Cheryl H Arrowsmith

Cheryl H Arrowsmith

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Cheryl H Arrowsmith

Publications by authors named "Cheryl H Arrowsmith"

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Targeting non-bromodomain chromatin readers.

Nat Struct Mol Biol 2019 Oct 3;26(10):863-869. Epub 2019 Oct 3.

Structural Genomics Consortium, University of Toronto, Toronto, Canada.

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http://dx.doi.org/10.1038/s41594-019-0290-2DOI Listing
October 2019

Identification and characterization of the first fragment hits for SETDB1 Tudor domain.

Bioorg Med Chem 2019 Sep 12;27(17):3866-3878. Epub 2019 Jul 12.

Structural Genomics Consortium, University of Toronto, Toronto, Canada; Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, Toronto, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2019.07.020DOI Listing
September 2019

Addendum: A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Nat Chem Biol 2019 Aug;15(8):846

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNCEshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.

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http://dx.doi.org/10.1038/s41589-019-0242-5DOI Listing
August 2019

Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation.

Cancer Cell 2019 Aug;36(2):194-209.e9

Institute of Molecular and Cell Biology, Agency for Science, Technology and Research (A(∗)STAR), Singapore 138673, Singapore; Department of Biochemistry, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 119077, Singapore; Department of Oncological Sciences and Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA; Department of Pharmacological Sciences and Mount Sinai Center for Therapeutics Discovery, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2019.07.003DOI Listing
August 2019

Structural basis of HMCES interactions with abasic DNA and multivalent substrate recognition.

Nat Struct Mol Biol 2019 Jul 24;26(7):607-612. Epub 2019 Jun 24.

Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada.

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http://dx.doi.org/10.1038/s41594-019-0246-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6609482PMC
July 2019

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).

J Med Chem 2019 Jul 24. Epub 2019 Jul 24.

Mount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute , Icahn School of Medicine at Mount Sinai , New York , New York 10029 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00522DOI Listing
July 2019

Target 2035: probing the human proteome.

Drug Discov Today 2019 Jul 3. Epub 2019 Jul 3.

Structural Genomics Consortium, University of Toronto, Toronto, Ontario, M5G 1L7, Canada.

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http://dx.doi.org/10.1016/j.drudis.2019.06.020DOI Listing
July 2019

AKT drives SOX2 overexpression and cancer cell stemness in esophageal cancer by protecting SOX2 from UBR5-mediated degradation.

Oncogene 2019 Jun 20;38(26):5250-5264. Epub 2019 Mar 20.

Shanghai Key Laboratory of Regulatory Biology, Fengxian District Central Hospital-ECNU Joint Center of Translational Medicine, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.

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http://dx.doi.org/10.1038/s41388-019-0790-xDOI Listing
June 2019

Discovery of selective activators of PRC2 mutant EED-I363M.

Sci Rep 2019 Apr 25;9(1):6524. Epub 2019 Apr 25.

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, 27599, USA.

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http://dx.doi.org/10.1038/s41598-019-43005-zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6484020PMC
April 2019

Arginine methylation of FOXP3 is crucial for the suppressive function of regulatory T cells.

J Autoimmun 2019 Feb 11;97:10-21. Epub 2018 Oct 11.

Tumor Immunotherapy Program, Campbell Family Institute for Breast Cancer Research, Campbell Family Cancer Research Institute, Princess Margaret Cancer Centre, University Health Network, Toronto, Ontario, M5G 2M9, Canada; Department of Immunology, University of Toronto, Toronto, Ontario, M5S 1A8, Canada. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S08968411183028
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http://dx.doi.org/10.1016/j.jaut.2018.09.011DOI Listing
February 2019

Characterization of inv(3) cell line OCI-AML-20 with stroma-dependent CD34 expression.

Exp Hematol 2019 01 22;69:27-36. Epub 2018 Oct 22.

