General Information of Drug Off-Target (DOT) (ID: OTJUGPK0)

DOT Name Glycerol-3-phosphate acyltransferase 3 (GPAT3)
Synonyms
GPAT-3; EC 2.3.1.15; 1-acyl-sn-glycerol-3-phosphate O-acyltransferase 10; AGPAT 10; 1-acyl-sn-glycerol-3-phosphate O-acyltransferase 9; 1-AGP acyltransferase 9; 1-AGPAT 9; EC 2.3.1.51; Acyl-CoA:glycerol-3-phosphate acyltransferase 3; hGPAT3; Lung cancer metastasis-associated protein 1; Lysophosphatidic acid acyltransferase theta; LPAAT-theta; MAG-1
Gene Name GPAT3
Related Disease
Acquired immune deficiency syndrome ( )
Endometritis ( )
Metastatic malignant neoplasm ( )
Neoplasm ( )
Obesity ( )
Acute myelogenous leukaemia ( )
Breast cancer ( )
Breast carcinoma ( )
UniProt ID
GPAT3_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
EC Number
2.3.1.15; 2.3.1.51
Pfam ID
PF01553
Sequence
MEGAELAGKILSTWLTLVLGFILLPSVFGVSLGISEIYMKILVKTLEWATIRIEKGTPKE
SILKNSASVGIIQRDESPMEKGLSGLRGRDFELSDVFYFSKKGLEAIVEDEVTQRFSSEE
LVSWNLLTRTNVNFQYISLRLTMVWVLGVIVRYCVLLPLRVTLAFIGISLLVIGTTLVGQ
LPDSSLKNWLSELVHLTCCRICVRALSGTIHYHNKQYRPQKGGICVANHTSPIDVLILTT
DGCYAMVGQVHGGLMGIIQRAMVKACPHVWFERSEMKDRHLVTKRLKEHIADKKKLPILI
FPEGTCINNTSVMMFKKGSFEIGGTIHPVAIKYNPQFGDAFWNSSKYNMVSYLLRMMTSW
AIVCDVWYMPPMTREEGEDAVQFANRVKSAIAIQGGLTELPWDGGLKRAKVKDIFKEEQQ
KNYSKMIVGNGSLS
Function
Converts glycerol-3-phosphate to 1-acyl-sn-glycerol-3-phosphate (lysophosphatidic acid or LPA) by incorporating an acyl moiety at the sn-1 position of the glycerol backbone. Also converts LPA into 1,2-diacyl-sn-glycerol-3-phosphate (phosphatidic acid or PA) by incorporating an acyl moiety at the sn-2 position of the glycerol backbone. Protects cells against lipotoxicity.
Tissue Specificity Widely expressed. Expressed in liver, kidney, testis, brain, heart, skeletal muscle, thyroid, prostate, thymus and placenta. Also expressed lung and adipose tissue.
KEGG Pathway
Glycerolipid metabolism (hsa00561 )
Glycerophospholipid metabolism (hsa00564 )
Metabolic pathways (hsa01100 )
Reactome Pathway
Synthesis of PA (R-HSA-1483166 )

Molecular Interaction Atlas (MIA) of This DOT

8 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Acquired immune deficiency syndrome DISL5UOX Strong Biomarker [1]
Endometritis DISHGJ6G Strong Biomarker [2]
Metastatic malignant neoplasm DIS86UK6 Strong Biomarker [3]
Neoplasm DISZKGEW Strong Biomarker [3]
Obesity DIS47Y1K Strong Biomarker [4]
Acute myelogenous leukaemia DISCSPTN moderate Genetic Variation [5]
Breast cancer DIS7DPX1 Limited Biomarker [6]
Breast carcinoma DIS2UE88 Limited Biomarker [6]
------------------------------------------------------------------------------------
⏷ Show the Full List of 8 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
41 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [7]
Ciclosporin DMAZJFX Approved Ciclosporin increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [8]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [9]
Acetaminophen DMUIE76 Approved Acetaminophen increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [10]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [11]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [12]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [8]
Ivermectin DMDBX5F Approved Ivermectin decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [13]
Quercetin DM3NC4M Approved Quercetin increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [14]
Temozolomide DMKECZD Approved Temozolomide decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [15]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide affects the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [16]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [17]
Phenobarbital DMXZOCG Approved Phenobarbital affects the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [18]
Menadione DMSJDTY Approved Menadione increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [16]
Bortezomib DMNO38U Approved Bortezomib increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [19]
Hydroquinone DM6AVR4 Approved Hydroquinone increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [20]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Azathioprine DMMZSXQ Approved Azathioprine increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
Cidofovir DMA13GD Approved Cidofovir increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Fenofibrate DMFKXDY Approved Fenofibrate increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Ifosfamide DMCT3I8 Approved Ifosfamide increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Clodronate DM9Y6X7 Approved Clodronate increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Ibuprofen DM8VCBE Approved Ibuprofen increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [21]
Lindane DMB8CNL Approved Lindane increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
Vitamin C DMXJ7O8 Approved Vitamin C increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
Ampicillin DMHWE7P Approved Ampicillin decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [14]
Phenol DM1QSM3 Phase 2/3 Phenol increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
DNCB DMDTVYC Phase 2 DNCB affects the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [23]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the mutagenesis of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [24]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [25]
Eugenol DM7US1H Patented Eugenol increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [22]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [26]
Formaldehyde DM7Q6M0 Investigative Formaldehyde decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [27]
Milchsaure DM462BT Investigative Milchsaure decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [28]
Sulforaphane DMQY3L0 Investigative Sulforaphane increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [29]
Nickel chloride DMI12Y8 Investigative Nickel chloride affects the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [23]
CH-223191 DMMJZYC Investigative CH-223191 decreases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [30]
Oleic acid DM54O1Z Investigative Oleic acid increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [31]
GW7647 DM9RD0C Investigative GW7647 increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [31]
CITCO DM0N634 Investigative CITCO increases the expression of Glycerol-3-phosphate acyltransferase 3 (GPAT3). [31]
------------------------------------------------------------------------------------
⏷ Show the Full List of 41 Drug(s)

