Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47.
Weinstock, Joseph, Wu, Jian, Cao, Ping, Kingsbury, William D., McDermott, Jeffrey L., Kodrasov, Matthew P., McKelvey, Devin M., Suresh Kumar, K. G. +3 more·2012·ACS Medicinal Chemistry Letters
Cited by (198)
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- USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4Tingzheng Pan, Xuetao Li, Yanyan Li, Zhennan Tao, Hui Yao, Yue Wu, Guangliang Chen, Kai Zhang, Youxin Zhou, Yulun Huang · 2021 · Cancer Cell International
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- Role of Ubiquitin-Specific Peptidase 47 in Cancers and Other DiseasesKailing Pan, Junhao Fu, Wenxia Xu · 2021 · Frontiers in Cell and Developmental Biology
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- Ubiquitin-Specific Proteases as Druggable Targets.Mindy I. Davis, Anton M. Simeonov · 2015 · PubMed
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- USP7 stabilizes EZH2 and enhances cancer malignant progression.Nana Zheng, Man Chu, Min Lin, Youhua He, Zhiwei Peter Wang · 2020 · PubMed Central
- Inhibition of the deubiquitinating enzyme USP47 as a novel targeted therapy for hematologic malignancies expressing mutant EZH2Jing Chun Yang, Ellen Weisberg, Shuang Qi, Wei Min NI, Husheng Mei, Zuowei Wang, Chengcheng Meng, Shengzhe Zhang, Mingqi Hou, Ziping Qi et al. · 2022 · Leukemia
- Targeting HAUSP in both p53 wildtype and p53-mutant tumorsOmid Tavana, Hongbin Sun, Wei Jun Gu · 2018 · Cell Cycle
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- Clinical Spectrum of USP8 Pathogenic Variants in Cushing's DiseaseRosa Rebollar‐Vega, Julia María Zuarth-Vázquez, Laura Cristina Hernández-Ramírez · 2023 · Archives of Medical Research
- USP47 deubiquitylates Groucho/TLE to promote Wnt–β-catenin signalingSara N. Kassel, Alison J. Hanson, Hassina Benchabane, Kenyi Saito‐Diaz, Carly R. Cabel, Lily Goldsmith, Muhammad Taha, Aksheta Kanuganti, Victoria H. Ng, George Jing Xu et al. · 2023 · Science Signaling
- The key vulnerabilities and therapeutic opportunities in the USP7-p53/MDM2 axis in cancerGouranga Saha, Mrinal K. Ghosh · 2025 · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research
- Ubiquitin-specific protease 12 interacting partners Uaf-1 and WDR20 are potential therapeutic targets in prostate cancerUrszula Lucja McClurg, Victoria J. Harle, Arash Nabbi, Amanda Batalha-Pereira, Scott C. Walker, Kelly Coffey, Luke Gaughan, Stuart R. McCracken, Craig N. Robson · 2015 · Oncotarget
- Discovery of USP7 small-molecule allosteric inhibitorsOlof Engström, Oscar Belda, Mari Kullman-Magnusson, Mikaela Rapp, Kerstin Böhm, Ralf Paul, Ian M. Henderson, Dean J. Derbyshire, Sofia Karlström, Kevin E. B. Parkes et al. · 2020 · Bioorganic & Medicinal Chemistry Letters
- A patent review of ubiquitin-specific protease 7 (USP7) inhibitors (2014-present)Peng Li, Ying Liu, Hong-Min Liu · 2022 · Expert Opinion on Therapeutic Patents
- Natural Agents as Novel Potential Source of Proteasome Inhibitors with Anti-Tumor Activity: Focus on Multiple MyelomaFrancesca Alessandra Ambrosio, Giosuè Costa, Maria Eugenia Gallo Cantafio, Roberta Torcasio, Francesco Trapasso, Stefano Alcaro, Giuseppe Viglietto, Nicola Amodio · 2023 · Molecules
