New approaches to molecular cancer therapeutics
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[1] P. Hergenrother,et al. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy , 2006, Nature chemical biology.
[2] R. Shoemaker. The NCI60 human tumour cell line anticancer drug screen , 2006, Nature Reviews Cancer.
[3] M. Lacouture. Mechanisms of cutaneous toxicities to EGFR inhibitors , 2006, Nature Reviews Cancer.
[4] Ronald A. DePinho,et al. Model organisms: The mighty mouse: genetically engineered mouse models in cancer drug development , 2006, Nature Reviews Drug Discovery.
[5] P. Sorger,et al. Systems biology and combination therapy in the quest for clinical efficacy , 2006, Nature chemical biology.
[6] Jaejoon Won,et al. Hexachlorophene Inhibits Wnt/β-Catenin Pathway by Promoting Siah-Mediated β-Catenin Degradation , 2006, Molecular Pharmacology.
[7] Adam Yasgar,et al. Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries. , 2006, Proceedings of the National Academy of Sciences of the United States of America.
[8] Herbert Waldmann,et al. Discovery of protein phosphatase inhibitor classes by biology-oriented synthesis. , 2006, Proceedings of the National Academy of Sciences of the United States of America.
[9] P. Workman,et al. Drugging the PI3 kinome , 2006, Nature Biotechnology.
[10] G. V. Paolini,et al. Global mapping of pharmacological space , 2006, Nature Biotechnology.
[11] N. Gray,et al. Rational design of inhibitors that bind to inactive kinase conformations , 2006, Nature chemical biology.
[12] R. Ficner,et al. Substrate and inhibitor specificity of class 1 and class 2 histone deacetylases. , 2006, Journal of biotechnology.
[13] Thomas LaFramboise,et al. Sensitive mutation detection in heterogeneous cancer specimens by massively parallel picoliter reactor sequencing , 2006, Nature Medicine.
[14] Rui Alves,et al. Tools for kinetic modeling of biochemical networks , 2006, Nature Biotechnology.
[15] M. Drysdale,et al. Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors , 2006, Molecular Cancer Therapeutics.
[16] Gerd Ulrich Nienhaus,et al. Automated high content screening for phosphoinositide 3 kinase inhibition using an AKT 1 redistribution assay. , 2006, Combinatorial chemistry & high throughput screening.
[17] Paul Workman,et al. Inhibitors of the HSP90 molecular chaperone: attacking the master regulator in cancer. , 2006, Current topics in medicinal chemistry.
[18] T. Haystead. The purinome, a complex mix of drug and toxicity targets. , 2006, Current topics in medicinal chemistry.
[19] S. Friend,et al. Cancer BiomarkersAn Invitation to the Table , 2006, Science.
[20] H. Varmus. The New Era in Cancer Research , 2006, Science.
[21] Sunkyu Kim,et al. Validating cancer drug targets , 2006, Nature.
[22] Paul Workman,et al. Minimally invasive pharmacokinetic and pharmacodynamic technologies in hypothesis-testing clinical trials of innovative therapies. , 2006, Journal of the National Cancer Institute.
[23] William A Weiss,et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. , 2006, Cancer cell.
[24] H. Madhani,et al. Selective kinase inhibition by exploiting differential pathway sensitivity. , 2006, Chemistry & biology.
[25] E. Sausville,et al. Contributions of human tumor xenografts to anticancer drug development. , 2006, Cancer research.
[26] E. Holland,et al. Genetically engineered models have advantages over xenografts for preclinical studies. , 2006, Cancer research.
[27] René Bernards,et al. An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors , 2006, Nature chemical biology.
[28] M. Clarke,et al. Stem Cells and Cancer: Two Faces of Eve , 2006, Cell.
[29] S. Fesik,et al. RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors , 2006, Oncogene.
[30] C. Marshall,et al. Identification of Inhibitors of the Kinase Activity of Oncogenic V600EBRAF in an Enzyme Cascade High-Throughput Screen , 2006, Journal of biomolecular screening.
[31] Todd R. Golub,et al. BRAF mutation predicts sensitivity to MEK inhibition , 2006, Nature.
[32] Dirk Strumberg,et al. Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment. , 2005, Drugs of today.
