Scaffold-based design of kinase inhibitors for cancer therapy.
暂无分享,去创建一个
[1] Kam Y. J. Zhang,et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity , 2008, Proceedings of the National Academy of Sciences.
[2] S. Agarwal,et al. Association of constitutively activated hepatocyte growth factor receptor (Met) with resistance to a dual EGFR/Her2 inhibitor in non-small-cell lung cancer cells , 2009, British Journal of Cancer.
[3] D. Barford,et al. Mechanism of Activation of the RAF-ERK Signaling Pathway by Oncogenic Mutations of B-RAF , 2004, Cell.
[4] Daniela Gabriel,et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity , 2008, Molecular Cancer Therapeutics.
[5] J. Llovet,et al. Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling , 2008, Molecular Cancer Therapeutics.
[6] John Kuriyan,et al. Activation of tyrosine kinases by mutation of the gatekeeper threonine , 2008, Nature Structural &Molecular Biology.
[7] M. Ratain,et al. Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis , 2006, British Journal of Cancer.
[8] Mathew J Garnett,et al. Guilty as charged: B-RAF is a human oncogene. , 2004, Cancer cell.
[9] John Kuriyan,et al. Protein-protein interactions in the allosteric regulation of protein kinases. , 2006, Current opinion in structural biology.
[10] Christopher W Murray,et al. Fragment-based lead discovery using X-ray crystallography. , 2005, Journal of medicinal chemistry.
[11] L. Sequist. First-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in EGFR Mutation: Positive Non-small Cell Lung Cancer Patients , 2008, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.
[12] Suzanne Schubbert,et al. Hyperactive Ras in developmental disorders and cancer , 2007, Nature Reviews Cancer.
[13] Nathanael Gray,et al. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors , 2009, Nature Reviews Drug Discovery.
[14] Yan Zhang,et al. KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients , 2009, Proceedings of the National Academy of Sciences.
[15] J. McCubrey,et al. Analysis of BRAF Mutation in Primary and Metastatic Melanoma , 2005, Cell cycle.
[16] N. Rosen,et al. HER kinase activation confers resistance to MET tyrosine kinase inhibition in MET oncogene-addicted gastric cancer cells , 2008, Molecular Cancer Therapeutics.
[17] H. Varmus,et al. Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain , 2005, PLoS medicine.
[18] M. Belvin,et al. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. , 2009, Cancer research.
[19] Irini Akritopoulou-Zanze,et al. Kinase-targeted libraries: the design and synthesis of novel, potent, and selective kinase inhibitors. , 2009, Drug discovery today.
[20] Zhengshuang Shi,et al. Networks for the allosteric control of protein kinases. , 2006, Current opinion in structural biology.
[21] J. Settleman,et al. Targeting the RAF-MEK-ERK pathway in cancer therapy. , 2009, Cancer letters.
[22] C. Antonescu,et al. Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor. , 2008, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[23] Yoshihisa Suzuki,et al. Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma. , 2005, Journal of molecular biology.
[24] Mladen Vinković,et al. Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. , 2009, Journal of medicinal chemistry.
[25] T. Hunter,et al. The Protein Kinase Complement of the Human Genome , 2002, Science.
[26] Apurva A Desai,et al. Sorafenib for treatment of renal cell carcinoma: Final efficacy and safety results of the phase III treatment approaches in renal cancer global evaluation trial. , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[27] Dexin Kong,et al. Advances in development of phosphatidylinositol 3-kinase inhibitors. , 2009, Current medicinal chemistry.
[28] T. Vitaz,et al. Factors affecting the outcome after treatment for metastatic melanoma to the brain. , 2009, Surgical neurology.
[29] I. Nagtegaal,et al. BRAF mutation in metastatic colorectal cancer. , 2009, The New England journal of medicine.
[30] T. Zhou,et al. Crystal Structure of the T315I Mutant of Abl Kinase , 2007, Chemical biology & drug design.
[31] P. Cohen. Protein kinases — the major drug targets of the twenty-first century? , 2002, Nature reviews. Drug discovery.
[32] Ming Zhou,et al. Regulation of Raf-1 by direct feedback phosphorylation. , 2005, Molecular cell.
