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المؤلفون: Van Aller GS; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA., Graves AP; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Elkins PA; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Bonnette WG; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., McDevitt PJ; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Zappacosta F; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Annan RS; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Dean TW; Department of Platform Technology and Science, GlaxoSmithKline, Collegeville, PA 19426, USA., Su DS; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA., Carpenter CL; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA., Mohammad HP; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA., Kruger RG; Cancer Epigenetics Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA. Electronic address: ryan.g.kruger@gsk.com.

المصدر: Structure (London, England : 1993) [Structure] 2016 May 03; Vol. 24 (5), pp. 774-781. Date of Electronic Publication: 2016 Apr 07.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Cell Press Country of Publication: United States NLM ID: 101087697 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1878-4186 (Electronic) Linking ISSN: 09692126 NLM ISO Abbreviation: Structure Subsets: MEDLINE

مواضيع طبية MeSH: Molecular Docking Simulation*, Enzyme Inhibitors/*pharmacology , Histone-Lysine N-Methyltransferase/*chemistry, Binding Sites ; Enzyme Inhibitors/chemistry ; Histone-Lysine N-Methyltransferase/antagonists & inhibitors ; Histone-Lysine N-Methyltransferase/genetics ; Histone-Lysine N-Methyltransferase/metabolism ; Humans ; MAP Kinase Kinase Kinase 2/metabolism ; Mutation ; Protein Binding ; S-Adenosylmethionine/pharmacology

المؤلفون: Mohammad HP; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Smitheman KN; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Kamat CD; Oncology Department, Johns Hopkins University, Baltimore, MD 21231, USA., Soong D; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Federowicz KE; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Van Aller GS; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Schneck JL; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., Carson JD; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., Liu Y; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Butticello M; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Bonnette WG; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., Gorman SA; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Degenhardt Y; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Bai Y; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., McCabe MT; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Pappalardi MB; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Kasparec J; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Tian X; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., McNulty KC; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Rouse M; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., McDevitt P; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., Ho T; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., Crouthamel M; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Hart TK; Safety Assessment Department, GlaxoSmithKline, Upper Merion, PA 19406, USA., Concha NO; Platform Technology and Sciences, GlaxoSmithKline, Collegeville, PA 19426, USA., McHugh CF; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Miller WH; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Dhanak D; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Tummino PJ; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Carpenter CL; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Johnson NW; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA., Hann CL; Oncology Department, Johns Hopkins University, Baltimore, MD 21231, USA., Kruger RG; Cancer Epigenetics Department, GlaxoSmithKline, Collegeville, PA 19426, USA. Electronic address: ryan.g.kruger@gsk.com.

المصدر: Cancer cell [Cancer Cell] 2015 Jul 13; Vol. 28 (1), pp. 57-69.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Cell Press Country of Publication: United States NLM ID: 101130617 Publication Model: Print Cited Medium: Internet ISSN: 1878-3686 (Electronic) Linking ISSN: 15356108 NLM ISO Abbreviation: Cancer Cell Subsets: MEDLINE

مواضيع طبية MeSH: Antineoplastic Agents/*administration & dosage , Benzoates/*administration & dosage , Cyclopropanes/*administration & dosage , DNA Methylation/*drug effects , Enzyme Inhibitors/*administration & dosage , Histone Demethylases/*antagonists & inhibitors , Lung Neoplasms/*drug therapy , Small Cell Lung Carcinoma/*drug therapy, Administration, Oral ; Animals ; Antineoplastic Agents/pharmacology ; Benzoates/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cyclopropanes/pharmacology ; Enzyme Inhibitors/pharmacology ; Epigenesis, Genetic/drug effects ; Gene Expression Regulation, Neoplastic/drug effects ; Histone Demethylases/genetics ; Humans ; Lung Neoplasms/genetics ; Lung Neoplasms/pathology ; Mice ; Molecular Sequence Data ; Small Cell Lung Carcinoma/genetics ; Small Cell Lung Carcinoma/pathology ; Xenograft Model Antitumor Assays