[33] M. Chatterjee‐Kishore,et al. Exploring the sounds of silence: RNAi-mediated gene silencing for target identification and validation. , 2005, Drug discovery today.
[34] L. Vassilev,et al. Targeting protein–protein interactions for cancer therapy , 2005, Journal of Molecular Medicine.
[35] Christopher W Murray,et al. Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation. , 2005, Journal of medicinal chemistry.
[36] James A. Lumley,et al. Compound selection and filtering in library design , 2005 .
[37] D. Bojanic,et al. Keynote review: in vitro safety pharmacology profiling: an essential tool for successful drug development. , 2005, Drug discovery today.
[38] P. Johnston,et al. Genomic profiling of cancer: what next? , 2005, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[39] P. Workman,et al. Pharmacokinetic-Pharmacodynamic Relationships for the Heat Shock Protein 90 Molecular Chaperone Inhibitor 17-Allylamino , 17-Demethoxygeldanamycin in Human Ovarian Cancer , 2005 .
[40] A. Saghatelian,et al. Target discovery in small-molecule cell-based screens by in situ proteome reactivity profiling , 2005, Nature Biotechnology.
[41] Paul Workman,et al. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. , 2005, Bioorganic & medicinal chemistry letters.
[42] T. Golub,et al. Integrative genomic analyses identify MITF as a lineage survival oncogene amplified in malignant melanoma , 2005, Nature.
[43] Derek S. Tan,et al. Diversity-oriented synthesis: exploring the intersections between chemistry and biology , 2005, Nature chemical biology.
[44] S. Lakhani,et al. Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies. , 2005, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[45] S. Korsmeyer,et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours , 2005, Nature.
[46] Xavier Barril,et al. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. , 2005, Journal of medicinal chemistry.
[47] Kevan M Shokat,et al. Features of selective kinase inhibitors. , 2005, Chemistry & biology.
[48] Rajiv Sharma,et al. Design and synthesis of protein superfamily-targeted chemical libraries for lead identification and optimization. , 2005, Current medicinal chemistry.
[49] Michael S. Cohen,et al. Structural Bioinformatics-Based Design of Selective, Irreversible Kinase Inhibitors , 2005, Science.
[50] P. Workman. Genomics and the second golden era of cancer drug development. , 2005, Molecular bioSystems.
[51] Andrew M Davis,et al. Components of successful lead generation. , 2005, Current topics in medicinal chemistry.
[52] Alan Ashworth,et al. Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy , 2005, Nature.
[53] C. Hart,et al. Finding the target after screening the phenotype. , 2005, Drug discovery today.
[54] C. Lindsley,et al. The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation. , 2005, Current topics in medicinal chemistry.
[55] Olaf Prien,et al. Target‐Family‐Oriented Focused Libraries for Kinases—Conceptual Design Aspects and Commercial Availability , 2005, Chembiochem : a European journal of chemical biology.
[56] P. Marks,et al. Drug Insight: histone deacetylase inhibitors—development of the new targeted anticancer agent suberoylanilide hydroxamic acid , 2005, Nature Clinical Practice Oncology.
[57] L. Wodicka,et al. A small molecule–kinase interaction map for clinical kinase inhibitors , 2005, Nature Biotechnology.
[58] Holger Wesche,et al. High throughput screening for protein kinase inhibitors. , 2005, Combinatorial chemistry & high throughput screening.
[59] S. Møller,et al. Identification of Akt Pathway Inhibitors Using Redistribution Screening on the FLIPR and the IN Cell 3000 Analyzer , 2005, Journal of biomolecular screening.
[60] Kam Y. J. Zhang,et al. A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design , 2005, Nature Biotechnology.
[61] György Kéri,et al. Cellular targets of gefitinib. , 2005, Cancer research.
[62] P. Johnston,et al. Molecular mechanisms of drug resistance , 2005, The Journal of pathology.
[63] A. Hopkins,et al. Navigating chemical space for biology and medicine , 2004, Nature.
[64] Christopher T. Walsh,et al. Lessons from natural molecules , 2004, Nature.
[65] A. Nassar,et al. Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability. , 2004, Drug discovery today.