Princess Margaret Cancer Centre, Toronto, Ontario, Canada; Department of Medical Biophysics, University of Toronto, Ontario, Canada. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0301472X183086
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http://dx.doi.org/10.1016/j.exphem.2018.10.006DOI Listing
January 2019

Guiding COMPASS: Dpy-30 Positions SET1/MLL Epigenetic Signaling.

Structure 2018 12;26(12):1567-1570

Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada; Princess Margaret Cancer Centre and Department of Medical Biophysics, University of Toronto, Toronto, ON, Canada. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S09692126183042
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http://dx.doi.org/10.1016/j.str.2018.11.010DOI Listing
December 2018

Functional diversification of the NleG effector family in enterohemorrhagic .

Proc Natl Acad Sci U S A 2018 10 14;115(40):10004-10009. Epub 2018 Sep 14.

Department of Chemical Engineering and Applied Chemistry, University of Toronto, Toronto, ON M5S 3E5, Canada;

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http://dx.doi.org/10.1073/pnas.1718350115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6176568PMC
October 2018

MYC Interacts with the G9a Histone Methyltransferase to Drive Transcriptional Repression and Tumorigenesis.

Cancer Cell 2018 10;34(4):579-595.e8

Princess Margaret Cancer Centre, Toronto, ON M5G1L7, Canada; Department of Medical Biophysics, University of Toronto, Toronto, ON M5G1L7, Canada. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S15356108183041
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http://dx.doi.org/10.1016/j.ccell.2018.09.001DOI Listing
October 2018

Identification and Structure-Activity Relationship of HDAC6 Zinc-Finger Ubiquitin Binding Domain Inhibitors.

J Med Chem 2018 05 9;61(10):4517-4527. Epub 2018 May 9.

Structural Genomics Consortium , University of Toronto , MaRS South Tower, Suite 700, 101 College Street , Toronto , Ontario M5G 1L7 , Canada.

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http://dx.doi.org/10.1021/acs.jmedchem.8b00258DOI Listing
May 2018

DOT1L inhibition attenuates graft-versus-host disease by allogeneic T cells in adoptive immunotherapy models.

Nat Commun 2018 05 15;9(1):1915. Epub 2018 May 15.

Tumor Immunotherapy Program, Campbell Family Institute for Breast Cancer Research, Campbell Family Cancer Research Institute, Princess Margaret Cancer Centre, University Health Network, Toronto, ON, M5G 2M9, Canada.

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http://dx.doi.org/10.1038/s41467-018-04262-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5954061PMC
May 2018

Discovery of Ubiquitin Deamidases in the Pathogenic Arsenal of Legionella pneumophila.

Cell Rep 2018 Apr;23(2):568-583

Department of Chemical Engineering and Applied Chemistry, University of Toronto, Toronto, ON, Canada; Department of Microbiology, Immunology and Infectious Diseases, University of Calgary, Calgary, AB, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.celrep.2018.03.060DOI Listing
April 2018

Small Molecule Antagonists of the Interaction between the Histone Deacetylase 6 Zinc-Finger Domain and Ubiquitin.

J Med Chem 2017 11 27;60(21):9090-9096. Epub 2017 Oct 27.

Structural Genomics Consortium, University of Toronto , MaRS South Tower, Suite 700, 101 College Street, Toronto, Ontario M5G 1L7, Canada.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00933DOI Listing
November 2017

WD40 repeat domain proteins: a novel target class?

Nat Rev Drug Discov 2017 Nov 13;16(11):773-786. Epub 2017 Oct 13.

Structural Genomics Consortium, University of Toronto, Toronto, 101 College St, MaRS South Tower, Suite 700, Ontario M5G 1L7, Canada.

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http://www.nature.com/doifinder/10.1038/nrd.2017.179
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http://dx.doi.org/10.1038/nrd.2017.179DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5975957PMC
November 2017

A p53 Super-tumor Suppressor Reveals a Tumor Suppressive p53-Ptpn14-Yap Axis in Pancreatic Cancer.

