 1697, 243, 10.1016/j.bbapap.2003.11.028 Chuaqui, 2005, Interaction profiles of protein kinase-inhibitor complexes and their application to virtual screening, J. Med. Chem., 48, 121, 10.1021/jm049312t Steinert, 2005, Imatinib mesylate in the treatment of gastrointestinal stromal tumour, Expert Opin. Pharmacother., 6, 105, 10.1517/14656566.6.1.105 Yan, 2005, Novel statistical approach for primary high-throughput screening hit selection, J. Chem. Inf. Model., 45, 1784, 10.1021/ci0502808 Buijsman, 2004, Structural aspects of kinases and their inhibitors, 191 Weinstein, 1997, An information-intensive approach to the molecular pharmacology of cancer, Science, 275, 343, 10.1126/science.275.5298.343 Covell, 2005, Linking tumor cell cytotoxicity to mechanism of drug action: an integrated analysis of gene expression, small-molecule screening and structural databases, Proteins, 59, 403, 10.1002/prot.20392 Zhou, 1998, Tumour amplified kinase STK15/BTAK induces centrosome amplification, aneuploidy and transformation, Nat. Genet., 20, 189, 10.1038/2496 Gilbertson, 2003, PDGFRB is overexpressed in metastatic medulloblastoma, Nat. Genet., 35, 197, 10.1038/ng1103-197 Daley, 1990, Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome, Science, 247, 824, 10.1126/science.2406902 Golub, 1994, Fusion of PDGF receptor beta to a novel ets-like gene, tel, in chronic myelomonocytic leukemia with t(5;12) chromosomal translocation, Cell, 77, 307, 10.1016/0092-8674(94)90322-0 Davies, 2002, Mutations of the BRAF gene in human cancer, Nature, 417, 949, 10.1038/nature00766 Cappellen, 1999, Frequent activating mutations of FGFR3 in human bladder and cervix carcinomas, Nat. Genet., 23, 18, 10.1038/12615 Baxter, 2005, Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders, Lancet, 365, 1054, 10.1016/S0140-6736(05)74230-6 Yamazaki, 1988, Amplification of the structurally and functionally altered epidermal growth factor receptor gene (c-erbB) in human brain tumors, Mol. Cell. Biol., 8, 1816, 10.1128/MCB.8.4.1816 Hirota, 1998, Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors, Science, 279, 577, 10.1126/science.279.5350.577 Kiyoi, 1997, Internal tandem duplication of FLT3 associated with leukocytosis in acute promyelocytic leukemia, Leukemia, 11, 1447, 10.1038/sj.leu.2400756 Hermanson, 1992, Platelet-derived growth factor and its receptors in human glioma tissue: expression of messenger RNA and protein suggests the presence of autocrine and paracrine loops, Cancer Res., 52, 3213 Li, 1997, PTEN, a putative protein tyrosine phosphatase gene mutated in human brain, breast, and prostate cancer, Science, 275, 1943, 10.1126/science.275.5308.1943