Allosteric targeting of the Fanconi anemia ubiquitin-conjugating enzyme Ube2T by fragment screening

Francesca Morreale, Alessio Bortoluzzi, Viduth Chaugule, Connor Arkinson, Helen Walden, Alessio Ciulli (Lead / Corresponding author)

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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 languageEnglish
Pages (from-to)4093-4098
Number of pages6
JournalJournal of Medicinal Chemistry
Volume60
Issue number9
Early online date24 Apr 2017
DOIs
Publication statusPublished - 11 May 2017

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