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

doi:10.1039/d1cc06525d

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

Biochemistry and Molecular Biology

Research output: Contribution to journal › Article › peer-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 language	English (US)
Pages (from-to)	2383-2386
Number of pages	4
Journal	Chemical Communications
Volume	58
Issue number	14
DOIs	https://doi.org/10.1039/d1cc06525d
State	Published - Feb 18 2022

ASJC Scopus subject areas

Electronic, Optical and Magnetic Materials
General Chemistry
Ceramics and Composites
Metals and Alloys
Materials Chemistry
Surfaces, Coatings and Films
Catalysis

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

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.",

author = "Yuqian Yan and Jingwei Shao and Donglin Ding and Yunqian Pan and Phuc Tran and Wei Yan and Zhengyu Wang and Li, {Hong Yu} and Haojie Huang",

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T1 - 3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O'PROTAC

AU - Yan, Yuqian

AU - Shao, Jingwei

AU - Ding, Donglin

AU - Pan, Yunqian

AU - Tran, Phuc

AU - Yan, Wei

AU - Wang, Zhengyu

AU - Li, Hong Yu

AU - Huang, Haojie

PY - 2022/2/18

Y1 - 2022/2/18

N2 - 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.

AB - 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.

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

Abstract

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