References

1 Efficacy of a novel reverse transcriptase-polymerase chain reaction (RT-PCR) for detecting Toxoplasma gondii bradyzoite gene expression in human clinical specimens.Mol Cell Probes. 2002 Feb;16(1):31-9. doi: 10.1006/mcpr.2001.0394.
2 Genomic breeding values, SNP effects and gene identification for disease traits in cow training sets.Anim Genet. 2018 Jun;49(3):178-192. doi: 10.1111/age.12661. Epub 2018 Apr 6.
3 Metastasis-associated gene, mag-1 improves tumour microenvironmental adaptation and potentiates tumour metastasis.J Cell Mol Med. 2012 Dec;16(12):3037-51. doi: 10.1111/j.1582-4934.2012.01633.x.
4 Molecular identification of microsomal acyl-CoA:glycerol-3-phosphate acyltransferase, a key enzyme in de novo triacylglycerol synthesis.Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19695-700. doi: 10.1073/pnas.0609140103. Epub 2006 Dec 14.
5 Genome-wide haplotype association study identify the FGFR2 gene as a risk gene for acute myeloid leukemia.Oncotarget. 2017 Jan 31;8(5):7891-7899. doi: 10.18632/oncotarget.13631.
6 AGPAT9 suppresses cell growth, invasion and metastasis by counteracting acidic tumor microenvironment through KLF4/LASS2/V-ATPase signaling pathway in breast cancer.Oncotarget. 2015 Jul 30;6(21):18406-17. doi: 10.18632/oncotarget.4074.
7 From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
8 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
9 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
10 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
11 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
12 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
13 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
14 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
15 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
16 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
17 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
18 Reproducible chemical-induced changes in gene expression profiles in human hepatoma HepaRG cells under various experimental conditions. Toxicol In Vitro. 2009 Apr;23(3):466-75. doi: 10.1016/j.tiv.2008.12.018. Epub 2008 Dec 30.
19 The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
20 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
21 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
22 Oxidative stress mechanisms do not discriminate between genotoxic and nongenotoxic liver carcinogens. Chem Res Toxicol. 2015 Aug 17;28(8):1636-46.
23 Preliminary discovery of novel markers for human cell line activation test (h-CLAT). Toxicol In Vitro. 2021 Aug;74:105154. doi: 10.1016/j.tiv.2021.105154. Epub 2021 Mar 25.
24 Exome-wide mutation profile in benzo[a]pyrene-derived post-stasis and immortal human mammary epithelial cells. Mutat Res Genet Toxicol Environ Mutagen. 2014 Dec;775-776:48-54. doi: 10.1016/j.mrgentox.2014.10.011. Epub 2014 Nov 4.
25 Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
26 Bisphenol A induces DSB-ATM-p53 signaling leading to cell cycle arrest, senescence, autophagy, stress response, and estrogen release in human fetal lung fibroblasts. Arch Toxicol. 2018 Apr;92(4):1453-1469.
27 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
28 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
29 Sulforaphane-induced apoptosis in human leukemia HL-60 cells through extrinsic and intrinsic signal pathways and altering associated genes expression assayed by cDNA microarray. Environ Toxicol. 2017 Jan;32(1):311-328.
30 The Ah receptor regulates growth factor expression in head and neck squamous cell carcinoma cell lines. Mol Carcinog. 2014 Oct;53(10):765-76.
31 Farnesol induces fatty acid oxidation and decreases triglyceride accumulation in steatotic HepaRG cells. Toxicol Appl Pharmacol. 2019 Feb 15;365:61-70.