Gene and Protein Information
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
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
Ligand Sp. Action Value Parameter Reference C1-27 Hs Inhibition 6.9 pIC50 3 ⤷ pIC50 6.9 (IC50 1.3x10-7 M) [3] compound 25 [PMID: 32105470] Hs Inhibition 6.6 pIC50 3 ⤷ pIC50 6.6 (IC50 2.5x10-7 M) [3] Description: Enzyme inhibition in a biochemical assay, utilising the substrate S-(4-nitrophenacyl)glutathione (4-NPG) and recombinant GSTO1-1.

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
GSTO1-1 deglutathionylates cysteine 253 in NIMA related kinase 7 (NEK7) to promote NLRP3 activation. Species:  Human Tissue:  References:  1

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].