3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O'PROTAC

Yuqian Yan, Jingwei Shao, Donglin Ding, Yunqian Pan, Phuc Tran, Wei Yan, Zhengyu Wang, Hong Yu Li, Haojie Huang

Research output: Contribution to journalArticlepeer-review

Abstract

In this study, we identified 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O'PROTAC for degradation of the ERG transcription factor. This phthalic acid-based O'PROTAC presented an efficacy in degrading ERG comparable to those displayed by pomalidomide-based ERG O'PROTACs. Moreover, phthalic acid - being more chemically stable and economical than classical immunomodulatory drugs (IMiDs) - represents, as a ligand, a new alternative for the development of PROTACs, especially O'PROTACs.

Original languageEnglish (US)
Pages (from-to)2383-2386
Number of pages4
JournalChemical Communications
Volume58
Issue number14
DOIs
StatePublished - Feb 18 2022
Externally publishedYes

ASJC Scopus subject areas

  • Catalysis
  • Electronic, Optical and Magnetic Materials
  • Ceramics and Composites
  • Chemistry(all)
  • Surfaces, Coatings and Films
  • Metals and Alloys
  • Materials Chemistry

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