Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Lasko, Loren M.; Jakob, Clarissa G.; Edalji, Rohinton P.; Qiu, Wei; Montgomery, Debra; Digiammarino, Enrico L.; Hansen, T. Matt; Risi, Roberto M.; Frey, Robin; Manaves, Vlasios; Shaw, Bailin; Algire, Mikkel; Hessler, Paul; Lam, Lloyd T.; Uziel, Tamar; Faivre, Emily; Ferguson, Debra; Buchanan, Fritz G.; Martin, Ruth L.; Torrent, Maricel; Chiang, Gary G.; Karukurichi, Kannan; Langston, J. William; Weinert, Brian T.; Choudhary, Chunaram; de Vries, Peter; Kluge, Arthur F.; Patane, Michael A.; Van Drie, John H.; Wang, Ce; McElligott, David; Kesicki, Ed; Marmorstein, Ronen; Sun, Chaohong; Cole, Philip A.; Rosenberg, Saul H.; Michaelides, Michael R.; Lai, Albert; Bromberg, Kenneth D.

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

Loren M. Lasko, Clarissa G. Jakob, Rohinton P. Edalji, Wei Qiu, Debra Montgomery, Enrico L. Digiammarino, T. Matt Hansen, Roberto M. Risi, Robin Frey, Vlasios Manaves, Bailin Shaw, Mikkel Algire, Paul Hessler, Lloyd T. Lam, Tamar Uziel, Emily Faivre, Debra Ferguson, Fritz G. Buchanan, Ruth L. Martin, Maricel Torrent, Gary G. Chiang, Kannan Karukurichi, J. William Langston, Brian T. Weinert, Chunaram Choudhary, Peter de Vries, Arthur F. Kluge, Michael A. Patane, John H. Van Drie, Ce Wang, David McElligott, Ed Kesicki, Ronen Marmorstein, Chaohong Sun, Philip A. Cole, Saul H. Rosenberg, Michael R. Michaelides, Albert Lai () and Kenneth D. Bromberg ()
Additional contact information
Loren M. Lasko: Discovery, Global Pharmaceutical Research and Development
Clarissa G. Jakob: Discovery, Global Pharmaceutical Research and Development
Rohinton P. Edalji: Discovery, Global Pharmaceutical Research and Development
Wei Qiu: Discovery, Global Pharmaceutical Research and Development
Debra Montgomery: Discovery, Global Pharmaceutical Research and Development
Enrico L. Digiammarino: Discovery, Global Pharmaceutical Research and Development
T. Matt Hansen: Discovery, Global Pharmaceutical Research and Development
Roberto M. Risi: Discovery, Global Pharmaceutical Research and Development
Robin Frey: Discovery, Global Pharmaceutical Research and Development
Vlasios Manaves: Discovery, Global Pharmaceutical Research and Development
Bailin Shaw: Discovery, Global Pharmaceutical Research and Development
Mikkel Algire: Discovery, Global Pharmaceutical Research and Development
Paul Hessler: Discovery, Global Pharmaceutical Research and Development
Lloyd T. Lam: Discovery, Global Pharmaceutical Research and Development
Tamar Uziel: Discovery, Global Pharmaceutical Research and Development
Emily Faivre: Discovery, Global Pharmaceutical Research and Development
Debra Ferguson: Discovery, Global Pharmaceutical Research and Development
Fritz G. Buchanan: Discovery, Global Pharmaceutical Research and Development
Ruth L. Martin: Discovery, Global Pharmaceutical Research and Development
Maricel Torrent: Discovery, Global Pharmaceutical Research and Development
Gary G. Chiang: Discovery, Global Pharmaceutical Research and Development
Kannan Karukurichi: Petra Pharma Corporation
J. William Langston: Faraday Pharmaceuticals, 1616 Eastlake Ave E.
Brian T. Weinert: the Novo Nordisk Foundation Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen
Chunaram Choudhary: the Novo Nordisk Foundation Center for Protein Research, Faculty of Health and Medical Sciences, University of Copenhagen
Peter de Vries: Cascadian Therapeutics, Inc., 2601 Fourth Avenue
Arthur F. Kluge: I-to-D, Inc.
Michael A. Patane: Mitobridge, Inc.
John H. Van Drie: Van Drie Research, 109 Millpond
Ce Wang: China Novartis In stitutes for BioMedical Research
David McElligott: Accelerator Corporation
Ed Kesicki: Petra Pharma Corporation
Ronen Marmorstein: Perelman School of Medicine, University of Pennsylvania
Chaohong Sun: Discovery, Global Pharmaceutical Research and Development
Philip A. Cole: Johns Hopkins University
Saul H. Rosenberg: Discovery, Global Pharmaceutical Research and Development
Michael R. Michaelides: Discovery, Global Pharmaceutical Research and Development
Albert Lai: Discovery, Global Pharmaceutical Research and Development
Kenneth D. Bromberg: Discovery, Global Pharmaceutical Research and Development

Nature, 2017, vol. 550, issue 7674, 128-132

Abstract: A potent and selective catalytic inhibitor of p300/CBP histone acetyltransferases suppresses tumour proliferation across multiple cell lineages, illustrating the therapeutic potential of drug-like small molecules that target histone acetyltransferases.

Date: 2017
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DOI: 10.1038/nature24028

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