MGST1

gene
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Also known as MGST-IPMAN

Summary

MGST1 (microsomal glutathione S-transferase 1, HGNC:7061) is a protein-coding gene on chromosome 12p12.3, encoding Microsomal glutathione S-transferase 1 (P10620). Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.

The MAPEG (Membrane Associated Proteins in Eicosanoid and Glutathione metabolism) family consists of six human proteins, two of which are involved in the production of leukotrienes and prostaglandin E, important mediators of inflammation. Other family members, demonstrating glutathione S-transferase and peroxidase activities, are involved in cellular defense against toxic, carcinogenic, and pharmacologically active electrophilic compounds. This gene encodes a protein that catalyzes the conjugation of glutathione to electrophiles and the reduction of lipid hydroperoxides. This protein is localized to the endoplasmic reticulum and outer mitochondrial membrane where it is thought to protect these membranes from oxidative stress. Several transcript variants, some non-protein coding and some protein coding, have been found for this gene.

Source: NCBI Gene 4257 — RefSeq curated summary.

At a glance

  • GWAS associations: 10
  • Clinical variants (ClinVar): 43 total
  • Druggable target: yes
  • MANE Select transcript: NM_020300

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:7061
Approved symbolMGST1
Namemicrosomal glutathione S-transferase 1
Location12p12.3
Locus typegene with protein product
StatusApproved
AliasesMGST-I, PMAN
Ensembl geneENSG00000008394
Ensembl biotypeprotein_coding
OMIM138330
Entrez4257

Gene structure

Transcript identifiers

Ensembl transcripts: 50 — 41 protein_coding, 6 protein_coding_CDS_not_defined, 2 retained_intron, 1 TEC

ENST00000010404, ENST00000359720, ENST00000396207, ENST00000396209, ENST00000396210, ENST00000534835, ENST00000535309, ENST00000535624, ENST00000536371, ENST00000537878, ENST00000538857, ENST00000538885, ENST00000539036, ENST00000539708, ENST00000540056, ENST00000540126, ENST00000542256, ENST00000543076, ENST00000624056, ENST00000902095, ENST00000902096, ENST00000902097, ENST00000902098, ENST00000902099, ENST00000902100, ENST00000902101, ENST00000902102, ENST00000902103, ENST00000902104, ENST00000902105, ENST00000902106, ENST00000902107, ENST00000902108, ENST00000902109, ENST00000902110, ENST00000902111, ENST00000902112, ENST00000902113, ENST00000902114, ENST00000902115, ENST00000902116, ENST00000921235, ENST00000921236, ENST00000921237, ENST00000921238, ENST00000921239, ENST00000921240, ENST00000921241, ENST00000960433, ENST00000960434

RefSeq mRNA: 24 — MANE Select: NM_020300 NM_001260511, NM_001260512, NM_001267598, NM_001414355, NM_001414356, NM_001414357, NM_001414358, NM_001414359, NM_001414361, NM_001414362, NM_001414363, NM_001414365, NM_001414367, NM_001414368, NM_001414369, NM_001414370, NM_001414371, NM_001414372, NM_001414373, NM_001414374, NM_020300, NM_145764, NM_145791, NM_145792

CCDS: CCDS58209, CCDS8677

Canonical transcript exons

ENST00000396210 — 4 exons

ExonStartEnd
ENSE000015242441636379516364410
ENSE000015242451634764516347710
ENSE000035283771635423116354378
ENSE000036696481635760516357699

Expression profiles

Bgee: expression breadth ubiquitous, 258 present calls, max score 99.86.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 302.1066 / max 5232.6914, expressed in 1686 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter IDTPM avgSamples expressed
124524247.82021682
12452535.50511622
1245227.93241098
1245237.54101330
1245210.8104287
1245290.5085230
1245310.4465216
1245270.3618155
1245300.3036134
1245280.2852121

