Jingfeng Fu

Shanghai Institute of Materia Medica

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Yubo Zhou

National Center for Drug Screening

Jia Li

Chinese Academy of Sciences

Yaxi Yang

University of Chinese Academy of Sciences

Yuan Pei

Shanghai Institute of Materia Medica

Bing Zhou

Chinese Academy of Sciences

Jingkun Ma

Shanghai Institute of Materia Medica

Tian Mi

Dalian University

Peipei Wang

University of Chinese Academy of Sciences

Ning Song

Shenzhen Children's Hospital

Guanghao Luo

Shanghai Institute of Materia Medica

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Chinese Academy of Sciences

Shanghai Institute of Materia Medica

University of Chinese Academy of Sciences

Zhejiang University

National Center for Drug Screening

Nanjing University of Chinese Medicine

Fudan University

Chinese Academy of Medical Sciences & Peking Union Medical College

East China Normal University

Shanghai Jiao Tong University

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Discovery of a Potent and Selective Degrader for USP7

Angewandte Chemie (2022)

Yuan Pei Jingfeng Fu Yunkai Shi Mengmeng Zhang Guanghao Luo

Abstract The tumor suppressor p53 is the most frequently mutated gene in human cancer and more than half of cancers contain p53 mutations. The development of novel and effective therapeutic strategies for p53 mutant cancer therapy is a big challenge and highly desirable. Ubiquitin‐specific protease 7 (USP7), also known as HAUSP, is a deubiquitinating enzyme and proposed to stabilize the oncogenic E3 ubiquitin ligase MDM2 that promotes the proteosomal degradation of p53. Herein, we report the design and characterization of U7D‐1 as the first selective USP7‐degrading Proteolysis Targeting Chimera (PROTAC). U7D‐1 showed selective and effective USP7 degradation, and maintained potent cell growth inhibition in p53 mutant cancer cells, with USP7 inhibitor showing no activity. These data clearly demonstrated the practicality and importance of PROTAC as a preliminary chemical tool for investigating USP7 protein functions and a promising method for potential p53 mutant cancer therapy.

Deubiquitinating enzyme

Proteolysis

MDMX

10.1002/ange.202204395

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Citations (7)

Discovery of a Highly Potent, Selective and Efficacious USP7 Degrader for the Treatment of Acute Lymphoblastic Leukemia

Journal of Medicinal Chemistry (2024)

Miaomiao Xu Jingfeng Fu Yuan Pei Mengna Li Weijuan Kan

USP7 is an attractive therapeutic target for cancers, especially for acute lymphoblastic leukemia (ALL) with wild-type p53. Herein, we report the discovery of

10.1021/acs.jmedchem.4c01134

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Discovery of a Potent and Selective Degrader for USP7

Angewandte Chemie International Edition (2022)

Yuan Pei Jingfeng Fu Yunkai Shi Mengmeng Zhang Guanghao Luo

Deubiquitinating enzyme

MDMX

Proteolysis

10.1002/anie.202204395

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Citations (29)