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

Yuqian Yan; Jingwei Shao; Donglin Ding; Yang Pan; Phuc Tran; Wei Yan; Zhengyu Wang; Hong-yu Li; Hanlin Huang

doi:10.1039/d1cc06525d

journal article Jan 01, 2022

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

Yuqian Yan Jingwei Shao Donglin Ding Yang Pan

Phuc Tran Wei Yan

Zhengyu Wang

Hong-yu Li Hanlin Huang

Chemical Communications Vol. 58 No. 14 pp. 2383-2386 · Royal Society of Chemistry (RSC)

View at Publisher Save 10.1039/d1cc06525d

Abstract

In this study, we discovered 3-aminophthalic acid as a new ligand of cereblon (CRBN) E3 ubiquitin ligase and developed a phthalic acid-based O’PROTAC for ERG destruction, expanding the pool of ligands for development of PROTACs, especially O’PROTACs.

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Details

Published: Jan 01, 2022
Vol/Issue: 58(14)
Pages: 2383-2386
License: View

Authors

Y

Yuqian Yan

Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA

J

Jingwei Shao

Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA

D

Donglin Ding

Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA

Y

Yang Pan

Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA

P

Phuc Tran

Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA

W

Wei Yan

Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA

Z

Zhengyu Wang

Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA

H

Hong-yu Li

Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA

H

Hanlin Huang

Department of Biochemistry and Molecular Biology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA; Department of Urology, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA; Mayo Clinic Cancer Center, Mayo Clinic College of Medicine and Science, Rochester, MN 55905, USA

Cite This Article

Yuqian Yan, Jingwei Shao, Donglin Ding, et al. (2022). 3-Aminophthalic acid, a new cereblon ligand for targeted protein degradation by O’PROTAC. Chemical Communications, 58(14), 2383-2386. https://doi.org/10.1039/d1cc06525d

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

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