Top tissues by expression

259 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
right adrenal glandUBERON:000123399.86gold quality
right adrenal gland cortexUBERON:003582799.86gold quality
left adrenal glandUBERON:000123499.83gold quality
adrenal cortexUBERON:000123599.81gold quality
left adrenal gland cortexUBERON:003582599.80gold quality
right lobe of liverUBERON:000111499.75gold quality
ileal mucosaUBERON:000033199.74gold quality
kidney epitheliumUBERON:000481999.72gold quality
adipose tissueUBERON:000101399.65gold quality
adrenal glandUBERON:000236999.65gold quality
adipose tissue of abdominal regionUBERON:000780899.61gold quality
liverUBERON:000210799.60gold quality
omental fat padUBERON:001041499.60gold quality
peritoneumUBERON:000235899.58gold quality
subcutaneous adipose tissueUBERON:000219099.57gold quality
pericardiumUBERON:000240799.46gold quality
upper leg skinUBERON:000426299.45gold quality
right lobe of thyroid glandUBERON:000111999.41gold quality
left lobe of thyroid glandUBERON:000112099.36gold quality
adrenal tissueUBERON:001830399.35gold quality
upper arm skinUBERON:000426399.32gold quality
nasal cavity epitheliumUBERON:000538499.30gold quality
mucosa of transverse colonUBERON:000499199.27gold quality
thyroid glandUBERON:000204699.22gold quality
deciduaUBERON:000245099.20gold quality
stromal cell of endometriumCL:000225599.19gold quality
colonic mucosaUBERON:000031799.15gold quality
thoracic mammary glandUBERON:000520099.13gold quality
mucosa of sigmoid colonUBERON:000499399.09gold quality
mammary glandUBERON:000191199.07gold quality

Single-cell (SCXA)

Detected in 36 experiment(s), a significant marker in 35.

ExperimentMarker?Max mean expression
E-MTAB-10553yes3501.15
E-HCAD-9yes3460.61
E-MTAB-8495yes3414.31
E-MTAB-6308yes3213.18
E-HCAD-15yes1663.43
E-MTAB-6701yes1515.55
E-HCAD-1yes1165.50
E-HCAD-24yes1163.44
E-CURD-126yes1036.50
E-GEOD-84465yes856.09
E-MTAB-5061yes850.67
E-MTAB-8884yes688.86
E-CURD-46yes580.08
E-GEOD-81547yes530.89
E-MTAB-11121yes498.04

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYC, NFE2L2, SP1

miRNA regulators (miRDB)

24 targeting MGST1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-808799.9069.551351
HSA-MIR-449599.8272.083080
HSA-MIR-7161-5P99.6868.921592
HSA-MIR-548U99.6567.781463
HSA-MIR-10393-5P99.6568.011368
HSA-MIR-513A-3P99.3970.633620
HSA-MIR-513C-3P99.3970.633620
HSA-MIR-664A-3P99.2271.082696
HSA-MIR-429199.2068.882969
HSA-MIR-452899.1869.771936
HSA-MIR-807799.1766.67862
HSA-MIR-3606-3P99.1169.843254
HSA-MIR-92299.0267.231838
HSA-MIR-3619-5P99.0068.872308
HSA-MIR-125798.9768.021133
HSA-MIR-607498.8969.642187
HSA-MIR-427298.7668.741810
HSA-MIR-76198.7168.072051
HSA-MIR-214-3P98.7168.122128
HSA-MIR-64098.4466.93644
HSA-MIR-10397-3P97.7865.70601
HSA-MIR-376A-5P97.7065.61863
HSA-MIR-6818-5P97.5067.101167

Literature-anchored findings (GeneRIF, showing 16)

