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

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

Autores: 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
Publicado en: Chemical Science, Edición 9/9, 2018, Página(s) 2452-2468, ISSN 2041-6520
Editor: Royal Society of Chemistry
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

Autores: Kwok-Ho Chan, Michael Zengerle, Andrea Testa, Alessio Ciulli
Publicado en: Journal of Medicinal Chemistry, 2017, ISSN 0022-2623
Editor: American Chemical Society
DOI: 10.1021/acs.jmedchem.6b01912

Chemical genetics approaches for selective intervention in epigenetics

Autores: Andrew C Runcie, Kwok-Ho Chan, Michael Zengerle, Alessio Ciulli
Publicado en: Current Opinion in Chemical Biology, Edición 33, 2016, Página(s) 186-194, ISSN 1367-5931
Editor: Elsevier BV
DOI: 10.1016/j.cbpa.2016.06.031

Structural basis of PROTAC cooperative recognition for selective protein degradation

Autores: Morgan S Gadd, Andrea Testa, Xavier Lucas, Kwok-Ho Chan, Wenzhang Chen, Douglas J Lamont, Michael Zengerle, Alessio Ciulli
Publicado en: Nature Chemical Biology, Edición 13/5, 2017, Página(s) 514-521, ISSN 1552-4450
Editor: Nature Publishing Group
DOI: 10.1038/nchembio.2329

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