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Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.

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Title: Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Authors: Pappalardi MB; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Keenan K; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Cockerill M; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK.; These authors contributed equally: Mark Cockerill, Wendy A. Kellner., Kellner WA; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA.; These authors contributed equally: Mark Cockerill, Wendy A. Kellner., Stowell A; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Sherk C; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Wong K; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Pathuri S; Department of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, TX, USA., Briand J; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Steidel M; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Chapman P; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Groy A; Future Pipeline Discovery, GlaxoSmithKline, Collegeville, PA, USA., Wiseman AK; Center for Epigenetics, Van Andel Research Institute, Grand Rapids, MI, USA., McHugh CF; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Campobasso N; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Graves AP; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Fairweather E; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Werner T; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Raoof A; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Butlin RJ; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Rueda L; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Horton JR; Department of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, TX, USA., Fosbenner DT; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Zhang C; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Handler JL; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Muliaditan M; Drug Metabolism and Pharmacokinetics Modelling, GlaxoSmithKline, Stevenage, UK., Mebrahtu M; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Jaworski JP; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., McNulty DE; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Burt C; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Eberl HC; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Taylor AN; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Ho T; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Merrihew S; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Foley SW; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Rutkowska A; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Li M; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Romeril SP; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Goldberg K; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Zhang X; Department of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, TX, USA., Kershaw CS; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Bantscheff M; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Jurewicz AJ; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Minthorn E; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Grandi P; Cellzome GmbH, Functional Genomics, GlaxoSmithKline, Heidelberg, Germany., Patel M; Medicinal Science & Technology, GlaxoSmithKline, Collegeville, PA, USA., Benowitz AB; Future Pipeline Discovery, GlaxoSmithKline, Collegeville, PA, USA., Mohammad HP; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Gilmartin AG; Future Pipeline Discovery, GlaxoSmithKline, Collegeville, PA, USA., Prinjha RK; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Ogilvie D; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Carpenter C; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Heerding D; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Baylin SB; Department of Oncology, The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, MD, USA., Jones PA; Center for Epigenetics, Van Andel Research Institute, Grand Rapids, MI, USA., Cheng X; Department of Epigenetics and Molecular Carcinogenesis, University of Texas MD Anderson Cancer Center, Houston, TX, USA., King BW; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Luengo JI; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., Jordan AM; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Waddell I; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, UK., Kruger RG; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA., McCabe MT; Cancer Epigenetics Research Unit, Oncology, GlaxoSmithKline, Collegeville, PA, USA.
Source: Nature cancer [Nat Cancer] 2021 Oct; Vol. 2 (10), pp. 1002-1017. Date of Electronic Publication: 2021 Sep 27.
Publication Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Journal Info: Publisher: Nature Publishing Group Country of Publication: England NLM ID: 101761119 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2662-1347 (Electronic) Linking ISSN: 26621347 NLM ISO Abbreviation: Nat Cancer
Database: MEDLINE Ultimate
FullText Text:
  Availability: 0
Header DbId: mdl
DbLabel: MEDLINE Ultimate
An: 34790902
AccessLevel: 2
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
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  Data: Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
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  Data: <searchLink fieldCode="JN" term="%22101761119%22">Nature cancer</searchLink> [Nat Cancer] 2021 Oct; Vol. 2 (10), pp. 1002-1017. <i>Date of Electronic Publication: </i>2021 Sep 27.
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          Name:
            NameFull: Prinjha RK
      – PersonEntity:
          Name:
            NameFull: Ogilvie D
      – PersonEntity:
          Name:
            NameFull: Carpenter C
      – PersonEntity:
          Name:
            NameFull: Heerding D
      – PersonEntity:
          Name:
            NameFull: Baylin SB
      – PersonEntity:
          Name:
            NameFull: Jones PA
      – PersonEntity:
          Name:
            NameFull: Cheng X
      – PersonEntity:
          Name:
            NameFull: King BW
      – PersonEntity:
          Name:
            NameFull: Luengo JI
      – PersonEntity:
          Name:
            NameFull: Jordan AM
      – PersonEntity:
          Name:
            NameFull: Waddell I
      – PersonEntity:
          Name:
            NameFull: Kruger RG
      – PersonEntity:
          Name:
            NameFull: McCabe MT
    IsPartOfRelationships:
      – BibEntity:
          Dates:
            – D: 01
              M: 10
              Text: 2021 Oct
              Type: published
              Y: 2021
          Identifiers:
            – Type: issn-electronic
              Value: 2662-1347
          Numbering:
            – Type: volume
              Value: 2
            – Type: issue
              Value: 10
          Titles:
            – TitleFull: Nature cancer
              Type: main
ResultId 1