[66] Mark J Ratain,et al. Phase II studies of modern drugs directed against new targets: if you are fazed, too, then resist RECIST. , 2004, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[67] J. Warmus,et al. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition , 2004, Nature Structural &Molecular Biology.
[68] J. Bajorath,et al. Docking and scoring in virtual screening for drug discovery: methods and applications , 2004, Nature Reviews Drug Discovery.
[69] Li Xing,et al. Influence of molecular flexibility and polar surface area metrics on oral bioavailability in the rat. , 2004, Journal of medicinal chemistry.
[70] D. Swinney,et al. Biochemical mechanisms of drug action: what does it take for success? , 2004, Nature Reviews Drug Discovery.
[71] P. Workman,et al. 322 Novel isoquinoline-5-sulfonamides as biochemical and cellular inhibitors of PKB/AKt , 2004 .
[72] M. Congreve,et al. Fragment-based lead discovery , 2004, Nature Reviews Drug Discovery.
[73] I. Kola,et al. Can the pharmaceutical industry reduce attrition rates? , 2004, Nature Reviews Drug Discovery.
[74] K. Kinzler,et al. Cancer genes and the pathways they control , 2004, Nature Medicine.
[75] I. Gout,et al. The TSC1-2 tumor suppressor controls insulin–PI3K signaling via regulation of IRS proteins , 2004, The Journal of cell biology.
[76] Ping Chen,et al. Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor , 2004, Science.
[77] J. R. Somoza,et al. Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases. , 2004, Structure.
[78] S. Gabriel,et al. EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy , 2004, Science.
[79] X. Barril,et al. Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. , 2004, Chemistry & biology.
[80] D. Kassel,et al. Applications of high-throughput ADME in drug discovery. , 2004, Current opinion in chemical biology.
[81] Paul A Clemons,et al. Complex phenotypic assays in high-throughput screening. , 2004, Current opinion in chemical biology.
[82] Li Di,et al. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. , 2004, Journal of pharmaceutical sciences.
[83] A. Hopkins,et al. Ligand efficiency: a useful metric for lead selection. , 2004, Drug discovery today.
[84] J. Wendoloski,et al. Identification of compounds with nanomolar binding affinity for checkpoint kinase-1 using knowledge-based virtual screening. , 2004, Journal of medicinal chemistry.
[85] Stuart L Schreiber,et al. Stuart Schreiber: biology from a chemist's perspective. Interview by Joanna Owens. , 2004, Drug discovery today.
[86] L. Johnson,et al. Protein Kinase Inhibitors: Insights into Drug Design from Structure , 2004, Science.
[87] T. Hubbard,et al. A census of human cancer genes , 2004, Nature Reviews Cancer.
[88] D. Lane,et al. Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. , 2004, Molecular cancer therapeutics.
[89] L. Vassilev,et al. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2 , 2004, Science.
[90] L. Meijer,et al. Synthesis and target identification of hymenialdisine analogs. , 2004, Chemistry & biology.
[91] Sebastian Meier-Ewert,et al. A three-hybrid approach to scanning the proteome for targets of small molecule kinase inhibitors. , 2004, Chemistry & biology.
[92] T. Möröy,et al. Identification of potent Ras signaling inhibitors by pathway-selective phenotype-based screening. , 2004, Angewandte Chemie.
[93] M. Machida,et al. Biopharmaceutics Classification by High Throughput Solubility Assay and PAMPA , 2004, Drug development and industrial pharmacy.
[94] C. Sawyers. Opportunities and challenges in the development of kinase inhibitor therapy for cancer. , 2003, Genes & development.
[95] Pamela A. Silver,et al. A chemical genetic screen identifies inhibitors of regulated nuclear export of a Forkhead transcription factor in PTEN-deficient tumor cells. , 2003, Cancer cell.
[96] S. Remiszewski. The discovery of NVP-LAQ824: from concept to clinic. , 2003, Current medicinal chemistry.
[97] G. Müller,et al. Medicinal chemistry of target family-directed masterkeys. , 2003, Drug discovery today.
[98] R. Hargreaves,et al. Clinical biomarkers in drug discovery and development , 2003, Nature Reviews Drug Discovery.
