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Bump and Hole approach to elucidate function of individual bromodomains of BET proteins

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Publications

Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition

Author(s): A. C. Runcie, M. Zengerle, K.-H. Chan, A. Testa, L. van Beurden, M. G. J. Baud, O. Epemolu, L. C. J. Ellis, K. D. Read, V. Coulthard, A. Brien, A. Ciulli
Published in: Chemical Science, Issue 9/9, 2018, Page(s) 2452-2468, ISSN 2041-6520
DOI: 10.1039/C7SC02536J

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Author(s): Kwok-Ho Chan, Michael Zengerle, Andrea Testa, Alessio Ciulli
Published in: Journal of Medicinal Chemistry, 2017, ISSN 0022-2623
DOI: 10.1021/acs.jmedchem.6b01912

Chemical genetics approaches for selective intervention in epigenetics

Author(s): Andrew C Runcie, Kwok-Ho Chan, Michael Zengerle, Alessio Ciulli
Published in: Current Opinion in Chemical Biology, Issue 33, 2016, Page(s) 186-194, ISSN 1367-5931
DOI: 10.1016/j.cbpa.2016.06.031

Structural basis of PROTAC cooperative recognition for selective protein degradation

Author(s): Morgan S Gadd, Andrea Testa, Xavier Lucas, Kwok-Ho Chan, Wenzhang Chen, Douglas J Lamont, Michael Zengerle, Alessio Ciulli
Published in: Nature Chemical Biology, Issue 13/5, 2017, Page(s) 514-521, ISSN 1552-4450
DOI: 10.1038/nchembio.2329