Cancer Cell 2017 10;32(4):460-473.e6

Department of Radiation Oncology, Stanford University School of Medicine, Stanford, CA 94305, USA; Stanford Cancer Institute, Stanford University School of Medicine, Stanford, CA 94305, USA; Department of Genetics, Stanford University School of Medicine, Stanford, CA 94305, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2017.09.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5659188PMC
October 2017

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.

Bioorg Med Chem 2017 08 19;25(16):4414-4423. Epub 2017 Jun 19.

Department of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States; Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2017.06.021DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5562403PMC
August 2017

ASCL1 Reorganizes Chromatin to Direct Neuronal Fate and Suppress Tumorigenicity of Glioblastoma Stem Cells.

Cell Stem Cell 2017 08 14;21(2):209-224.e7. Epub 2017 Jul 14.

Developmental and Stem Cell Biology Program and Arthur and Sonia Labatt Brain Tumor Research Centre, The Hospital for Sick Children, Toronto, ON M5G 0A4, Canada; Department of Molecular Genetics, University of Toronto, Toronto, ON M5S 1A8, Canada; Department of Laboratory Medicine and Pathobiology, University of Toronto, Toronto, ON M5S 1A8, Canada; Division of Neurosurgery, University of Toronto, Toronto, ON M5S 1A8, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.stem.2017.06.004DOI Listing
August 2017

Early-life antibiotic treatment enhances the pathogenicity of CD4 T cells during intestinal inflammation.

J Leukoc Biol 2017 04 29;101(4):893-900. Epub 2016 Dec 29.

The Biomedical Research Centre, University of British Columbia, Vancouver, British Columbia, Canada;

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http://dx.doi.org/10.1189/jlb.3MA0716-334RRDOI Listing
April 2017

Targeting human SET1/MLL family of proteins.

Protein Sci 2017 04 6;26(4):662-676. Epub 2017 Mar 6.

Structural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7.

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http://dx.doi.org/10.1002/pro.3129DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5368065PMC
April 2017

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

J Med Chem 2017 03 14;60(5):1876-1891. Epub 2017 Feb 14.

Department of Pharmacological Sciences and Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01645DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5352984PMC
March 2017

Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.

ACS Comb Sci 2017 03 22;19(3):161-172. Epub 2017 Feb 22.

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill , Chapel Hill, North Carolina 27599, United States.

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http://dx.doi.org/10.1021/acscombsci.6b00174DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5376495PMC
March 2017

The SMX DNA Repair Tri-nuclease.

Mol Cell 2017 Mar;65(5):848-860.e11

The Francis Crick Institute, 1 Midland Road, London NW1 1AT, UK. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S10972765173008
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http://dx.doi.org/10.1016/j.molcel.2017.01.031DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5344696PMC
March 2017

A Suite of Biochemical Assays for Screening RNA Methyltransferase BCDIN3D.

SLAS Discov 2017 01 27;22(1):32-39. Epub 2016 Sep 27.

1 Structural Genomics Consortium, University of Toronto, Toronto, ON, Canada.

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http://dx.doi.org/10.1177/1087057116666276DOI Listing
January 2017

Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma.

Cancer Cell 2017 01;31(1):50-63

Cell and Molecular Biology Section, Pediatric Oncology Branch, Center for Cancer Research, National Cancer Institute, CRC, 1-3940, 10 Center Drive MSC-1105, Bethesda, MD 20892, USA. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2016.12.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5233415PMC
January 2017

Integrated (epi)-Genomic Analyses Identify Subgroup-Specific Therapeutic Targets in CNS Rhabdoid Tumors.