  • As an addition to the high-density SNP (single-nucleotide polymorphism) maps of 12 glutathione S-transferase and related genes reported earlier, a SNP map of the microsomal glutathione S-transferase 1 (MGST1) gene is provided. (PMID:11587073)
  • The results indicate that Sp1 is the protein mediating the basal transcription of MGST1 (PMID:12818425)
  • Genes encoding KU70, MGST1 and BIK show age-related mRNA expression levels in hematopoietic stem cells. (PMID:17714764)
  • MGST1 protects cells (and mitochondria) by both conjugation and glutathione peroxidase functions. A new protective mechanism against cisplatin is also indicated (PMID:20727966)
  • The results suggest that MGST1 gene polymorphisms as one of environment gene may contribute to colorectal cancer risk in younger ages. (PMID:23314968)
  • Differential expression of SOD2, ALDH1A1, and MGST1 genes in the anterior lens capsules of patients with pseudoexfoliation syndrome suggest that diseased tissue appears to respond to the previously reported oxidative stress. (PMID:23805041)
  • possibly marked variations in NB mitochondrial homeostasis, they also imply that the results of these earlier studies using NB cells are not transferable to other tumor and cell types that express MGST1 at high concentrations. (PMID:24486338)
  • This study provides the most comprehensive evaluation of inflammation-related germline variation in relation to risk of BE/OA and suggests that variants in MGST1 influence disease susceptibility. (PMID:27486097)
  • The MSGT1 displays a preexisting dynamic equilibrium between high- and low-activity forms. (PMID:28558199)
  • High MGST1 expression is associated with Bendamustine-resistance in Mantle Cell Lymphoma. (PMID:29695404)
  • Significant association for germline variations only in the COX pathway (specifically in the antioxidant microsomal glutathione S-transferase 1 [MGST1] gene), with risk for Barrett’s esophagus and the combined outcome of Barrett’s esophagus and esophageal adenocarcinoma was found. (PMID:29713984)
  • MGST1 plays an important role in lung adenocarcinoma (LUAD)tumorigenesis and might serve as a potential prognostic factor and therapeutic target in LUAD. (PMID:31707341)
  • MGST1 is a redox-sensitive repressor of ferroptosis in pancreatic cancer cells. (PMID:33539732)
  • MiR-379-5p targets microsomal glutathione transferase 1 (MGST1) to regulate human glioma in cell proliferation, migration and invasion and epithelial-mesenchymal transition (EMT). (PMID:34171541)
  • Microsomal glutathione S-transferase 1 targets the autophagy signaling pathway to suppress ferroptosis in gastric carcinoma cells. (PMID:37161854)
  • A role for microsomal glutathione transferase 1 in melanin biosynthesis and melanoma progression. (PMID:37321450)

Cross-species orthologs

7 orthologs

OrganismSymbolGene ID
danio_reriomgst1.2ENSDARG00000022165
danio_reriomgst1.1ENSDARG00000032618
mus_musculusMgst1ENSMUSG00000008540
rattus_norvegicusMgst1ENSRNOG00000007743
drosophila_melanogasterMgstlFBGN0025814
drosophila_melanogasterCG33177FBGN0053177
drosophila_melanogasterCG33178FBGN0053178

Paralogs (1): PTGES (ENSG00000148344)

Protein

Protein identifiers

Microsomal glutathione S-transferase 1P10620 (reviewed: P10620)

Alternative names: Microsomal GST-I

All UniProt accessions (6): P10620, F5GX73, F5H613, F5H6X2, F5H760, F5H7F6

UniProt curated annotations — full annotation on UniProt →

Function. Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.

Subunit / interactions. Homotrimer; The trimer binds only one molecule of glutathione.

Subcellular location. Endoplasmic reticulum membrane. Mitochondrion outer membrane.

Tissue specificity. Highly expressed in liver.

Similarity. Belongs to the MAPEG family.

Isoforms (2)

UniProt IDNamesCanonical?
P10620-11yes
P10620-22

RefSeq proteins (24): NP_001247440, NP_001247441, NP_001254527, NP_001401284, NP_001401285, NP_001401286, NP_001401287, NP_001401288, NP_001401290, NP_001401291, NP_001401292, NP_001401294, NP_001401296, NP_001401297, NP_001401298, NP_001401299, NP_001401300, NP_001401301, NP_001401302, NP_001401303, NP_064696, NP_665707, NP_665734, NP_665735 (=MANE)

Domains & families (InterPro)

IDNameType
IPR001129Membr-assoc_MAPEGFamily
IPR023352MAPEG-like_dom_sfHomologous_superfamily
IPR040162MGST1-likeFamily

Pfam: PF01124

Catalyzed reactions (Rhea), 1 shown:

  • RX + glutathione = an S-substituted glutathione + a halide anion + H(+) (RHEA:16437)

UniProt features (20 total): binding site 6, topological domain 5, transmembrane region 4, modified residue 3, chain 1, splice variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P10620-F178.650.07

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (6): 38; 73; 74; 76; 81; 121

Post-translational modifications (3): 42, 55, 60

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

IDPathway
R-HSA-156590Glutathione conjugation
R-HSA-5423646Aflatoxin activation and detoxification
R-HSA-6798695Neutrophil degranulation
R-HSA-1430728Metabolism
R-HSA-156580Phase II - Conjugation of compounds
R-HSA-168249Innate Immune System
R-HSA-168256Immune System
R-HSA-211859Biological oxidations