[99] J. Lehár,et al. Systematic discovery of multicomponent therapeutics , 2003, Proceedings of the National Academy of Sciences of the United States of America.
[100] S. Haggarty,et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. , 2003, Chemistry & biology.
[101] A. Ullrich,et al. Mutation of Threonine 766 in the Epidermal Growth Factor Receptor Reveals a Hotspot for Resistance Formation against Selective Tyrosine Kinase Inhibitors* , 2003, The Journal of Biological Chemistry.
[102] P. Cohen,et al. The specificities of protein kinase inhibitors: an update. , 2003, The Biochemical journal.
[103] P. Workman. How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development. , 2003, Current pharmaceutical design.
[104] L. Elmore,et al. Telomerase as a Target for Cancer Immunotherapy , 2003, Cancer biology & therapy.
[105] P. Workman. Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics. , 2003, Molecular cancer therapeutics.
[106] G. Rishton. Nonleadlikeness and leadlikeness in biochemical screening. , 2003, Drug discovery today.
[107] P. Workman. Challenges of PK/PD measurements in modern drug development. , 2002, European journal of cancer.
[108] B. Riedl,et al. Design and discovery of small molecules targeting raf-1 kinase. , 2002, Current pharmaceutical design.
[109] I. Judson. Gastrointestinal stromal tumours (GIST): biology and treatment. , 2002, Annals of oncology : official journal of the European Society for Medical Oncology.
[110] K. Shokat,et al. Novel chemical genetic approaches to the discovery of signal transduction inhibitors. , 2002, Drug discovery today.
[111] I. Weinstein. Addiction to Oncogenes--the Achilles Heal of Cancer , 2002, Science.
[112] Alex Matter,et al. Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug , 2002, Nature Reviews Drug Discovery.
[113] A. Nicholson,et al. Mutations of the BRAF gene in human cancer , 2002, Nature.
[114] Stephen R. Johnson,et al. Molecular properties that influence the oral bioavailability of drug candidates. , 2002, Journal of medicinal chemistry.
[115] P. Cohen. Protein kinases — the major drug targets of the twenty-first century? , 2002, Nature reviews. Drug discovery.
[116] B. Shoichet,et al. A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. , 2002, Journal of medicinal chemistry.
[117] John Mann,et al. Natural products in cancer chemotherapy: past, present and future , 2002, Nature Reviews Cancer.
[118] Tudor I. Oprea,et al. Is There a Difference between Leads and Drugs? A Historical Perspective , 2001, J. Chem. Inf. Comput. Sci..
[119] P. N. Rao,et al. Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification , 2001, Science.
[120] N. Rosen,et al. A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells. , 2001, Chemistry & biology.
[121] D. W. Fry,et al. Site-directed irreversible inhibitors of the erbB family of receptor tyrosine kinases as novel chemotherapeutic agents for cancer. , 2000, Anti-cancer drug design.
[122] D. Hanahan,et al. The Hallmarks of Cancer , 2000, Cell.
[123] A. Jackman,et al. Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors. , 1999, Journal of medicinal chemistry.
[124] P. Marks,et al. Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors , 1999, Nature.
[125] L. Pearl,et al. Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin. , 1999, Journal of medicinal chemistry.
[126] L. Dick,et al. Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. , 1998, Bioorganic & medicinal chemistry letters.
[127] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .
[128] Stuart L. Schreiber,et al. Structure of the FKBP12-Rapamycin Complex Interacting with Binding Domain of Human FRAP , 1996, Science.
[129] S. Minucci,et al. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer , 2006, Nature Reviews Cancer.
[130] Peter G Schultz,et al. A genome-wide overexpression screen in yeast for small-molecule target identification. , 2005, Chemistry & biology.
[131] M. Hutzler,et al. Predicting drug-drug interactions in drug discovery: where are we now and where are we going? , 2005, Current opinion in drug discovery & development.
[132] P. Workman. Drugging the cancer kinome: progress and challenges in developing personalized molecular cancer therapeutics. , 2005, Cold Spring Harbor symposia on quantitative biology.
[133] Ian A. Watson,et al. Characteristic physical properties and structural fragments of marketed oral drugs. , 2004, Journal of medicinal chemistry.