Authors:
Jonathon Torchia Brian Golbourn Shengrui Feng King Ching Ho Patrick Sin-Chan Alexandre Vasiljevic Joseph D Norman Paul Guilhamon Livia Garzia Natalia R Agamez Mei Lu Tiffany S Chan Daniel Picard Pasqualino de Antonellis Dong-Anh Khuong-Quang Aline C Planello Constanze Zeller Dalia Barsyte-Lovejoy Lucie Lafay-Cousin Louis Letourneau Mathieu Bourgey Man Yu Deena M A Gendoo Misko Dzamba Mark Barszczyk Tiago Medina Alexandra N Riemenschneider A Sorana Morrissy Young-Shin Ra Vijay Ramaswamy Marc Remke Christopher P Dunham Stephen Yip Ho-Keung Ng Jian-Qiang Lu Vivek Mehta Steffen Albrecht Jose Pimentel Jennifer A Chan Gino R Somers Claudia C Faria Lucia Roque Maryam Fouladi Lindsey M Hoffman Andrew S Moore Yin Wang Seung Ah Choi Jordan R Hansford Daniel Catchpoole Diane K Birks Nicholas K Foreman Doug Strother Almos Klekner Laszló Bognár Miklós Garami Péter Hauser Tibor Hortobágyi Beverly Wilson Juliette Hukin Anne-Sophie Carret Timothy E Van Meter Eugene I Hwang Amar Gajjar Shih-Hwa Chiou Hideo Nakamura Helen Toledano Iris Fried Daniel Fults Takafumi Wataya Chris Fryer David D Eisenstat Katrin Scheinemann Adam J Fleming Donna L Johnston Jean Michaud Shayna Zelcer Robert Hammond Samina Afzal David A Ramsay Nongnuch Sirachainan Suradej Hongeng Noppadol Larbcharoensub Richard G Grundy Rishi R Lulla Jason R Fangusaro Harriet Druker Ute Bartels Ronald Grant David Malkin C Jane McGlade Theodore Nicolaides Tarik Tihan Joanna Phillips Jacek Majewski Alexandre Montpetit Guillaume Bourque Gary D Bader Alyssa T Reddy G Yancey Gillespie Monika Warmuth-Metz Stefan Rutkowski Uri Tabori Mathieu Lupien Michael Brudno Ulrich Schüller Torsten Pietsch Alexander R Judkins Cynthia E Hawkins Eric Bouffet Seung-Ki Kim Peter B Dirks Michael D Taylor Anat Erdreich-Epstein Cheryl H Arrowsmith Daniel D De Carvalho James T Rutka Nada Jabado Annie Huang

Cancer Cell 2016 Dec;30(6):891-908

Department of Laboratory Medicine and Pathobiology, University of Toronto, Toronto, ON M5G0A4, Canada; Department of Paediatrics, University of Toronto, Toronto, ON M5G0A4, Canada; Division of Hematology/Oncology, Hospital for Sick Children, Toronto, ON M5G1X8, Canada; Arthur and Sonia Labatt Brain Tumour Research Centre, Hospital for Sick Children, Toronto, ON M5G1X8, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.ccell.2016.11.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5500911PMC
December 2016

Solution NMR structure of the HLTF HIRAN domain: a conserved module in SWI2/SNF2 DNA damage tolerance proteins.

J Biomol NMR 2016 11 22;66(3):209-219. Epub 2016 Oct 22.

Department of Molecular Biology and Biophysics, University of Connecticut Health, Farmington, CT, 06030, USA.

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http://dx.doi.org/10.1007/s10858-016-0070-9DOI Listing
November 2016

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

J Med Chem 2016 11 2;59(21):9881-9889. Epub 2016 Nov 2.

Department of Pharmacological Sciences and Department of Oncological Sciences, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01244DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5148670PMC
November 2016

Methyltransferase inhibitors for modulation of the epigenome and beyond.

Curr Opin Chem Biol 2016 08 16;33:81-7. Epub 2016 Jun 16.

Structural Genomics Consortium, University of Toronto, 101 College St., Toronto, ON M5G 1L7, Canada; Department of Medical Biophysics, University of Toronto, 101 College St., Toronto, ON M5G 1L7, Canada; Princess Margaret Cancer Centre, 101 College St., Toronto, ON M5G 1L7, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.cbpa.2016.05.030DOI Listing
August 2016

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

J Med Chem 2016 08 11;59(16):7617-33. Epub 2016 Aug 11.

