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target has curated data in GtoImmuPdb
Target id: 3110
Nomenclature: glutathione S-transferase omega 1
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 241 | 10q25.1 | GSTO1 | glutathione S-transferase omega 1 | |
Mouse | - | 240 | 19 D1 | Gsto1 | glutathione S-transferase omega 1 | |
Rat | - | 241 | 1q54 | Gsto1 | glutathione S-transferase omega 1 | |
Gene and Protein Information Comments | ||||||
Three transcript variants encoding different isoforms are reported for the human gene. |
Previous and Unofficial Names ![]() |
GSTO 1-1 | GSTO1-1 | GSTTLp28 |
Database Links ![]() |
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Alphafold | P78417 (Hs), O09131 (Mm) |
ChEMBL Target | CHEMBL3174 (Hs), CHEMBL4523122 (Mm) |
Ensembl Gene | ENSG00000148834 (Hs), ENSMUSG00000025068 (Mm), ENSRNOG00000028746 (Rn) |
Entrez Gene | 9446 (Hs), 14873 (Mm), 114846 (Rn) |
Human Protein Atlas | ENSG00000148834 (Hs) |
KEGG Gene | hsa:9446 (Hs), mmu:14873 (Mm), rno:114846 (Rn) |
OMIM | 605482 (Hs) |
Pharos | P78417 (Hs) |
RefSeq Nucleotide | NM_004832 (Hs), NM_010362 (Mm), NM_001007602 (Rn) |
RefSeq Protein | NP_004823 (Hs), NP_034492 (Mm), NP_001007603 (Rn) |
UniProtKB | P78417 (Hs), O09131 (Mm) |
Wikipedia | GSTO1 (Hs) |
Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immunopharmacology Comments |
GSTO1-1 is reported to act as a NLRP3 inflammasome regulator, via deglutathionylation of NIMA related kinase 7 (NEK7; a NLRP3 inflammasome component [1]). GSTO1-1 inhibition suppresses lipopolysaccharide (LPS)-induced production of proinflammatory cytokines (via TLR4) such as IL-1β, IL-6 and TNF. Thus, GSTO1-1 has potential as a drug target to limit NLRP3-mediated inflammation, and GSTO1-1 inhibitors are being actively pursued for the treatment of inflammatory conditions and pathologies that result from NLRP3 inflammasome activation. To date (March 2020) no GSTO1-1 inhibitors have cleared preclinical development. |
Physiological Functions ![]() |
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General Comments |
Glutathione transferase omega-1 (GSTO1-1) is an omega class cytosolic glutathione transferase (GST). It also exhibits dehydroascorbate reductase, monomethylarsonate reductase, and thioltransferase activities. GSTO1-1 is the only GST to display S-(phenacyl)glutathione reductase and deglutathionylase activities [2]. |
1. Hughes MM, Hooftman A, Angiari S, Tummala P, Zaslona Z, Runtsch MC, McGettrick AF, Sutton CE, Diskin C, Rooke M et al.. (2019) Glutathione Transferase Omega-1 Regulates NLRP3 Inflammasome Activation through NEK7 Deglutathionylation. Cell Rep, 29 (1): 151-161.e5. [PMID:31577945]
2. Xie Y, Dahlin JL, Oakley AJ, Casarotto MG, Board PG, Baell JB. (2018) Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. J Med Chem, 61 (17): 7448-7470. [PMID:29652143]
3. Xie Y, Tummala P, Oakley AJ, Deora GS, Nakano Y, Rooke M, Cuellar ME, Strasser JM, Dahlin JL, Walters MA et al.. (2020) Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors. J Med Chem, 63 (6): 2894-2914. [PMID:32105470]
2.5.1.18 Glutathione transferases: glutathione S-transferase omega 1. Last modified on 17/03/2020. Accessed on 10/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3110.