المؤلفون: Mazur PK; 1] Department of Pediatrics, Stanford University School of Medicine, California 94305, USA [2] Department of Genetics, Stanford University School of Medicine, California 94305, USA [3]., Reynoird N; 1] Department of Biology, Stanford University, California 94305, USA [2]., Khatri P; Institute for Immunity, Transplantation and Infection, and Department of Medicine, Stanford University School of Medicine, California 94305, USA., Jansen PW; Department of Molecular Cancer Research and Department of Medical Oncology, University Medical Center Utrecht, 3508 AB Utrecht, The Netherlands., Wilkinson AW; Department of Biology, Stanford University, California 94305, USA., Liu S; Epigenetics Program and Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA., Barbash O; Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA., Van Aller GS; Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA., Huddleston M; Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA., Dhanak D; 1] Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA [2] Janssen Research and Development, 1400 McKean Road, Spring House, Pennsylvania 19477, USA (D.D.); Department of Molecular Biology, Faculty of Science, Radboud Institute for Molecular Life Sciences (RIMLS), Radboud University, 6525GA Nijmegen, The Netherlands (M.V.)., Tummino PJ; Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA., Kruger RG; Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, Collegeville, Pennsylvania 19426 USA., Garcia BA; Epigenetics Program and Department of Biochemistry and Biophysics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA., Butte AJ; 1] Department of Pediatrics, Stanford University School of Medicine, California 94305, USA [2] Department of Genetics, Stanford University School of Medicine, California 94305, USA., Vermeulen M; 1] Department of Molecular Cancer Research and Department of Medical Oncology, University Medical Center Utrecht, 3508 AB Utrecht, The Netherlands [2] Janssen Research and Development, 1400 McKean Road, Spring House, Pennsylvania 19477, USA (D.D.); Department of Molecular Biology, Faculty of Science, Radboud Institute for Molecular Life Sciences (RIMLS), Radboud University, 6525GA Nijmegen, The Netherlands (M.V.)., Sage J; 1] Department of Pediatrics, Stanford University School of Medicine, California 94305, USA [2] Department of Genetics, Stanford University School of Medicine, California 94305, USA [3]., Gozani O; 1] Department of Biology, Stanford University, California 94305, USA [2].

المصدر: Nature [Nature] 2014 Jun 12; Vol. 510 (7504), pp. 283-7. Date of Electronic Publication: 2014 May 21.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 0410462 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1476-4687 (Electronic) Linking ISSN: 00280836 NLM ISO Abbreviation: Nature Subsets: MEDLINE

مواضيع طبية MeSH: Cell Transformation, Neoplastic/*metabolism , Histone-Lysine N-Methyltransferase/*metabolism , Lysine/*metabolism , MAP Kinase Kinase Kinase 2/*metabolism , MAP Kinase Kinase Kinases/*metabolism , Oncogene Protein p21(ras)/*metabolism, Adenocarcinoma/enzymology ; Adenocarcinoma/genetics ; Adenocarcinoma/metabolism ; Adenocarcinoma/pathology ; Adenocarcinoma of Lung ; Animals ; Cell Line, Tumor ; Cell Transformation, Neoplastic/genetics ; Cell Transformation, Neoplastic/pathology ; Disease Models, Animal ; Humans ; Lung Neoplasms/enzymology ; Lung Neoplasms/genetics ; Lung Neoplasms/metabolism ; Lung Neoplasms/pathology ; MAP Kinase Kinase Kinase 2/chemistry ; MAP Kinase Kinase Kinases/chemistry ; Methylation ; Mice ; Mitogen-Activated Protein Kinases/metabolism ; Oncogene Protein p21(ras)/genetics ; Pancreatic Neoplasms/enzymology ; Pancreatic Neoplasms/genetics ; Pancreatic Neoplasms/metabolism ; Pancreatic Neoplasms/pathology ; Protein Phosphatase 2/antagonists & inhibitors ; Protein Phosphatase 2/metabolism ; Proto-Oncogene Proteins A-raf/metabolism ; Signal Transduction

المؤلفون: Van Aller GS; Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D and ‡Platform Technology and Sciences, GlaxoSmithKline, 1250 S. Collegeville Road, Collegeville, Pennsylvania 19426, United States., Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG

المصدر: ACS chemical biology [ACS Chem Biol] 2014 Mar 21; Vol. 9 (3), pp. 622-9. Date of Electronic Publication: 2013 Dec 31.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101282906 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1554-8937 (Electronic) Linking ISSN: 15548929 NLM ISO Abbreviation: ACS Chem Biol Subsets: MEDLINE