- Structural and functional characterization of USP47 reveals a hot spot for inhibitor designSang Chul Shin, Jin‐Young Park, Kyung‐Hee Kim, Jung Min Yoon, Jinhong Cho, Byung Hak Ha, Yeonji Oh, Hyunah Choo, Eun Joo Song, Eunice EunKyeong Kim · 2023 · Communications Biology
- Inhibition of USP7 upregulates USP22 and activates its downstream cancer-related signaling pathways in human cancer cellsKeqiang Zhang, Ting Sun, Wendong Li, Yuming Guo, Aimin Li, Marcus Hsieh, Jinghan Wang, Jun Wu, Leonidas D. Arvanitis, Dan J. Raz · 2023 · Cell Communication and Signaling
- Deubiquitinating Enzyme: A Potential Secondary Checkpoint of Cancer ImmunityXing Huang, Xiaozhen Zhang, Jian Xu, Xun Wang, Gang Zhang, Tianyu Tang, Xiaochao Shen, Tingbo Liang, Xueli Bai · 2020 · Frontiers in Oncology
- Ubiquitination of Nonhistone Proteins in Cancer Development and TreatmentXiuzhen Zhang, Tong Meng, Shuaishuai Cui, Ling Feng, Dongwu Liu, Qiuxiang Pang, Ping Wang · 2021 · Frontiers in Oncology
- Design, synthesis and biological evaluation of 2-aminopyridine derivatives as USP7 inhibitorsXiaoming Xu, Mingchen Wang, Hailong Xu, Na Liu, Kaixian Chen, Cheng Luo, Shijie Chen, Hua Chen · 2022 · Bioorganic Chemistry
- Parallel synthesis of 2,4,5-trisubstituted thiophene-3-carbonitrile derivatives on traceless solid supportSuyoun Lee, Doohyun Lee, Kyung‐Sik Song, Kwang‐Hyeon Liu, Young‐Dae Gong, Tae‐Ho Lee · 2014 · Tetrahedron
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- Targeting USP47 enhances the efficacy of KRAS inhibitor in KRASG12C mutated non-small cell lung cancer by controlling deubiquitination of c-MycH. Y. Shin, SuA Hwang, Jeong Hyun Jeong, Sang Chul Shin, Yeonji Oh, Jin Hyeok Kim, Inah Hwang, Eunice EunKyeong Kim, Hyunah Choo, Eun Joo Song · 2025 · Pharmacological Research
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- Steuerung der intrazellulären Proteinmenge durch niedermolekulare Modulatoren des Ubiquitin‐Proteasom‐SystemsDennis L. Buckley, Craig M. Crews · 2014 · Angewandte Chemie
- Discovery of a Potent and Selective Degrader for USP7Yuan Pei, Jingfeng Fu, Yunkai Shi, Mengmeng Zhang, Guanghao Luo, Xiaomin Luo, Ning Song, Tian Mi, Yaxi Yang, Jia Xuan Li et al. · 2022 · Angewandte Chemie
- Discovery of Therapeutic Deubiquitylase Effector Molecules: Current PerspectivesBenjamin Nicholson, Suresh Kumar, Saket Agarwal, Michael J. Eddins, Jeffrey G. Marblestone, J. Wu, Matthew P. Kodrasov, James P. LaRocque, David E. Sterner, Michael R. Mattern · 2014 · SLAS DISCOVERY
- Discovery of pyrrolo[2,3-d]pyrimidin-4-one derivative YCH3124 as a potent USP7 inhibitor for cancer therapyZhen Zhuang, Yu-Ling Miao, Shanshan Song, Guang-Tong Leng, Xiaofei Zhang, Qian He, Jian Ding, Jin‐Xue He, Chunhao Yang · 2024 · European Journal of Medicinal Chemistry
- Diarylcarbonates are a new class of deubiquitinating enzyme inhibitorMarcus J. C. Long, Ann P. Lawson, Rick Baggio, Qian Yu, Lior Rozhansky, Domenico Fasci, Farid El Oualid, Eranthie Weerapana, Lizbeth Hedstrom · 2018 · Bioorganic & Medicinal Chemistry Letters
- Comprehensive analysis of the role of ubiquitin-specific peptidases in colorectal cancer: A systematic reviewEman Al-Balushi, Amina M Al Marzouqi, Shima Tavoosi, Amir Hossein Baghsheikhi, Arash Sadri, Leyla Sharifi Aliabadi, Mohammad-Mahdi Salarabedi, Syed Azizur Rahman, Nabeel Al‐Yateem, Alireza Mosavi Jarrahi et al. · 2024 · World Journal of Gastrointestinal Oncology
