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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  2. Covalent Small Molecule Immunomodulators Targeting the Protease Active Site
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  3. Deubiquitylating enzymes as cancer stem cell therapeutics
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  4. The role of deubiquitinating enzymes in gastric cancer (Review)
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  8. USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4
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  9. Assay Systems for Profiling Deubiquitinating Activity
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  10. Role of Ubiquitin-Specific Peptidase 47 in Cancers and Other Diseases
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  11. Diaryl Sulfoxides from Aryl Benzyl Sulfoxides: A Single Palladium‐Catalyzed Triple Relay Process
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  12. Ubiquitin-Specific Proteases as Druggable Targets.
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  13. USP7 substrates identified by proteomics analysis reveal the specificity of USP7
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  14. An Integrated in silico Approach and in vitro Study for the Discovery of Small‐Molecule USP7 Inhibitors as Potential Cancer Therapies
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  15. Ubiquitin specific peptidases and prostate cancer
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  16. Structural basis for the bi-specificity of USP25 and USP28 inhibitors
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  17. USP7 stabilizes EZH2 and enhances cancer malignant progression.
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  18. Inhibition of the deubiquitinating enzyme USP47 as a novel targeted therapy for hematologic malignancies expressing mutant EZH2
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  21. Therapeutic targeting of ubiquitin-specific protease 7 (USP7): Mechanistic insights, dysregulation, and advances in drug discovery
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  23. USP47 deubiquitylates Groucho/TLE to promote Wnt–β-catenin signaling
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  24. The key vulnerabilities and therapeutic opportunities in the USP7-p53/MDM2 axis in cancer
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  25. Ubiquitin-specific protease 12 interacting partners Uaf-1 and WDR20 are potential therapeutic targets in prostate cancer
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  26. Discovery of USP7 small-molecule allosteric inhibitors
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  28. Natural Agents as Novel Potential Source of Proteasome Inhibitors with Anti-Tumor Activity: Focus on Multiple Myeloma
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  29. Structural and functional characterization of USP47 reveals a hot spot for inhibitor design
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  30. Inhibition of USP7 upregulates USP22 and activates its downstream cancer-related signaling pathways in human cancer cells
    Keqiang 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
  31. Deubiquitinating Enzyme: A Potential Secondary Checkpoint of Cancer Immunity
    Xing Huang, Xiaozhen Zhang, Jian Xu, Xun Wang, Gang Zhang, Tianyu Tang, Xiaochao Shen, Tingbo Liang, Xueli Bai · 2020 · Frontiers in Oncology
  32. Ubiquitination of Nonhistone Proteins in Cancer Development and Treatment
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  33. Design, synthesis and biological evaluation of 2-aminopyridine derivatives as USP7 inhibitors
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  35. Mechanisms of mitophagy: putting the powerhouse into the doghouse
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  36. Targeting USP47 enhances the efficacy of KRAS inhibitor in KRASG12C mutated non-small cell lung cancer by controlling deubiquitination of c-Myc
    H. 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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  38. Steuerung der intrazellulären Proteinmenge durch niedermolekulare Modulatoren des Ubiquitin‐Proteasom‐Systems
    Dennis L. Buckley, Craig M. Crews · 2014 · Angewandte Chemie
  39. Discovery of a Potent and Selective Degrader for USP7
    Yuan 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
  40. Discovery of Therapeutic Deubiquitylase Effector Molecules: Current Perspectives
    Benjamin 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
  41. Discovery of pyrrolo[2,3-d]pyrimidin-4-one derivative YCH3124 as a potent USP7 inhibitor for cancer therapy
    Zhen 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
  42. Diarylcarbonates are a new class of deubiquitinating enzyme inhibitor
    Marcus 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
  43. Comprehensive analysis of the role of ubiquitin-specific peptidases in colorectal cancer: A systematic review
    Eman 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
  44. Harnessing the Oxidation Susceptibility of Deubiquitinases for Inhibition with Small Molecules
    Shimrit Ohayon, Maya Refua, Adi Hendler‐Neumark, Amir Aharoni, Ashraf Brik · 2014 · Angewandte Chemie
  45. A closer look at the role of deubiquitinating enzymes in the Hypoxia Inducible Factor pathway
    Tekle Pauzaite, James A. Nathan · 2024 · Biochemical Society Transactions
  46. Therapeutic potential of targeting ubiquitin-specific proteases in colorectal cancer
    Chern Ein Oon, Padmanabhan Anbazhagan, Chong Teik Tan · 2025 · Drug Discovery Today
  47. USP7 at the Crossroads of Ubiquitin Signaling, Cell Cycle, and Tumorigenesis
