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.

Computer-Aided Identification and Design of Ligands for Multi-Targeting Inhibition of a Molecular Acute Myeloid Leukemia Network.

Autor: Asfa, Seyedeh Sadaf^1,2,3,4 (AUTHOR) sadaf.asfa@gmail.com, Arshinchi Bonab, Reza^1,2,3,4 (AUTHOR) rezaarshinchi1994@gmail.com, Önder, Onur^1,2 (AUTHOR) onderonur1205@gmail.com, Uça Apaydın, Merve^1,2 (AUTHOR) merve.uca@ibg.edu.tr, Döşeme, Hatice^1,2 (AUTHOR) hatice.doseme@ibg.edu.tr, Küçük, Can⁵ (AUTHOR) can.kucuk@deu.edu.tr, Georgakilas, Alexandros G.⁶ (AUTHOR) alexg@mail.ntua.gr, Stadler, Bernhard M.⁷ (AUTHOR) Bernhard.stadler@th-nuernberg.de, Logotheti, Stella⁸ (AUTHOR) styliani.logotheti@dkfz-heidelberg.de, Kale, Seyit^1,9 (AUTHOR) seyit.kale@ibg.edu.tr, Pavlopoulou, Athanasia^1,2 (AUTHOR) athanasia.pavlopoulou@ibg.edu.tr

Publikováno v: Cancers. Nov2024, Vol. 16 Issue 21, p3607. 30p.

Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis.

Autor: Savitski MM; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany; Genome Biology Unit, European Molecular Biology Laboratory, 69117 Heidelberg, Germany. Electronic address: mikhail.savitski@embl.de., Zinn N; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Faelth-Savitski M; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Poeckel D; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Gade S; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Becher I; Genome Biology Unit, European Molecular Biology Laboratory, 69117 Heidelberg, Germany., Muelbaier M; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Wagner AJ; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Strohmer K; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Werner T; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Melchert S; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Petretich M; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Rutkowska A; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Vappiani J; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Franken H; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Steidel M; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Sweetman GM; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Gilan O; Cancer Research Division, Peter MacCallum Cancer Centre, East Melbourne, VIC 3002, Australia., Lam EYN; Cancer Research Division, Peter MacCallum Cancer Centre, East Melbourne, VIC 3002, Australia., Dawson MA; Cancer Research Division, Peter MacCallum Cancer Centre, East Melbourne, VIC 3002, Australia., Prinjha RK; Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK., Grandi P; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Bergamini G; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany. Electronic address: giovanna.2.bergamini@gsk.com., Bantscheff M; Cellzome GmbH, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany. Electronic address: marcus.x.bantscheff@gsk.com.

Publikováno v: Cell [Cell] 2018 Mar 22; Vol. 173 (1), pp. 260-274.e25. Date of Electronic Publication: 2018 Mar 15.

Targeting DNA Methylation Machinery in Pediatric Solid Tumors.

Autor: Cristalli, Camilla¹ (AUTHOR) camilla.cristalli@ior.it, Scotlandi, Katia¹ (AUTHOR) camilla.cristalli@ior.it

Publikováno v: Cells (2073-4409). Jul2024, Vol. 13 Issue 14, p1209. 37p.

Histone deficiency and hypoacetylation in the aging retinal pigment epithelium.

Autor: Dubey, Sushil K.¹ (AUTHOR), Dubey, Rashmi¹ (AUTHOR), Prajapati, Subhash C.² (AUTHOR), Jung, Kyungsik¹ (AUTHOR), Mohan, Kabhilan¹ (AUTHOR), Liu, Xinan³ (AUTHOR), Roney, Jacob⁴ (AUTHOR), Tian, Wenjian¹ (AUTHOR), Abney, Jennifer⁴ (AUTHOR), Giarmarco, Michelle M.⁵ (AUTHOR), Hernandez, Alvaro G.⁶ (AUTHOR), Liu, Jinze⁷ (AUTHOR), Kleinman, Mark E.¹ (AUTHOR) kleinman@etsu.edu

Publikováno v: Aging Cell. May2024, Vol. 23 Issue 5, p1-17. 17p.