Projects per year
Abstract
Ube2T is the E2 ubiquitin-conjugating enzyme of the Fanconi anemia DNA repair pathway and it is overexpressed in several cancers, representing an attractive target for the development of inhibitors. Despite the extensive efforts in targeting the ubiquitin system, very few E2 binders have currently been discovered. Herein we report the identification of a new allosteric pocket on Ube2T through a fragment screening using biophysical methods. Several fragments binding to this site inhibit ubiquitin conjugation in vitro.
Original language | English |
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Pages (from-to) | 4093-4098 |
Number of pages | 6 |
Journal | Journal of Medicinal Chemistry |
Volume | 60 |
Issue number | 9 |
Early online date | 24 Apr 2017 |
DOIs | |
Publication status | Published - 11 May 2017 |
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Dive into the research topics of 'Allosteric targeting of the Fanconi anemia ubiquitin-conjugating enzyme Ube2T by fragment screening'. Together they form a unique fingerprint.Projects
- 3 Finished
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Regulation of DNA Interstrand Crosslink Repaid by Ubiquitin (ICLUB) (ERC Consolidator)
Walden, H. (Investigator)
COMMISSION OF THE EUROPEAN COMMUNITIES
1/09/16 → 31/08/22
Project: Research
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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
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Dissecting and Exploiting Molecular Recognition at Protein-Protein Interfaces (David Phillips Fellowship)
Ciulli, A. (Investigator)
Biotechnology and Biological Sciences Research Council
8/04/13 → 7/07/15
Project: Research
Profiles
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Ciulli, Alessio
- Centre for Targeted Protein Degradation - Professor of Chemical and Structural Biology
Person: Academic