MSigDB gene sets: 282 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_UP, REACTOME_BIOLOGICAL_OXIDATIONS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOCC_VACUOLAR_MEMBRANE, GOCC_SECRETORY_GRANULE, MODULE_151, GOBP_MODIFIED_AMINO_ACID_TRANSPORT, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOMF_GLUTATHIONE_TRANSFERASE_ACTIVITY, GOLDRATH_ANTIGEN_RESPONSE, HERNANDEZ_MITOTIC_ARREST_BY_DOCETAXEL_2_UP, WEI_MYCN_TARGETS_WITH_E_BOX, SCHUHMACHER_MYC_TARGETS_UP, GOBP_CELLULAR_RESPONSE_TO_TOXIC_SUBSTANCE

GO Biological Process (3): glutathione transport (GO:0034635), cellular response to lipid hydroperoxide (GO:0071449), cellular oxidant detoxification (GO:0098869)

GO Molecular Function (4): glutathione transferase activity (GO:0004364), glutathione peroxidase activity (GO:0004602), protein binding (GO:0005515), transferase activity (GO:0016740)

GO Cellular Component (8): mitochondrion (GO:0005739), mitochondrial outer membrane (GO:0005741), peroxisomal membrane (GO:0005778), endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), plasma membrane (GO:0005886), membrane (GO:0016020), azurophil granule membrane (GO:0035577)

Reactome top-level categories

Rollup of top-5 pathways:

CategoryPathways
Biological oxidations2
Phase II - Conjugation of compounds1
Innate Immune System1
Immune System1
Metabolism1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cytoplasm2
intracellular membrane-bounded organelle2
tripeptide transport1
modified amino acid transport1
sulfur compound transport1
response to lipid hydroperoxide1
cellular response to lipid1
cellular response to hydroperoxide1
cellular detoxification1
transferase activity, transferring alkyl or aryl (other than methyl) groups1
peroxidase activity1
binding1
catalytic activity1
mitochondrial membrane1
organelle outer membrane1
peroxisome1
microbody membrane1
endomembrane system1
organelle membrane1
nuclear outer membrane-endoplasmic reticulum membrane network1
endoplasmic reticulum subcompartment1
membrane1
cell periphery1
cellular anatomical structure1
lysosomal membrane1
secretory granule membrane1
azurophil granule1

Protein interactions and networks

STRING

1220 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
MGST1MGST2Q99735968
MGST1MGST3O14880948
MGST1LTC4SQ16873916
MGST1ALOX5APP20292894
MGST1HPGDSO60760759
MGST1GSTA3Q16772663
MGST1SLCO6A1Q86UG4646
MGST1GSTO1P78417589
MGST1GSTK1Q9Y2Q3564
MGST1GSTM2P28161532
MGST1GSTP1P09211531
MGST1ALOX5P09917515
MGST1GSTA1P08263504
MGST1GSTT2BP0CG30497
MGST1PPIFP30405494

IntAct

79 interactions, top by confidence:

ABTypeScore
RAF1CALUpsi-mi:“MI:0914”(association)0.640
VIPMGST1psi-mi:“MI:0915”(physical association)0.560
FZD7MGST1psi-mi:“MI:0915”(physical association)0.560
MGST1SIGLEC12psi-mi:“MI:0915”(physical association)0.560
EGFMGST1psi-mi:“MI:0915”(physical association)0.560
TNFRSF10CMGST1psi-mi:“MI:0915”(physical association)0.560
MGST1FXYD3psi-mi:“MI:0915”(physical association)0.560
ARMC6SLC27A2psi-mi:“MI:0914”(association)0.530
ANKHFAM234Bpsi-mi:“MI:0914”(association)0.530
ERBB2NDUFA4psi-mi:“MI:0914”(association)0.530
NELFBMGST1psi-mi:“MI:0915”(physical association)0.520
RAB11ALANCL1psi-mi:“MI:2364”(proximity)0.420
ESYT2psi-mi:“MI:0914”(association)0.350
E5ESYT2psi-mi:“MI:0914”(association)0.350
HAX1psi-mi:“MI:0914”(association)0.350
Prdm16ESYT2psi-mi:“MI:0914”(association)0.350
MecomESYT2psi-mi:“MI:0914”(association)0.350
LRRK2psi-mi:“MI:0914”(association)0.350
NMES1COX7A2Lpsi-mi:“MI:0914”(association)0.350
CHCHD10ACSL4psi-mi:“MI:0914”(association)0.350
COQ9ACOT7psi-mi:“MI:0914”(association)0.350
FAM136AALDH1L1psi-mi:“MI:0914”(association)0.350
NDUFA4NDUFS8psi-mi:“MI:0914”(association)0.350

