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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy, Dalia; Li, Fengling; Oudhoff, Menno J; Tatlock, John H; Dong, Aiping; Zeng, Hong; Wu, Hong; Freeman, Spencer A; Schapira, Matthieu; Senisterra, Guillermo A; Kuznetsova, Ekaterina; Marcellus, Richard; Allali-Hassani, Abdellah; Kennedy, Steven; Lambert, Jean-Philippe; Couzens, Amber L; Aman, Ahmed; Gingras, Anne-Claude; Al-Awar, Rima; Fish, Paul V; Gerstenberger, Brian S; Roberts, Lee; Benn, Caroline L; Grimley, Rachel L; Braam, Mitchell J S; Rossi, Fabio M V; Sudol, Marius; Brown, Peter J; Bunnage, Mark E; Owen, Dafydd R; Zaph, Colby; Vedadi, Masoud; Arrowsmith, Cheryl H.
Afiliación
  • Barsyte-Lovejoy D; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7; carrow@uhnres.utoronto.ca m.vedadi@utoronto.ca d.barsyte@utoronto.ca.
  • Li F; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Oudhoff MJ; Biomedical Research Centre, University of British Columbia, Vancouver, BC, Canada V6T1Z3;
  • Tatlock JH; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, San Diego, CA 92121;
  • Dong A; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Zeng H; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Wu H; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Freeman SA; Department of Microbiology and Immunology, University of British Columbia, Vancouver, BC, Canada V6T1Z3;
  • Schapira M; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7; Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada M5S 1A8;
  • Senisterra GA; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Kuznetsova E; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Marcellus R; Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, ON, Canada M5G 0A3;
  • Allali-Hassani A; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Kennedy S; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Lambert JP; Centre for Systems Biology, Lunenfeld-Tanenbaum Research Institute, Toronto, ON, Canada M5G 1X5;
  • Couzens AL; Centre for Systems Biology, Lunenfeld-Tanenbaum Research Institute, Toronto, ON, Canada M5G 1X5;
  • Aman A; Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, ON, Canada M5G 0A3;
  • Gingras AC; Centre for Systems Biology, Lunenfeld-Tanenbaum Research Institute, Toronto, ON, Canada M5G 1X5; Department of Molecular Genetics, University of Toronto, Toronto, ON, Canada M5S 1A8;
  • Al-Awar R; Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada M5S 1A8; Drug Discovery Program, Ontario Institute for Cancer Research, Toronto, ON, Canada M5G 0A3;
  • Fish PV; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom;
  • Gerstenberger BS; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Groton, CT 06340;
  • Roberts L; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Cambridge, MA 02139;
  • Benn CL; Neusentis Research Unit, Pfizer Worldwide Research and Development, Cambridge CB21 6GS, United Kingdom;
  • Grimley RL; Neusentis Research Unit, Pfizer Worldwide Research and Development, Cambridge CB21 6GS, United Kingdom;
  • Braam MJ; Biomedical Research Centre, University of British Columbia, Vancouver, BC, Canada V6T1Z3;
  • Rossi FM; Biomedical Research Centre, University of British Columbia, Vancouver, BC, Canada V6T1Z3; Department of Medical Genetics, University of British Columbia, Vancouver, BC, Canada V6T1Z3;
  • Sudol M; Weis Center for Research, Geisinger Clinic, Danville, PA 17821;
  • Brown PJ; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7;
  • Bunnage ME; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Cambridge, MA 02139;
  • Owen DR; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Cambridge, MA 02139;
  • Zaph C; Biomedical Research Centre, University of British Columbia, Vancouver, BC, Canada V6T1Z3; Department of Pathology and Laboratory Medicine, University of British Columbia, Vancouver, BC, Canada V6T1Z3; and.
  • Vedadi M; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7; Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada M5S 1A8; carrow@uhnres.utoronto.ca m.vedadi@utoronto.ca d.barsyte@utoronto.ca.
  • Arrowsmith CH; Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada M5G 1L7; Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, ON, Canada M5G 1L7 carrow@uhnres.utoronto.ca m.vedadi@utoronto.ca d.barsyte@utoronto.ca.
Proc Natl Acad Sci U S A ; 111(35): 12853-8, 2014 Sep 02.
Article en En | MEDLINE | ID: mdl-25136132
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirrolidinas / Sulfonamidas / Transducción de Señal / N-Metiltransferasa de Histona-Lisina / Tetrahidroisoquinolinas / Epigénesis Genética / Inhibidores Enzimáticos Límite: Humans Idioma: En Revista: Proc Natl Acad Sci U S A Año: 2014 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirrolidinas / Sulfonamidas / Transducción de Señal / N-Metiltransferasa de Histona-Lisina / Tetrahidroisoquinolinas / Epigénesis Genética / Inhibidores Enzimáticos Límite: Humans Idioma: En Revista: Proc Natl Acad Sci U S A Año: 2014 Tipo del documento: Article