Departments of Pharmacological Sciences and Oncological Sciences, Icahn School of Medicine at Mount Sinai , One Gustave L. Levy Place, Room 16-20B, Box 1677, New York, New York 10029, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b00855DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5003625PMC
August 2016

PR Domain-containing Protein 7 (PRDM7) Is a Histone 3 Lysine 4 Trimethyltransferase.

J Biol Chem 2016 Jun 29;291(26):13509-19. Epub 2016 Apr 29.

From the Structural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, the Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario M5S 1A8, Canada

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http://dx.doi.org/10.1074/jbc.M116.721472DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4919437PMC
June 2016

An Integrative Proteomic Approach Identifies Novel Cellular SMYD2 Substrates.

J Proteome Res 2016 06 10;15(6):2052-9. Epub 2016 May 10.

Structural Genomics Consortium, University of Toronto , 101 College Street, MaRS Centre, South Tower, Toronto, Ontario M5G 1L7, Canada.

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http://dx.doi.org/10.1021/acs.jproteome.6b00220DOI Listing
June 2016

Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreatic cancer.

Genes Dev 2016 Apr 17;30(7):772-85. Epub 2016 Mar 17.

Department of Pediatrics, Stanford University School of Medicine, Stanford, California 94305, USA; Department of Genetics, Stanford University School of Medicine, Stanford, California 94305, USA;

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http://dx.doi.org/10.1101/gad.275529.115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4826394PMC
April 2016

SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling.

Dev Cell 2016 Apr;37(1):47-57

The Biomedical Research Centre, University of British Columbia, Vancouver, BC V6T 1Z3, Canada; Department of Pathology and Laboratory Medicine, University of British Columbia, Vancouver, BC V6T 1Z3, Canada; Infection and Immunity Program, Department of Biochemistry and Molecular Biology, Monash Biomedicine Discovery Institute, Monash University, Clayton, VIC 3800, Australia. Electronic address:

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http://dx.doi.org/10.1016/j.devcel.2016.03.002DOI Listing
April 2016

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

ACS Chem Biol 2016 Mar 8;11(3):772-781. Epub 2015 Dec 8.

Departments of Structural and Chemical Biology, Oncological Sciences, and Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.

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http://dx.doi.org/10.1021/acschembio.5b00839DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4798913PMC
March 2016

A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5.

J Biomol Screen 2016 Mar 23;21(3):290-7. Epub 2015 Dec 23.

Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada

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http://dx.doi.org/10.1177/1087057115623264DOI Listing
March 2016

A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1.

Nat Chem Biol 2016 Mar 25;12(3):180-7. Epub 2016 Jan 25.

Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.

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http://dx.doi.org/10.1038/nchembio.2007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4755828PMC
March 2016

WDR5 Supports an N-Myc Transcriptional Complex That Drives a Protumorigenic Gene Expression Signature in Neuroblastoma.

Cancer Res 2015 Dec 15;75(23):5143-54. Epub 2015 Oct 15.

Children's Cancer Institute Australia, Randwick, Sydney, New South Wales, Australia. School of Women's and Children's Health, Faculty of Medicine, University of New South Wales, Randwick, Sydney, New South Wales, Australia.

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http://dx.doi.org/10.1158/0008-5472.CAN-15-0423DOI Listing
December 2015

MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin.

Cancer Cell 2015 Dec 25;28(6):715-729. Epub 2015 Nov 25.

Developmental and Stem Cell Biology Program and Arthur and Sonia Labatt Brain Tumour Research Centre, The Hospital for Sick Children, Toronto, ON M5G 0A4, Canada; Department of Molecular Genetics, University of Toronto, Toronto, ON M5S 1A8, Canada; Laboratory Medicine and Pathobiology, University of Toronto, Toronto, ON M5S 1A8, Canada; Division of Neurosurgery, University of Toronto, Toronto, ON M5S 1A8, Canada. Electronic address:

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http://www.cell.com/cancer-cell/pdf/S1535-6108(15)00382-7.pd
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http://linkinghub.elsevier.com/retrieve/pii/S153561081500382
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http://dx.doi.org/10.1016/j.ccell.2015.10.005DOI Listing
December 2015

Tackling reproducibility in academic preclinical drug discovery.

