C
Caroline Hughes
Publications - 2
Citations - 206
Caroline Hughes is an academic researcher. The author has contributed to research in topics: Druggability & Allosteric regulation. The author has an hindex of 2, co-authored 2 publications receiving 152 citations.
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Discovery and characterization of highly potent and selective allosteric USP7 inhibitors
Gerald Gavory,Colin O'Dowd,Matthew Helm,Jakub T. Flasz,Elias Arkoudis,Anthony Dossang,Caroline Hughes,Eamon Cassidy,Keeva McClelland,Ewa Odrzywol,Natalie Page,Oliver Barker,Hugues Miel,Tim Harrison +13 more
TL;DR: The identification, optimization and detailed characterization of highly potent, selective USP7 inhibitors together with their less active, enantiomeric counterparts are described and co-crystal structures of a human DUB enzyme complexed with small-molecule inhibitors are disclosed, revealing a previously undisclosed allosteric binding site.
Journal ArticleDOI
Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors
Colin O'Dowd,Matthew Helm,J. S. Shane Rountree,Jakub T. Flasz,Elias Arkoudis,Hugues Miel,Peter Hewitt,Linda Jordan,Oliver Barker,Caroline Hughes,Ewelina Rozycka,Eamon Cassidy,Keeva McClelland,Ewa Odrzywol,Natalie Page,Stephanie Feutren-Burton,Scarlett Dvorkin,Gerald Gavory,Tim Harrison +18 more
TL;DR: Potent, novel, and selective inhibitors of USP7 have been developed using both rational and structure-guided design enabled by high-resolution cocrystallography, and initial efforts aimed at developing compounds suitable for in vivo experiments are described.