Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras (PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described the use of sulfonyl exchange chemistry to design binders that covalently engage histidine 353 in CRBN for the first time....

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Bibliographic Details

Published in:	RSC chemical biology Vol. 4; no. 11; pp. 96 - 912
Main Authors:	Nowak, Rados aw P, Ragosta, Leah, Huerta, Fidel, Liu, Hu, Ficarro, Scott B, Cruite, Justin T, Metivier, Rebecca J, Donovan, Katherine A, Marto, Jarrod A, Fischer, Eric S, Zerfas, Breanna L, Jones, Lyn H
Format:	Journal Article
Language:	English
Published:	England RSC 01.11.2023
Subjects:	Chemistry
ISSN:	2633-0679, 2633-0679
Online Access:	Get full text
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