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

Autor: 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.

Publikováno v: Nature cancer [Nat Cancer] 2021 Oct; Vol. 2 (10), pp. 1002-1017. Date of Electronic Publication: 2021 Sep 27.

GC skew defines distinct RNA polymerase pause sites in CpG island promoters.

Autor: Kellner WA; Department of Radiation Oncology, Emory University School of Medicine, Atlanta, Georgia 30322, USA;, Bell JS; Department of Radiation Oncology, Emory University School of Medicine, Atlanta, Georgia 30322, USA;, Vertino PM; Department of Radiation Oncology, Emory University School of Medicine, Atlanta, Georgia 30322, USA; Winship Cancer Institute of Emory University, Atlanta, Georgia 30322, USA.

Publikováno v: Genome research [Genome Res] 2015 Nov; Vol. 25 (11), pp. 1600-9. Date of Electronic Publication: 2015 Aug 14.

Genome-wide phosphoacetylation of histone H3 at Drosophila enhancers and promoters.

Autor: Kellner WA; Department of Biology, Emory University, Atlanta, Georgia 30322, USA., Ramos E, Van Bortle K, Takenaka N, Corces VG

Publikováno v: Genome research [Genome Res] 2012 Jun; Vol. 22 (6), pp. 1081-8. Date of Electronic Publication: 2012 Apr 16.

Chemical and biological folding contribute to temperature-sensitive DeltaF508 CFTR trafficking.

Autor: Wang X; Department of Cell Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA. xiaodong.wang@utoledo.edu, Koulov AV, Kellner WA, Riordan JR, Balch WE

Publikováno v: Traffic (Copenhagen, Denmark) [Traffic] 2008 Nov; Vol. 9 (11), pp. 1878-93. Date of Electronic Publication: 2008 Jul 30.