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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.
Sharma, Shikhar; Chung, Chi-Yeh; Uryu, Sean; Petrovic, Jelena; Cao, Joan; Rickard, Amanda; Nady, Nataliya; Greasley, Samantha; Johnson, Eric; Brodsky, Oleg; Khan, Showkhin; Wang, Hui; Wang, Zhenxiong; Zhang, Yong; Tsaparikos, Konstantinos; Chen, Lei; Mazurek, Anthony; Lapek, John; Kung, Pei-Pei; Sutton, Scott; Richardson, Paul F; Greenwald, Eric C; Yamazaki, Shinji; Jones, Rhys; Maegley, Karen A; Bingham, Patrick; Lam, Hieu; Stupple, Alexandra E; Kamal, Aileen; Chueh, Anderly; Cuzzupe, Anthony; Morrow, Benjamin J; Ren, Bin; Carrasco-Pozo, Catalina; Tan, Chin Wee; Bhuva, Dharmesh D; Allan, Elizabeth; Surgenor, Elliot; Vaillant, François; Pehlivanoglu, Havva; Falk, Hendrik; Whittle, James R; Newman, Janet; Cursons, Joseph; Doherty, Judy P; White, Karen L; MacPherson, Laura; Devlin, Mark; Dennis, Matthew L; Hattarki, Meghan K.
  • 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 (
  • 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.
Cell Chem Biol ; 30(10): 1191-1210.e20, 2023 10 19.
Article en En | MEDLINE | ID: mdl-37557181
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Neoplasias de la Mama Límite: Female / Humans Idioma: En Año: 2023 Tipo del documento: Article
Texto completo
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Neoplasias de la Mama Límite: Female / Humans Idioma: En Año: 2023 Tipo del documento: Article