[33] V. Sondak,et al. Targeting mutant BRAF and KIT in metastatic melanoma: ASCO 2009 meeting report , 2009, Pigment Cell & Melanoma Research.
[34] L. Pollak. Moyamoya disease and moyamoya syndrome. , 2009, The New England journal of medicine.
[35] C. Bokemeyer,et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. , 2008, Blood.
[36] PhD Mingzhao Xing MD,et al. BRAF Mutation in Papillary Thyroid Microcarcinoma: The Promise of Better Risk Management , 2008, Annals of Surgical Oncology.
[37] Jeffrey A. Engelman,et al. Targeting PI3K signalling in cancer: opportunities, challenges and limitations , 2009, Nature Reviews Cancer.
[38] C. Venot,et al. Insulin-Like Growth Factor-1 Receptor Inhibition Induces a Resistance Mechanism via the Epidermal Growth Factor Receptor/HER3/AKT Signaling Pathway: Rational Basis for Cotargeting Insulin-Like Growth Factor-1 Receptor and Epidermal Growth Factor Receptor in Hepatocellular Carcinoma , 2009, Clinical Cancer Research.
[39] Ralph Weissleder,et al. Effective Use of PI3K and MEK Inhibitors to Treat Mutant K-Ras G12D and PIK3CA H1047R Murine Lung Cancers , 2008, Nature Medicine.
[40] W. Sellers,et al. PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancers. , 2009, Cancer research.
[41] Edward S. Kim,et al. Implication of the Insulin-like Growth Factor-IR Pathway in the Resistance of Non–small Cell Lung Cancer Cells to Treatment with Gefitinib , 2007, Clinical Cancer Research.
[42] L. Wodicka,et al. A small molecule–kinase interaction map for clinical kinase inhibitors , 2005, Nature Biotechnology.
[43] Pixu Liu,et al. Targeting the phosphoinositide 3-kinase pathway in cancer , 2009, Nature Reviews Drug Discovery.
[44] Daniel Rauh,et al. A new screening assay for allosteric inhibitors of cSrc. , 2009, Nature chemical biology.
[45] N. Thomas. BRAF somatic mutations in malignant melanoma and melanocytic naevi , 2006, Melanoma research.
[46] C. Sander,et al. V600EBRAF is associated with disabled feedback inhibition of RAF–MEK signaling and elevated transcriptional output of the pathway , 2009, Proceedings of the National Academy of Sciences.
[47] A. Santoro,et al. Sorafenib therapy in advanced hepatocellular carcinoma: the SHARP trial , 2009, Expert review of anticancer therapy.
[48] A. Nicholson,et al. Mutations of the BRAF gene in human cancer , 2002, Nature.
[49] Kam Y. J. Zhang,et al. A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design , 2005, Nature Biotechnology.
[50] L. Johnson,et al. Protein Kinase Inhibitors: Insights into Drug Design from Structure , 2004, Science.
[51] Robert P. Davis,et al. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. , 2008, Bioorganic & medicinal chemistry letters.
[52] David Bebbington,et al. The discovery of the potent aurora inhibitor MK-0457 (VX-680). , 2009, Bioorganic & medicinal chemistry letters.
[53] Antonella Isacchi,et al. Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358. , 2007, Cancer research.
[54] Todd R. Golub,et al. BRAF mutation predicts sensitivity to MEK inhibition , 2006, Nature.
[55] William Pao,et al. MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib , 2007, Proceedings of the National Academy of Sciences.
[56] J. Bergh. Quo vadis with targeted drugs in the 21st century? , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[57] C. Erlichman,et al. HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924 , 2008, Molecular Cancer Therapeutics.
[58] Sung-Hou Kim,et al. Chapter 18:The Impact of Protein Kinase Structures on Drug Discovery , 2007 .
[59] N. Gray,et al. Targeting cancer with small molecule kinase inhibitors , 2009, Nature Reviews Cancer.
[60] P. Seeburg,et al. Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. , 2000, Science.
[61] Hieu T. Do,et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. , 2006, Cancer research.
[62] C. Sawyers,et al. Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. , 2001, The New England journal of medicine.
[63] Abran Q. Costales,et al. Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors. , 2008, Journal of medicinal chemistry.