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  48. USP7 - A novel target for controlling periodontal inflammation through modulation of macrophage polarization
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  49. Ubiquitin specific peptidase 47 promotes proliferation of lung squamous cell carcinoma
    Lin Yu, Jiayu Fu, Chunjian Shen · 2022 · Genes & Genomics
  50. Cell-Based Covalent-Capture Deubiquitinase Assay for Inhibitor Discovery
    Megan N. Doleschal, Jenna O. Miller, Sankalp Jain, Alexey V. Zakharov, Ganesha Rai, Anton M. Simeonov, Bolormaa Baljinnyam, Zhihao Zhuang · 2024 · ACS Pharmacology & Translational Science
  51. 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 Mode
    Larissa 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
  52. Rapid optimization of labeled ubiquitinated peptides for monitoring deubiquitinases activities
    Shimrit Ohayon, Maya Refua, Ashraf Brik · 2015 · Organic & Biomolecular Chemistry
  53. Transcription Factors, R-Loops and Deubiquitinating Enzymes: Emerging Targets in Myelodysplastic Syndromes and Acute Myeloid Leukemia
    Silvia M.L. Barabino, Elisabetta Citterio, Antonella Ellena Ronchi · 2021 · Cancers
  54. Targeting the Ubiquitin Proteasome System in Cancer
    Nishi Kumari, Kwok Kin Lee, Sudhakar Jha · 2018 · InTech eBooks
  55. Identifying Inhibitors of USP7-HDM2 Protein-Protein Interaction (PPI) by the in Silico Fragment-mapping Method
    Kensuke Misawa, Shin-ichiro Ozawa, Tomoki Yoshida, Izumi Nakagome, Noriyuki Yamaotsu, Shuichi Hirono · 2019 · YAKUGAKU ZASSHI
  56. Discovery and characterization of potent macrocycle inhibitors of ubiquitin-specific protease-7
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  57. The roles of ubiquitination‐mediated intrinsic apoptotic signalling in cancer therapy
    Tiantian Che, Zhenghong Lin · 2022 · Clinical and Translational Discovery
  58. HAUSP Stabilizes SOX2 through Deubiquitination to Maintain Self-renewal and Tumorigenic Potential of Glioma Stem Cells
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  59. The diverse functions of ubiquitin-specific protease 47 and its role in diseases
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  60. Recent Progress of Ubiquitin-Specific-Processing Protease 7 Inhibitors
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  61. Targeting Proteasomal Degradation of Soluble, Misfolded Proteins
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  62. A small HDM2 antagonist peptide and a USP7 inhibitor synergistically inhibit the p53‐HDM2‐USP7 circuit
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  63. ob ABPP-HT*: A Precision-Engineered Activity Proteomics Pipeline for the Streamlined Discovery of Deubiquitinase Inhibitors
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  64. Development and validation of a fluorescence polarization-based assay for USP7: From probe design to inhibitor evaluation
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  67. USP7 as part of non-canonical PRC1.1 is a druggable target in leukemia
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  68. USP7 Inhibition Induces Apoptosis in Glioblastoma by Stabilizing ARF4
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  69. Structural Insight into the Mechanisms of Activation and Substrate Specificity of Human Deubiquitinating Enzyme USP7
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  70. Peer Review #3 of "Ubiquitin specific peptidases and prostate cancer (v0.1)"
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  78. Additional file 3 of USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4
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  79. Additional file 1 of USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4
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  80. Additional file 2 of USP7 inhibition induces apoptosis in glioblastoma by enhancing ubiquitination of ARF4
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  83. Virtual Screening–Guided Identification of Candidate USP7-Inhibitory Scaffolds Exhibiting Antiproliferative Activity
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  85. Activity-based proteomics discovery of deubiquitinating enzyme inhibitors with immunomodulatory activity
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  86. BindingDB Entry 50002263: Sulawesins A-C, Furanosesterterpene Tetronic Acids That Inhibit USP7, from a Psammocinia sp. Marine Sponge.
    BindingDB · 2020 · UC San Diego
  87. BindingDB Entry 50049096: Synthesis and biological evaluation of thiazole derivatives as novel USP7 inhibitors.
    BindingDB · 2019 · UC San Diego
  88. BindingDB Entry 50018466: Recent advances in the development of ubiquitin-specific-processing protease 7 (USP7) inhibitors.
    BindingDB · 2024 · UC San Diego
  89. BindingDB Entry 50012817: Discovery of USP7 small-molecule allosteric inhibitors.
    BindingDB · 2022 · UC San Diego
  90. BindingDB Entry 50007936: Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors.
    BindingDB · 2021 · UC San Diego
  91. 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
  92. BindingDB Entry 50017489: Discovery of Orally Bioavailable
    BindingDB · 2023 · UC San Diego
  93. BindingDB Entry 50045592: Inhibiting the deubiquitinating enzymes (DUBs).
    BindingDB · 2016 · UC San Diego
  94. BindingDB Entry 50043109: Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitor.
    BindingDB · 2014 · UC San Diego
  95. 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
  96. BindingDB Entry 50021261: Recent advances in the development of deubiquitinases inhibitors as antitumor agents.
    BindingDB · 2025 · UC San Diego
  97. 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
  98. BindingDB Entry 50018635: Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.
    BindingDB · 2024 · UC San Diego