Cereblon covalent modulation through structure-based design of histidine targeting chemical probes-Reference-Cited by-同舟云学术

Cereblon covalent modulation through structure-based design of histidine targeting chemical probes

Published:2022 Issue:9 Volume:3 Page:1105-1110
ISSN:2633-0679
Container-title:RSC Chemical Biology
language:en
Short-container-title:RSC Chem. Biol.

Author:

Cruite Justin T.¹²,Dann Geoffrey P.¹²,Che Jianwei¹²,Donovan Katherine A.²³,Ferrao Silas¹,Ficarro Scott B.⁴⁵,Fischer Eric S.¹²³^ORCID,Gray Nathanael S.⁶,Huerta Fidel¹,Kong Nikki R.¹²,Liu Hu¹²,Marto Jarrod A.⁴⁵,Metivier Rebecca J.³,Nowak Radosław P.¹²^ORCID,Zerfas Breanna L.¹²,Jones Lyn H.¹²^ORCID

Affiliation:

1. Center for Protein Degradation, Dana-Farber Cancer Institute, Boston, MA, USA

2. Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA

3. Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA

4. Department of Cancer Biology, Department of Oncologic Pathology, and Blais Proteomics Center, Dana-Farber Cancer Institute, Boston, MA, USA

5. Department of Pathology, Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA

6. Department of Chemical and Systems Biology, ChEM-H, Stanford Cancer Institute, School of Medicine, Stanford University, Stanford, CA, USA

Abstract

Synthetic re-engineering of a surface histidine residue on cereblon using sulfonyl exchange chemistry yielded potent irreversible modulators of the E3 ubiquitin ligase complex, including a molecular glue degrader of the novel neosubstrate NTAQ1.

Publisher

Royal Society of Chemistry (RSC)

Subject

Biochemistry, Genetics and Molecular Biology (miscellaneous),Molecular Biology,Biochemistry,Chemistry (miscellaneous)

Link

http://pubs.rsc.org/en/content/articlepdf/2022/CB/D2CB00078D

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