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Target not currently curated in GtoImmuPdb
Target id: 2428
Nomenclature: ubiquitin specific peptidase 1
Family: C19: Ubiquitin-specific protease
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 785 | 1p31.3 | USP1 | ubiquitin specific peptidase 1 | |
Mouse | - | 784 | 4 C6 | Usp1 | ubiquitin specific peptidase 1 | |
Rat | - | 784 | 5q33 | Usp1 | ubiquitin specific peptidase 1 |
Previous and Unofficial Names ![]() |
deubiquitinating enzyme 1 | ubiquitin carboxyl-terminal hydrolase 1 | ubiquitin specific protease 1 | ubiquitin thioesterase 1 | ubiquitin thiolesterase 1 |
Database Links ![]() |
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Specialist databases | |
MEROPS | C19.019 (Hs) |
Other databases | |
Alphafold | O94782 (Hs), Q8BJQ2 (Mm), Q569C3 (Rn) |
BRENDA | 3.4.19.12 |
ChEMBL Target | CHEMBL1795087 (Hs) |
Ensembl Gene | ENSG00000162607 (Hs), ENSMUSG00000028560 (Mm), ENSRNOG00000007890 (Rn) |
Entrez Gene | 7398 (Hs), 230484 (Mm), 313387 (Rn) |
Human Protein Atlas | ENSG00000162607 (Hs) |
KEGG Enzyme | 3.4.19.12 |
KEGG Gene | hsa:7398 (Hs), mmu:230484 (Mm), rno:313387 (Rn) |
OMIM | 603478 (Hs) |
Pharos | O94782 (Hs) |
RefSeq Nucleotide | NM_001017416 (Hs), NM_003368 (Hs), NM_001017415 (Hs), NM_146144 (Mm), NM_001015015 (Rn) |
RefSeq Protein | NP_003359 (Hs), NP_001017416 (Hs), NP_001017415 (Hs), NP_666256 (Mm), NP_001015015 (Rn) |
UniProtKB | O94782 (Hs), Q8BJQ2 (Mm), Q569C3 (Rn) |
Wikipedia | USP1 (Hs) |
Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
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General Comments |
USP1 has been shown to promote the survival of cancer cells by facilitating DNA repair. USP1 is an active oncology drug target. USP1 inhibition is proposed as an alternative to PARP inhibition, in particular for cancers that develop resistance to PARP inhibitors or are resistant to it. The experimental inhibitor ML323 has been used to confirm potential utility of USP1 inhibition in cancer models [2-3,7-8]. KSQ Therapeutics' KSQ-4279 is in early stage clinical development. |
1. Brenneman JB, Krall EB, Schlabach M, Wylie AA. (2020) Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (usp1) inhibitors. Patent number: WO2020132269A1. Assignee: KSQ Therapeutics, Inc.. Priority date: 20/12/2018. Publication date: 25/06/2020.
2. Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A et al.. (2014) Synthesis and Structure-Activity Relationship Studies of N-Benzyl-2-phenylpyrimidin-4-amine Derivatives as Potent USP1/UAF1 Deubiquitinase Inhibitors with Anticancer Activity against Nonsmall Cell Lung Cancer. J Med Chem, 57 (19): 8099-110. [PMID:25229643]
3. Ma A, Tang M, Zhang L, Wang B, Yang Z, Liu Y, Xu G, Wu L, Jing T, Xu X et al.. (2019) USP1 inhibition destabilizes KPNA2 and suppresses breast cancer metastasis. Oncogene, 38 (13): 2405-2419. [PMID:30531833]
4. Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD et al.. (2013) Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther, 12 (12): 2651-62. [PMID:24130053]
5. Tan L, Shan H, Han C, Zhang Z, Shen J, Zhang X, Xiang H, Lu K, Qi C, Li Y et al.. (2022) Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem, 65 (20): 13645-13659. [PMID:36221183]
6. Throner S, Jönsson D. (2024) Purine derivatives as anticancer agents. Patent number: US20240059689A1. Assignee: Medivir AB, Tango Therapeutics Inc. Priority date: 15/09/2023. Publication date: 22/02/2024.
7. Xu X, Li S, Cui X, Han K, Wang J, Hou X, Cui L, He S, Xiao J, Yang Y. (2019) Inhibition of Ubiquitin Specific Protease 1 Sensitizes Colorectal Cancer Cells to DNA-Damaging Chemotherapeutics. Front Oncol, 9: 1406. [PMID:31921663]
8. Zhao Y, Xue C, Xie Z, Ouyang X, Li L. (2020) Comprehensive analysis of ubiquitin-specific protease 1 reveals its importance in hepatocellular carcinoma. Cell Prolif, 53 (10): e12908. [PMID:32951278]
C19: Ubiquitin-specific protease: ubiquitin specific peptidase 1. Last modified on 28/03/2024. Accessed on 08/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2428.