Nature Communications (Apr 2019)
A chemical toolbox for the study of bromodomains and epigenetic signaling
- Qin Wu,
- David Heidenreich,
- Stanley Zhou,
- Suzanne Ackloo,
- Andreas Krämer,
- Kiran Nakka,
- Evelyne Lima-Fernandes,
- Genevieve Deblois,
- Shili Duan,
- Ravi N. Vellanki,
- Fengling Li,
- Masoud Vedadi,
- Jeffrey Dilworth,
- Mathieu Lupien,
- Paul E. Brennan,
- Cheryl H. Arrowsmith,
- Susanne Müller,
- Oleg Fedorov,
- Panagis Filippakopoulos,
- Stefan Knapp
Affiliations
- Qin Wu
- Structural Genomics Consortium, University of Toronto
- David Heidenreich
- Structural Genomics Consortium, University of Toronto
- Stanley Zhou
- Princess Margaret Cancer Centre, University Health Network
- Suzanne Ackloo
- Structural Genomics Consortium, University of Toronto
- Andreas Krämer
- Structural Genomics Consortium, Buchmann Institute for Life Sciences, Goethe-University Frankfurt
- Kiran Nakka
- Sprott Centre for Stem Cell Research, Regenerative Medicine Program, Ottawa Hospital Research Institute
- Evelyne Lima-Fernandes
- Structural Genomics Consortium, University of Toronto
- Genevieve Deblois
- Princess Margaret Cancer Centre, University Health Network
- Shili Duan
- Princess Margaret Cancer Centre, University Health Network
- Ravi N. Vellanki
- Princess Margaret Cancer Centre, University Health Network
- Fengling Li
- Structural Genomics Consortium, University of Toronto
- Masoud Vedadi
- Structural Genomics Consortium, University of Toronto
- Jeffrey Dilworth
- Sprott Centre for Stem Cell Research, Regenerative Medicine Program, Ottawa Hospital Research Institute
- Mathieu Lupien
- Princess Margaret Cancer Centre, University Health Network
- Paul E. Brennan
- Target Discovery Institute and Structural Genomics Consortium, University of Oxford
- Cheryl H. Arrowsmith
- Structural Genomics Consortium, University of Toronto
- Susanne Müller
- Structural Genomics Consortium, Buchmann Institute for Life Sciences, Goethe-University Frankfurt
- Oleg Fedorov
- Target Discovery Institute and Structural Genomics Consortium, University of Oxford
- Panagis Filippakopoulos
- Target Discovery Institute and Structural Genomics Consortium, University of Oxford
- Stefan Knapp
- Structural Genomics Consortium, Buchmann Institute for Life Sciences, Goethe-University Frankfurt
- DOI
- https://doi.org/10.1038/s41467-019-09672-2
- Journal volume & issue
-
Vol. 10,
no. 1
pp. 1 – 14
Abstract
Bromodomains are conserved protein interaction modules that recognize acetyl-lysine modifications. Here the authors present a set of 25 selective small molecule inhibitors covering 29 human bromodomain targets and comprehensively evaluate the selectivity of this probe-set.
