Details of the Target

General Information of Target

Target ID LDTP06885
Target Name Glycerol-3-phosphate acyltransferase 3 (GPAT3)
Gene Name GPAT3
Gene ID 84803
Synonyms
AGPAT9; MAG1; Glycerol-3-phosphate acyltransferase 3; 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
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEGAELAGKILSTWLTLVLGFILLPSVFGVSLGISEIYMKILVKTLEWATIRIEKGTPKE
SILKNSASVGIIQRDESPMEKGLSGLRGRDFELSDVFYFSKKGLEAIVEDEVTQRFSSEE
LVSWNLLTRTNVNFQYISLRLTMVWVLGVIVRYCVLLPLRVTLAFIGISLLVIGTTLVGQ
LPDSSLKNWLSELVHLTCCRICVRALSGTIHYHNKQYRPQKGGICVANHTSPIDVLILTT
DGCYAMVGQVHGGLMGIIQRAMVKACPHVWFERSEMKDRHLVTKRLKEHIADKKKLPILI
FPEGTCINNTSVMMFKKGSFEIGGTIHPVAIKYNPQFGDAFWNSSKYNMVSYLLRMMTSW
AIVCDVWYMPPMTREEGEDAVQFANRVKSAIAIQGGLTELPWDGGLKRAKVKDIFKEEQQ
KNYSKMIVGNGSLS
Target Bioclass
Enzyme
Family
1-acyl-sn-glycerol-3-phosphate acyltransferase family
Subcellular location
Endoplasmic reticulum membrane
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.
Uniprot ID
Q53EU6
Ensemble ID
ENST00000264409.5
HGNC ID
HGNC:28157
ChEMBL ID
CHEMBL4523318

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		14.69  LDD0402  [1]
YN-1
 Probe Info  		100.00  LDD0444  [2]
STPyne
 Probe Info  		K284(7.26); K287(5.43); K293(10.00); K388(1.23)  LDD0277  [3]
BTD
 Probe Info  		C266(1.07)  LDD2104  [4]
AHL-Pu-1
 Probe Info  		C306(3.06)  LDD0169  [5]
EA-probe
 Probe Info  		C306(1.87)  LDD2210  [6]
Acrolein
 Probe Info  		N.A.  LDD0221  [7]
IA-alkyne
 Probe Info  		C306(0.00); C266(0.00)  LDD0162  [8]
IPM
 Probe Info  		N.A.  LDD2156  [9]
Methacrolein
 Probe Info  		N.A.  LDD0218  [7]
AOyne
 Probe Info  		15.00  LDD0443  [10]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-DA
 Probe Info  		2.70  LDD0143  [11]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C266(0.69)  LDD2142  [4]
 LDCM0026  4SU-RNA+native RNA HEK-293T C306(3.06)  LDD0169  [5]
 LDCM0156  Aniline NCI-H1299 12.35  LDD0403  [1]
 LDCM0083  Avasimibe A-549 2.70  LDD0143  [11]
 LDCM0630  CCW28-3 231MFP C306(2.01)  LDD2214  [12]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [7]
 LDCM0175  Ethacrynic acid HeLa C306(1.87)  LDD2210  [6]
 LDCM0107  IAA HeLa N.A.  LDD0221  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C266(1.07)  LDD2104  [4]
 LDCM0627  NUDT7-COV-1 HEK-293T C266(1.42)  LDD2206  [13]
 LDCM0628  OTUB2-COV-1 HEK-293T C266(0.91)  LDD2207  [13]
 LDCM0084  Ro 48-8071 A-549 2.93  LDD0145  [11]

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
3 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
4 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
5 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
6 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
7 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
8 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
9 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
10 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
11 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.
12 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
13 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.