Sign in
BiochemistryJournal of the American Chemical Society
Peer-reviewed journal article

Harnessing FBXO31 with terminal amide-functionalized molecules for targeted protein degradation

Chenlu ZhangiD, Xiaokang JiniD, Chen ZhouiD, M. Jamal Jenkins, Isabella A. RihaiD, Xiaoyu ZhangiD

Abstract

Targeted protein degradation (TPD) is a powerful strategy for controlling protein abundance. Here, we establish FBXO31 as a TPD-competent E3 ligase by exploiting its recognition of C-terminal amide-bearing degrons. Using an amidated Ala-Phe motif as a chemical recruiter, multiple small-molecule binders can be transformed into FBXO31-dependent degraders that induce rapid and potent target degradation. Mechanistic studies confirm FBXO31-mediated ternary complex formation and identify key residues in FBXO31 required for recruiter engagement and target degradation. We further show that an FBXO31-based multi-kinase degrader exhibits a distinct and broader degradation profile than a CRBN-based degrader, highlighting a potentially expanded degradable target space beyond CRBN.

PDFDOI

02 /Specification & Classification

Click any tag to browse matching papers
Citations
1
FWCI
2.08
Field percentile
top 15%

Reproducibility ledger

Nobody has reported trying to reproduce this paper yet. Did you replicate an experiment or run the code? Your report saves the next lab a week.

Sign in to file a reproducibility report.

Similarity Map
SelectedSame fieldCross-field
THISBasu '25Ichikawa '23Glennie '26Yu '25Qiu '25Hanzl '23
75% semantic matchBiochemistry
Ananya A. Basu, Chenlu Zhang, Milad Rouhimoghadam+3 more·Journal of the American Chemical Society·Feb 6, 2025· 4 citations