A new avenue for molecular glues: Rapid discovery of a NFKB1 degrader

Angela T Fan; Bridget T Boyle; Fleur M Ferguson

doi:10.1016/j.chembiol.2023.04.002

A new avenue for molecular glues: Rapid discovery of a NFKB1 degrader

Cell Chem Biol. 2023 Apr 20;30(4):340-342. doi: 10.1016/j.chembiol.2023.04.002.

Authors

Angela T Fan¹, Bridget T Boyle¹, Fleur M Ferguson²

Affiliations

¹ Department of Chemistry and Biochemistry, University of California San Diego, La Jolla, CA, USA.
² Department of Chemistry and Biochemistry, University of California San Diego, La Jolla, CA, USA; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, CA, USA.

PMID: 37084716
DOI: 10.1016/j.chembiol.2023.04.002

Abstract

Targeted protein degradation using molecular glues is a powerful method for targeting traditionally undruggable proteins. One challenge in molecular glue discovery is the absence of rational discovery methods. Here, King et al. leverage covalent library screening with chemoproteomics platforms to rapidly discover a molecular glue targeting NFKB1 via UBE2D recruitment.

Publication types

Comment

MeSH terms

Drug Discovery* / methods
NF-kappa B p50 Subunit* / chemistry
NF-kappa B p50 Subunit* / metabolism
Proteolysis Targeting Chimera / chemistry
Proteolysis Targeting Chimera / metabolism
Proteolysis*

Substances

NF-kappa B p50 Subunit
Proteolysis Targeting Chimera