Nat Rev Drug Discov 2015 11 21;14(11):733-4. Epub 2015 Sep 21.

Johns Hopkins Drug Discovery, Johns Hopkins School of Medicine, Rangos Suite 277, 855 North Wolfe Street, Baltimore, Maryland 21205, USA.

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http://dx.doi.org/10.1038/nrd4737DOI Listing
November 2015

Kinetic characterization of human histone H3 lysine 36 methyltransferases, ASH1L and SETD2.

Biochim Biophys Acta 2015 Sep 19;1850(9):1842-8. Epub 2015 May 19.

Structural Genomics Consortium, University of Toronto, Toronto, ON M5G 1L7, Canada; Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON M5S 1A8, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.bbagen.2015.05.013DOI Listing
September 2015

Structural Characterization of Interaction between Human Ubiquitin-specific Protease 7 and Immediate-Early Protein ICP0 of Herpes Simplex Virus-1.

J Biol Chem 2015 Sep 29;290(38):22907-18. Epub 2015 Jul 29.

From the Department of Molecular Biology and Biophysics, University of Connecticut Health, Farmington, Connecticut 06030,

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http://dx.doi.org/10.1074/jbc.M115.664805DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4645603PMC
September 2015

Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth.

Nature 2015 Sep 2;525(7568):206-11. Epub 2015 Sep 2.

Cell and Developmental Biology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

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http://dx.doi.org/10.1038/nature15251DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4568559PMC
September 2015

Probing the epigenome.

Nat Chem Biol 2015 Aug;11(8):542-5

1] Structural Genomics Consortium, University of Toronto, Toronto, Ontario, Canada. [2] Department of Pharmacology and Toxicology, University of Toronto, Toronto, Ontario, Canada.

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http://dx.doi.org/10.1038/nchembio.1871DOI Listing
August 2015

Solution-state NMR structure of the putative morphogene protein BolA (PFE0790c) from Plasmodium falciparum.

Acta Crystallogr F Struct Biol Commun 2015 May 18;71(Pt 5):514-21. Epub 2015 Apr 18.

Department of Medical Biophysics, University of Toronto, Toronto, Ontario, Canada.

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http://dx.doi.org/10.1107/S2053230X1402799XDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4427159PMC
May 2015

Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.

ACS Chem Biol 2015 Apr 28;10(4):1072-81. Epub 2015 Jan 28.

†Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.

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http://dx.doi.org/10.1021/cb500956gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4402254PMC
April 2015

Cbx2 targets PRC1 to constitutive heterochromatin in mouse zygotes in a parent-of-origin-dependent manner.

Mol Cell 2015 Apr 19;58(1):157-71. Epub 2015 Mar 19.

Friedrich Miescher Institute for Biomedical Research, 4058 Basel, Switzerland; Faculty of Sciences, University of Basel, 4056 Basel, Switzerland. Electronic address:

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http://dx.doi.org/10.1016/j.molcel.2015.02.013DOI Listing
April 2015

Discovery of a Dual PRMT5-PRMT7 Inhibitor.

ACS Med Chem Lett 2015 Apr 2;6(4):408-12. Epub 2015 Mar 2.

Structural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada ; The Department of Pharmacology and Toxicology, University of Toronto , Toronto, ON M5S 1A8, Canada.

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http://dx.doi.org/10.1021/ml500467hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4394339PMC
April 2015

Preclinical target validation using patient-derived cells.

Nat Rev Drug Discov 2015 Mar 20;14(3):149-50. Epub 2015 Feb 20.

Structural Genomics Consortium, Department of Medicine, Karolinska University Hospital and Karolinska Institutet, 171 76 Stockholm, Sweden.

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March 2015