- Harnessing the Oxidation Susceptibility of Deubiquitinases for Inhibition with Small MoleculesShimrit Ohayon, Maya Refua, Adi Hendler‐Neumark, Amir Aharoni, Ashraf Brik · 2014 · Angewandte Chemie
- A closer look at the role of deubiquitinating enzymes in the Hypoxia Inducible Factor pathwayTekle Pauzaite, James A. Nathan · 2024 · Biochemical Society Transactions
- Therapeutic potential of targeting ubiquitin-specific proteases in colorectal cancerChern Ein Oon, Padmanabhan Anbazhagan, Chong Teik Tan · 2025 · Drug Discovery Today
- USP7 at the Crossroads of Ubiquitin Signaling, Cell Cycle, and TumorigenesisMatteo Lusardi, Federica Rapetti, Andrea Spallarossa, Marta Massone, Elena Cichero, Chiara Brullo · 2025 · Molecules
- USP7 - A novel target for controlling periodontal inflammation through modulation of macrophage polarizationYan Wang, Hailin Mu, Chang Yang, Chang Yang, Wei Dong, Jiawei Wang · 2025 · Immunology Letters
- Ubiquitin specific peptidase 47 promotes proliferation of lung squamous cell carcinomaLin Yu, Jiayu Fu, Chunjian Shen · 2022 · Genes & Genomics
- Cell-Based Covalent-Capture Deubiquitinase Assay for Inhibitor DiscoveryMegan N. Doleschal, Jenna O. Miller, Sankalp Jain, Alexey V. Zakharov, Ganesha Rai, Anton M. Simeonov, Bolormaa Baljinnyam, Zhihao Zhuang · 2024 · ACS Pharmacology & Translational Science
- Design, Synthesis, and Molecular Evaluation of S N Ar‐Reactive N ‐(6‐Fluoro‐3‐Nitropyridin‐2‐yl)Isoquinolin‐3‐Amines as Covalent USP7 Inhibitors Reveals an Unconventional Binding ModeLarissa N. Ernst, Jason Stahlecker, Finn Mier, Ricardo A. M. Serafim, Valentin R. Wydra, Benedikt Masberg, Simon Jaag, Cornelius Knappe, Michael Lämmerhofer, Thilo Stehle et al. · 2025 · Archiv der Pharmazie
- Rapid optimization of labeled ubiquitinated peptides for monitoring deubiquitinases activitiesShimrit Ohayon, Maya Refua, Ashraf Brik · 2015 · Organic & Biomolecular Chemistry
- Transcription Factors, R-Loops and Deubiquitinating Enzymes: Emerging Targets in Myelodysplastic Syndromes and Acute Myeloid LeukemiaSilvia M.L. Barabino, Elisabetta Citterio, Antonella Ellena Ronchi · 2021 · Cancers
- Targeting the Ubiquitin Proteasome System in CancerNishi Kumari, Kwok Kin Lee, Sudhakar Jha · 2018 · InTech eBooks
- Identifying Inhibitors of USP7-HDM2 Protein-Protein Interaction (PPI) by the in Silico Fragment-mapping MethodKensuke Misawa, Shin-ichiro Ozawa, Tomoki Yoshida, Izumi Nakagome, Noriyuki Yamaotsu, Shuichi Hirono · 2019 · YAKUGAKU ZASSHI
- Discovery and characterization of potent macrocycle inhibitors of ubiquitin-specific protease-7Rafael Miranda, Francesca Anson, Shannon T. Smith, Mark H. Ultsch, Connie A. Tenorio, Lionel Rougé, Brennan Farrell, Emel Adaligil, Jeffrey K. Holden, Seth F. Harris et al. · 2025 · Structure
- The roles of ubiquitination‐mediated intrinsic apoptotic signalling in cancer therapyTiantian Che, Zhenghong Lin · 2022 · Clinical and Translational Discovery
- HAUSP Stabilizes SOX2 through Deubiquitination to Maintain Self-renewal and Tumorigenic Potential of Glioma Stem CellsZhi Huang, Kui Zhai, Qiulian Wu, Xiaoguang Fang, Qian Huang, Weiwei Tao, Justin Durla Lathia, Jennifer S. Yu, Jeremy N. Rich, Shideng Bao · 2021 · bioRxiv (Cold Spring Harbor Laboratory)
