Details of the Target

General Information of Target

Target ID LDTP13129
Target Name Phosphatidylethanolamine N-methyltransferase (PEMT)
Gene Name PEMT
Gene ID 10400
Synonyms
PEMPT; PNMT; Phosphatidylethanolamine N-methyltransferase; PEAMT; PEMT; EC 2.1.1.17; EC 2.1.1.71; PEMT2; Phospholipid methyltransferase; PLMT
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAAQPKYPAGATARRLARGCWSALWDYETPKVIVVRNRRLGVLYRAVQLLILLYFVWYV
FIVQKSYQESETGPESSIITKVKGITTSEHKVWDVEEYVKPPEGGSVFSIITRVEATHSQ
TQGTCPESIRVHNATCLSDADCVAGELDMLGNGLRTGRCVPYYQGPSKTCEVFGWCPVED
GASVSQFLGTMAPNFTILIKNSIHYPKFHFSKGNIADRTDGYLKRCTFHEASDLYCPIFK
LGFIVEKAGESFTELAHKGGVIGVIINWDCDLDLPASECNPKYSFRRLDPKHVPASSGYN
FRFAKYYKINGTTTRTLIKAYGIRIDVIVHGQAGKFSLIPTIINLATALTSVGVGSFLCD
WILLTFMNKNKVYSHKKFDKVCTPSHPSGSWPVTLARVLGQAPPEPGHRSEDQHPSPPSG
QEGQQGAECGPAFPPLRPCPISAPSEQMVDTPASEPAQASTPTDPKGLAQL
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Class VI-like SAM-binding methyltransferase superfamily, PEMT/PEM2 methyltransferase family
Subcellular location
Endoplasmic reticulum membrane; Endoplasmic reticulum
Function
Catalyzes the three sequential steps of the methylation pathway for the biosynthesis of phosphatidylcholine, a critical and essential component for membrane structure. Uses S-adenosylmethionine (S-adenosyl-L-methionine, SAM or AdoMet) as the methyl group donor for the methylation of phosphatidylethanolamine (1,2-diacyl-sn-glycero-3-phosphoethanolamine, PE) to phosphatidylmonomethylethanolamine (1,2-diacyl-sn-glycero-3-phospho-N-methylethanolamine, PMME), PMME to phosphatidyldimethylethanolamine (1,2-diacyl-sn-glycero-3-phospho-N,N-dimethylethanolamine, PDME), and PDME to phosphatidylcholine (1,2-diacyl-sn-glycero-3-phosphocholine, PC), producing S-adenosyl-L-homocysteine in each step. Responsible for approximately 30% of hepatic PC with the CDP-choline pathway accounting for the other 70% (Probable).; [Isoform 1]: Catalyzes the three sequential steps of the methylation of 1,2-diacyl-sn-glycero-3-phospho-N-methylethanolamine (PMME) to 1,2-diacyl-sn-glycero-3-phospho-N,N-dimethylethanolamine (PDME) more efficiently than isoform 2. Induces increase in PC species with longer polyunsaturated chains than isoform 2.; [Isoform 2]: Produces a higher increase in the level of PC species containing long chains with three double bonds than isoform 1.
TTD ID
T66206
Uniprot ID
Q9UBM1
DrugMap ID
TT735V2
Ensemble ID
ENST00000255389.10
HGNC ID
HGNC:8830

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K38(5.91)  LDD0277  [1]
IA-alkyne
 Probe Info  		C70(1.32)  LDD2182  [2]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [3]
TFBX
 Probe Info  		N.A.  LDD0027  [4]
IPM
 Probe Info  		N.A.  LDD0005  [5]
NAIA_5
 Probe Info  		C53(0.00); C70(0.00)  LDD2223  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C70(1.55)  LDD1702  [7]
 LDCM0625  F8 Ramos C70(0.81)  LDD2187  [2]
 LDCM0575  Fragment13 Ramos C70(0.44)  LDD2192  [2]
 LDCM0576  Fragment14 Ramos C70(1.69)  LDD2193  [2]
 LDCM0580  Fragment21 Ramos C70(1.83)  LDD2195  [2]
 LDCM0582  Fragment23 Ramos C70(1.13)  LDD2196  [2]
 LDCM0578  Fragment27 Ramos C70(0.99)  LDD2197  [2]
 LDCM0586  Fragment28 Ramos C70(1.53)  LDD2198  [2]
 LDCM0588  Fragment30 Ramos C70(0.47)  LDD2199  [2]
 LDCM0589  Fragment31 Ramos C70(0.63)  LDD2200  [2]
 LDCM0468  Fragment33 Ramos C70(0.84)  LDD2202  [2]
 LDCM0596  Fragment38 Ramos C70(4.40)  LDD2203  [2]
 LDCM0614  Fragment56 Ramos C70(1.41)  LDD2205  [2]
 LDCM0022  KB02 Ramos C70(1.32)  LDD2182  [2]
 LDCM0627  NUDT7-COV-1 HEK-293T C70(1.03)  LDD2206  [8]
 LDCM0628  OTUB2-COV-1 HEK-293T C70(0.64)  LDD2207  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Stomatin (STOM) Band 7/mec-2 family P27105
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520

References

1 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
2 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
3 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
5 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
6 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
7 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
8 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.