Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

Author:

Fedorov Oleg12ORCID,Castex Josefina3,Tallant Cynthia12,Owen Dafydd R.4,Martin Sarah12,Aldeghi Matteo15,Monteiro Octovia12,Filippakopoulos Panagis26,Picaud Sarah2,Trzupek John D.4ORCID,Gerstenberger Brian S.4,Bountra Chas12ORCID,Willmann Dominica3,Wells Christopher12ORCID,Philpott Martin12,Rogers Catherine12ORCID,Biggin Philip C.5,Brennan Paul E.12ORCID,Bunnage Mark E.4,Schüle Roland378,Günther Thomas3,Knapp Stefan128ORCID,Müller Susanne12ORCID

Affiliation:

1. Target Discovery Institute, University of Oxford, NDM Research Building, Roosevelt Drive, Oxford OX3 7FZ, UK.

2. Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.

3. Urologische Klinik und Zentrale Klinische Forschung, Klinikum der Universität Freiburg, Breisacher Strasse 66, 79106 Freiburg, Germany.

4. Pfizer Worldwide Medicinal Chemistry, 610 Main Street, Cambridge, MA 02139, USA.

5. Department of Biochemistry, University of Oxford, South Parks Road, Oxford OX1 3QU, UK.

6. Ludwig Institute for Cancer Research, University of Oxford, Oxford OX3 7DQ, UK.

7. Deutsches Konsortium für Translationale Krebsforschung, Standort Freiburg, 79106 Freiburg, Germany.

8. Institute for Pharmaceutical Chemistry and Buchmann Institute for Molecular Life Sciences, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.

Abstract

PFI-3, a novel inhibitor targeting the bromodomains of essential components of the BAF/PBAF complex, affects the differentiation of ESC and TSC.

Funder

Wellcome Trust

SGC

Else Kröner-Fresenius-Stiftung

European Research Council

Deutsche Forschungsgemeinschaft

Engineering and Physical Sciences Research Council

DTC

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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