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

Kwok Ho Chan
, Michael Zengerle
, Andrea Testa
, Alessio Ciulli (Lead / Corresponding author)

Biological Chemistry and Drug Discovery

Research output: Contribution to journal › Article › peer-review

193 Citations (Scopus)

470 Downloads (Pure)

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Finished
Bump-BET; Bump and Hole Approach to Ellucidate Function of Individual Bromodomains of BET Proteins (Marie Curie Fellowship)
Chan, K. H. (Investigator) & Ciulli, A. (Investigator)
COMMISSION OF THE EUROPEAN COMMUNITIES
1/10/15 → 30/09/17
Project: Research
DrugE3CRL's: Probing Druggability of Multisubunit Complexes: E3 Cullin RING Ligases (ERC Starting Grant)
Ciulli, A. (Investigator)
COMMISSION OF THE EUROPEAN COMMUNITIES
1/05/13 → 30/04/18
Project: Research
A Systems Approach for the Fragment-based Development of Selective Chemical Probes of Bromodomain Function (joint with University of Oxford)
Ciulli, A. (Investigator)
Biotechnology and Biological Sciences Research Council
8/04/13 → 7/06/15
Project: Research
A Translational Engine for Biomedical Discoveries (Strategic Grant)
Fairlamb, A. (Investigator) & Gilbert, I. (Investigator)
1/01/13 → 30/09/15
Project: Research