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Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.

Autor: Sharma S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA. Electronic address: shikhar.sharma@pfizer.com., Chung CY; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Uryu S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Petrovic J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Cao J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Rickard A; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Nady N; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Greasley S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Johnson E; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Brodsky O; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Khan S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Wang H; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Wang Z; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Zhang Y; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Tsaparikos K; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Chen L; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Mazurek A; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Lapek J; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Kung PP; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Sutton S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Richardson PF; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Greenwald EC; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Yamazaki S; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Jones R; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Maegley KA; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Bingham P; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Lam H; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA., Stupple AE; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Kamal A; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Chueh A; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Cuzzupe A; SYNthesis Med Chem (Australia) Pty Ltd, Bio21 Institute, 30 Flemington Road, Parkville, VIC 3052, Australia., Morrow BJ; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia., Ren B; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Carrasco-Pozo C; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Discovery Biology, Centre for Cellular Phenomics, Griffith University, Brisbane QLD 4111, Australia., Tan CW; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Bhuva DD; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Allan E; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Surgenor E; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Vaillant F; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Pehlivanoglu H; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Falk H; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Whittle JR; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Newman J; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Cursons J; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Doherty JP; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., White KL; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., MacPherson L; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Devlin M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dennis ML; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Hattarki MK; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., De Silva M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Camerino MA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Butler MS; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dolezal O; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Pilling P; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Foitzik R; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; OncologyOne Pty Ltd, Melbourne, VIC 3000, Australia., Stupple PA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Lagiakos HR; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Walker SR; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Hediyeh-Zadeh S; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Nuttall S; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Spall SK; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Charman SA; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Connor T; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Peat TS; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Commonwealth Scientific and Industrial Research Organisation (CSIRO), Parkville, VIC 3052, Australia., Avery VM; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Discovery Biology, Centre for Cellular Phenomics, Griffith University, Brisbane QLD 4111, Australia., Bozikis YE; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; Medicinal Chemistry and Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Yang Y; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Zhang M; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia., Monahan BJ; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; CANThera Discovery, Melbourne, VIC 3000, Australia., Voss AK; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Thomas T; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Street IP; Cancer Therapeutics CRC, Melbourne, VIC 3000, Australia; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; OncologyOne Pty Ltd, Melbourne, VIC 3000, Australia; Children's Cancer Institute, Randwick, NSW 2031, Australia; University of New South Wales, Randwick, NSW 2021, Australia., Dawson SJ; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Dawson MA; Peter MacCallum Cancer Centre, Melbourne VIC 3000, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Parkville, VIC 3052, Australia., Lindeman GJ; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medicine, Royal Melbourne Hospital, The University of Melbourne, Parkville, VIC 3010, Australia; Parkville Familial Cancer Centre and Department of Medical Oncology, The Royal Melbourne Hospital and Peter MacCallum Cancer Centre, Parkville, VIC 3050, Australia., Davis MJ; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia; Department of Clinical Pathology, Faculty of Medicine, Dentistry and Health Sciences, University of Melbourne, Parkville, VIC 3010, Australia., Visvader JE; The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3052, Australia., Paul TA; Pfizer, Oncology Research & Development, San Diego, CA 92121, USA. Electronic address: thomas.a.paul@pfizer.com.

Publikováno v: Cell chemical biology [Cell Chem Biol] 2023 Oct 19; Vol. 30 (10), pp. 1191-1210.e20. Date of Electronic Publication: 2023 Aug 08.

Temporal Analysis of Brd4 Displacement in the Control of B Cell Survival, Proliferation, and Differentiation.

Autor: Kong IY; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Rimes JS; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Light A; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Todorovski I; Cancer Therapeutics and Cancer Immunology Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia., Jones S; Centre for Inflammatory Diseases, School of Clinical Sciences, Monash University, Parkville, VIC 3052, Australia., Morand E; Centre for Inflammatory Diseases, School of Clinical Sciences, Monash University, Parkville, VIC 3052, Australia., Knight DA; Cancer Therapeutics and Cancer Immunology Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia., Bergman YE; Cancer Therapeutics CRC (CTx), Melbourne, VIC 3000, Australia; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Hogg SJ; Cancer Therapeutics and Cancer Immunology Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia., Falk H; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Cancer Therapeutics CRC (CTx), Melbourne, VIC 3000, Australia., Monahan BJ; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Cancer Therapeutics CRC (CTx), Melbourne, VIC 3000, Australia., Stupple PA; Cancer Therapeutics CRC (CTx), Melbourne, VIC 3000, Australia; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia., Street IP; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Cancer Therapeutics CRC (CTx), Melbourne, VIC 3000, Australia., Heinzel S; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Bouillet P; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Johnstone RW; Cancer Therapeutics and Cancer Immunology Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia., Hodgkin PD; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia., Vervoort SJ; Cancer Therapeutics and Cancer Immunology Program, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia. Electronic address: stephin.vervoort@petermac.org., Hawkins ED; Walter and Eliza Hall Institute of Medical Research, The University of Melbourne, 1G Royal Parade, Parkville, VIC 3052, Australia; Department of Medical Biology, The University of Melbourne, Parkville, VIC 3010, Australia. Electronic address: hawkins.e@wehi.edu.au.

Publikováno v: Cell reports [Cell Rep] 2020 Oct 20; Vol. 33 (3), pp. 108290.