BioGRID (164): LTC4S (Two-hybrid), MGST1 (Affinity Capture-MS), MGST1 (Proximity Label-MS), MGST1 (Affinity Capture-MS), MGST1 (Affinity Capture-MS), MGST1 (Affinity Capture-RNA), MGST1 (Affinity Capture-MS), MGST1 (Affinity Capture-MS), MGST1 (Proximity Label-MS), MGST1 (Affinity Capture-MS), MGST1 (Proximity Label-MS), MGST1 (Affinity Capture-MS), MGST1 (Affinity Capture-MS), MGST1 (Proximity Label-MS), MGST1 (Co-fractionation)

ESM2 similar proteins: A0A2I1C3V3, A0SYQ0, A1L2F6, A2RST1, A4DA06, A6XA80, A8X8R3, J7FIJ6, O14684, O14880, O74507, O94511, P08011, P0DN89, P10620, P64515, P64516, P70245, P73795, P79382, Q15125, Q16873, Q17428, Q28GF8, Q296J9, Q2KJG4, Q2NKS0, Q3T100, Q41745, Q54GA9, Q57ZC7, Q5R9A6, Q60490, Q60860, Q64L89, Q6GNM0, Q6GPW4, Q6PWL6, Q8HZJ2, Q91VS7

Diamond homologs: A0SYQ0, O14684, P08011, P10620, P79382, Q64L89, Q6PWL6, Q8HZJ2, Q91VS7, Q95L14, Q9JHF3, Q9JM51

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 85 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

GO biological processes:

GO termPartnersFoldFDR
positive regulation of MAPK cascade78.2×9e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

43 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance24
Likely benign6
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1778 predictions. Top by Δscore:

VariantEffectΔscore
12:16560408:CTTA:Cdonor_loss1.0000
12:16560409:TTAC:Tdonor_loss1.0000
12:16560410:TA:Tdonor_loss1.0000
12:16560411:A:Cdonor_loss1.0000
12:16560412:CCT:Cdonor_gain1.0000
12:16560535:GAGCC:Gacceptor_loss1.0000
12:16560537:GC:Gacceptor_gain1.0000
12:16560537:GCCTA:Gacceptor_loss1.0000
12:16560538:CC:Cacceptor_gain1.0000
12:16560538:CCT:Cacceptor_loss1.0000
12:16560539:C:CAacceptor_loss1.0000
12:16560539:C:CCacceptor_gain1.0000
12:16560540:T:Aacceptor_loss1.0000
12:16590509:A:ACdonor_gain1.0000
12:16600746:T:TAdonor_gain1.0000
12:16600864:TATAC:Tacceptor_gain1.0000
12:16600865:ATAC:Aacceptor_gain1.0000
12:16600866:TAC:Tacceptor_gain1.0000
12:16600866:TACC:Tacceptor_loss1.0000
12:16600869:C:CCacceptor_gain1.0000
12:16600869:CTAAA:Cacceptor_loss1.0000
12:16354219:A:Gacceptor_gain0.9900
12:16354228:A:AGacceptor_gain0.9900
12:16354229:A:Gacceptor_gain0.9900
12:16354374:GAAAG:Gdonor_gain0.9900
12:16354376:AAG:Adonor_loss0.9900
12:16354377:AG:Adonor_loss0.9900
12:16354378:GG:Gdonor_loss0.9900
12:16354380:T:Adonor_loss0.9900
12:16357600:GATA:Gacceptor_loss0.9900

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000005682 (12:16517888 A>C,G), RS1000015119 (12:16477572 G>C,T), RS1000018649 (12:16359891 T>G), RS1000029810 (12:16359618 A>G,T), RS1000057979 (12:16571474 A>C,G), RS1000071537 (12:16469519 G>A), RS1000080146 (12:16386496 T>C), RS1000099350 (12:16488357 A>G,T), RS1000100626 (12:16426832 C>A,T), RS1000112128 (12:16398869 G>T), RS1000145160 (12:16438853 A>G), RS1000149954 (12:16553826 G>C), RS1000164506 (12:16505620 A>G,T), RS1000166261 (12:16378117 T>G), RS1000183115 (12:16516209 CAA>C)