مواضيع طبية MeSH: Enzyme Inhibitors/*pharmacology , Indoles/*pharmacology , Polycomb Repressive Complex 2/*antagonists & inhibitors , Pyridones/*pharmacology, Allosteric Regulation ; Allosteric Site ; Binding, Competitive ; Dose-Response Relationship, Drug ; Enhancer of Zeste Homolog 2 Protein ; Enzyme Inhibitors/chemistry ; HeLa Cells ; Humans ; Indoles/chemistry ; Methylation ; Nucleosomes/drug effects ; Nucleosomes/enzymology ; Point Mutation ; Polycomb Repressive Complex 2/genetics ; Protein Binding ; Pyridones/chemistry ; Structure-Activity Relationship ; Substrate Specificity ; Time Factors

المؤلفون: Béguelin W; Division of Hematology/Oncology, Department of Medicine, Weill Cornell Medical College, New York, NY 10021, USA., Popovic R, Teater M, Jiang Y, Bunting KL, Rosen M, Shen H, Yang SN, Wang L, Ezponda T, Martinez-Garcia E, Zhang H, Zheng Y, Verma SK, McCabe MT, Ott HM, Van Aller GS, Kruger RG, Liu Y, McHugh CF, Scott DW, Chung YR, Kelleher N, Shaknovich R, Creasy CL, Gascoyne RD, Wong KK, Cerchietti L, Levine RL, Abdel-Wahab O, Licht JD, Elemento O, Melnick AM

المصدر: Cancer cell [Cancer Cell] 2013 May 13; Vol. 23 (5), pp. 677-92.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Cell Press Country of Publication: United States NLM ID: 101130617 Publication Model: Print Cited Medium: Internet ISSN: 1878-3686 (Electronic) Linking ISSN: 15356108 NLM ISO Abbreviation: Cancer Cell Subsets: MEDLINE

مواضيع طبية MeSH: Mutation*, B-Lymphocytes/*metabolism , Cell Transformation, Neoplastic/*genetics , Germinal Center/*metabolism , Polycomb Repressive Complex 2/*physiology, Animals ; Cell Differentiation ; Cell Proliferation ; Enhancer of Zeste Homolog 2 Protein ; Gene Deletion ; Gene Expression Regulation, Neoplastic ; Germinal Center/drug effects ; Histones/metabolism ; Methylation ; Mice ; Polycomb Repressive Complex 2/genetics ; Polycomb Repressive Complex 2/metabolism ; Promoter Regions, Genetic ; Proto-Oncogene Proteins c-bcl-2/metabolism ; Proto-Oncogene Proteins c-bcl-2/physiology

المؤلفون: McCabe MT; Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road, Collegeville, Pennsylvania 19426, USA., Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL

المصدر: Nature [Nature] 2012 Dec 06; Vol. 492 (7427), pp. 108-12. Date of Electronic Publication: 2012 Oct 10.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 0410462 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1476-4687 (Electronic) Linking ISSN: 00280836 NLM ISO Abbreviation: Nature Subsets: MEDLINE

مواضيع طبية MeSH: Indoles/*pharmacology , Indoles/*therapeutic use , Lymphoma, Follicular/*drug therapy , Lymphoma, Large B-Cell, Diffuse/*drug therapy , Mutation/*genetics , Polycomb Repressive Complex 2/*antagonists & inhibitors , Pyridones/*pharmacology , Pyridones/*therapeutic use, Animals ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Enhancer of Zeste Homolog 2 Protein ; Gene Expression Regulation, Neoplastic/drug effects ; Gene Silencing/drug effects ; Histone Methyltransferases ; Histone-Lysine N-Methyltransferase/antagonists & inhibitors ; Histone-Lysine N-Methyltransferase/genetics ; Histone-Lysine N-Methyltransferase/metabolism ; Histones/chemistry ; Histones/metabolism ; Humans ; Lymphoma, Follicular/enzymology ; Lymphoma, Follicular/genetics ; Lymphoma, Follicular/pathology ; Lymphoma, Large B-Cell, Diffuse/enzymology ; Lymphoma, Large B-Cell, Diffuse/genetics ; Lymphoma, Large B-Cell, Diffuse/pathology ; Methylation/drug effects ; Mice ; Neoplasm Transplantation ; Polycomb Repressive Complex 2/genetics ; Polycomb Repressive Complex 2/metabolism ; Repressor Proteins/chemistry ; Repressor Proteins/metabolism ; Transcriptional Activation/drug effects ; Transplantation, Heterologous