- The diverse functions of ubiquitin-specific protease 47 and its role in diseasesHu Lei, Hanzhang Xu, Yingli Wu · 2025 · International Journal of Biological Macromolecules
- Recent Progress of Ubiquitin-Specific-Processing Protease 7 InhibitorsL. Chi, Hexiao Wang, F. Yu, C. Gao, H. Dai, Xi. Si, Lifang Liu, Zongyue Wang, Jun-Hui Zheng, Y. Ke et al. · 2023 · Russian Journal of Bioorganic Chemistry
- Targeting Proteasomal Degradation of Soluble, Misfolded ProteinsPierfausto Seneci · 2015 · Elsevier eBooks
- A small HDM2 antagonist peptide and a USP7 inhibitor synergistically inhibit the p53‐HDM2‐USP7 circuitSrijata Mukherjee, Gouranga Saha, Neeladri Sekhar Roy, Gitashri Naiya, Mrinal K. Ghosh, Siddhartha Roy · 2023 · Chemical Biology & Drug Design
- ob ABPP-HT*: A Precision-Engineered Activity Proteomics Pipeline for the Streamlined Discovery of Deubiquitinase InhibitorsHannah B. L. Jones, Simeon D. Draganov, Sofia Schönbauer Huamán, Peter A. C. Wing, Chuong Nguyen, Zhu Liang, Julia Dörner, Jasper Lithgow, Emma J. Murphy, Alice Beard et al. · 2025 · bioRxiv (Cold Spring Harbor Laboratory)
- Development and validation of a fluorescence polarization-based assay for USP7: From probe design to inhibitor evaluationSiji Chen, Mingchen Wang, Yasi Zeng, Xinyuan Li, Hui Zhong, Yiling Liu, Yunsu Tao, Xu Yang, Cheng Luo, Shijie Chen et al. · 2026 · European Journal of Medicinal Chemistry
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- BindingDB Entry 50002263: Sulawesins A-C, Furanosesterterpene Tetronic Acids That Inhibit USP7, from a Psammocinia sp. Marine Sponge.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50049096: Synthesis and biological evaluation of thiazole derivatives as novel USP7 inhibitors.BindingDB · 2019 · UC San Diego
- BindingDB Entry 50018466: Recent advances in the development of ubiquitin-specific-processing protease 7 (USP7) inhibitors.BindingDB · 2024 · UC San Diego
- BindingDB Entry 50012817: Discovery of USP7 small-molecule allosteric inhibitors.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50007936: Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors.BindingDB · 2021 · UC San Diego
- BindingDB Entry 50013565: Design, synthesis, biological evaluation and structure-activity relationship study of quinazolin-4(3H)-one derivatives as novel USP7 inhibitors.BindingDB · 2022 · UC San Diego
- BindingDB Entry 50017489: Discovery of Orally BioavailableBindingDB · 2023 · UC San Diego
- BindingDB Entry 50045592: Inhibiting the deubiquitinating enzymes (DUBs).BindingDB · 2016 · UC San Diego
- BindingDB Entry 50043109: Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitor.BindingDB · 2014 · UC San Diego
- BindingDB Entry 50022200: Discovery of pyrrolo[2,3-d]pyrimidin-4-one derivative YCH3124 as a potent USP7 inhibitor for cancer therapy.BindingDB · 2025 · UC San Diego
- BindingDB Entry 50021261: Recent advances in the development of deubiquitinases inhibitors as antitumor agents.BindingDB · 2025 · UC San Diego
- BindingDB Entry 50001159: Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.BindingDB · 2020 · UC San Diego
- BindingDB Entry 50018635: Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.BindingDB · 2024 · UC San Diego