Disease associations

OMIM: gene MIM:138330 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): pulmonary disease, chronic obstructive, susceptibility to (MONDO:0100167)

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

10 associations (top):

StudyTraitp-value
GCST001525_20Visceral fat5.000000e-06
GCST002816_1Colorectal cancer (aspirin and/or NSAID use interaction)5.000000e-09
GCST009391_71Metabolite levels4.000000e-06
GCST009524_200Household income (MTAG)6.000000e-09
GCST011354_10Bell’s palsy8.000000e-06
GCST011461_2Barrett’s esophagus or Esophageal adenocarcinoma1.000000e-08
GCST011461_7Barrett’s esophagus or Esophageal adenocarcinoma5.000000e-09
GCST011462_2Barrett’s esophagus or esophageal adenocarcinoma x sex interaction (2df test)4.000000e-08
GCST011584_1Metastatic colorectal cancer survival in treatment with chemotherapy plus biologics1.000000e-06
GCST90026416_16Mild age-related type 2 diabetes8.000000e-06

EFO canonical traits (8, from GWAS)

EFO IDTrait name
EFO:0007010drug use measurement
EFO:0007012NSAID use measurement
EFO:0007013aspirin use measurement
EFO:0010353diacylglycerol 34:2 measurement
EFO:0009695household income
EFO:0008343sex interaction measurement
EFO:0000714survival time
EFO:1001480metastatic colorectal cancer

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1743184 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

Binding affinities (BindingDB)

2 measured of 4 human assays (4 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
640/359KI32700 nM
CEFOPERAZONEKI245000 nM

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
5.42Kd3764nMCHEMBL5653589
5.42ED503764nMCHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 6 total; 1 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide2148747: Binding affinity to human MGST1 incubated for 45 mins by Kinobead based pull down assaykd3.7638uM

CTD chemical–gene interactions

111 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Tobacco Smoke Pollutiondecreases expression, increases expression6
Benzo(a)pyreneincreases methylation, increases expression5
bisphenol Aaffects expression, decreases expression, increases expression, increases methylation4
sodium arseniteincreases abundance, increases expression, increases reaction, decreases expression4
Acetaminophendecreases expression, affects cotreatment, affects expression4
Valproic Acidaffects cotreatment, increases expression, affects expression, decreases methylation4
Cadmium Chlorideincreases expression, decreases reaction, increases abundance, increases palmitoylation, decreases expression4
trichostatin Aincreases expression, affects cotreatment3
Cadmiumdecreases expression, increases expression, decreases reaction, increases abundance, increases palmitoylation3
Estradiolaffects cotreatment, increases expression, decreases expression3
Tetrachlorodibenzodioxindecreases expression, increases expression3
Tretinoindecreases expression3
lead acetateincreases expression2
arseniteaffects binding, increases reaction, increases abundance, increases expression2
nickel sulfateincreases expression2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, decreases expression, increases expression2
Arsenicincreases expression, increases abundance2
Nickeldecreases expression2
Sodium Selenitedecreases expression, increases expression2
beta-Naphthoflavoneincreases expression2
bisphenol Fincreases expression1
TL8-506affects cotreatment, increases expression1
bismuth tripotassium dicitrateincreases expression1
methylmercuric chlorideincreases expression1
triphenyl phosphateaffects expression1
6-hydroxy-5-((p- sulfophenyl)azo)-2-naphthalenesulfonic acid disodium saltaffects cotreatment, increases expression1
sodium arsenateincreases abundance, increases expression1
O,O-diethyl O-3,5,6-trichloro-2-pyridyl phosphateaffects response to substance, affects expression1
pyrogallol 1,3-dimethyl etheraffects cotreatment, increases expression1
beta-lapachoneincreases expression1

ChEMBL screening assays

3 unique, capped per target: 2 admet, 1 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1743239ADMETSubstrates for human microsomal glutathione transferase MGST1Casarett and Doull’s Toxicology The Basic Science of Poisons, 7th edition
CHEMBL5651789BindingBinding affinity to human MGST1 incubated for 45 mins by Kinobead based pull down assayNVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_E1MUHyCyte SK-HEP-1 KO-hMGST1Cancer cell lineMale

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.