General Information of Drug Therapeutic Target (DTT) (ID: TTDNFMT)

DTT Name Platelet-activating factor acetylhydrolase (PLA2G7)
Synonyms
gVIIA-PLA2; PAFAH; PAF acetylhydrolase; PAF 2-acylhydrolase; Lipoprotein-associated phospholipase A2; LDL-associated phospholipase A2; LDL-PLA(2); Group-VIIA phospholipase A2; 2-acetyl-1-alkylglycerophosphocholine esterase; 1-alkyl-2-acetylglycerophosphocholine esterase
Gene Name PLA2G7
DTT Type
Clinical trial target
[1]
BioChemical Class
Carboxylic ester hydrolase
UniProt ID
PAFA_HUMAN
TTD ID
T69912
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.1.1.47
Sequence
MVPPKLHVLFCLCGCLAVVYPFDWQYINPVAHMKSSAWVNKIQVLMAAASFGQTKIPRGN
GPYSVGCTDLMFDHTNKGTFLRLYYPSQDNDRLDTLWIPNKEYFWGLSKFLGTHWLMGNI
LRLLFGSMTTPANWNSPLRPGEKYPLVVFSHGLGAFRTLYSAIGIDLASHGFIVAAVEHR
DRSASATYYFKDQSAAEIGDKSWLYLRTLKQEEETHIRNEQVRQRAKECSQALSLILDID
HGKPVKNALDLKFDMEQLKDSIDREKIAVIGHSFGGATVIQTLSEDQRFRCGIALDAWMF
PLGDEVYSRIPQPLFFINSEYFQYPANIIKMKKCYSPDKERKMITIRGSVHQNFADFTFA
TGKIIGHMLKLKGDIDSNVAIDLSNKASLAFLQKHLGLHKDFDQWDCLIEGDDENLIPGT
NINTTNQHIMLQNSSGIEKYN
Function
Has a specificity for substrates with a short residue at the sn-2 position. It is inactive against long-chain phospholipids. Modulates the action of platelet-activating factor (PAF) by hydrolyzing the sn-2 ester bond to yield the biologically inactive lyso-PAF.
KEGG Pathway
Ether lipid metabolism (hsa00565 )
Metabolic pathways (hsa01100 )
Biosynthesis of antibiotics (hsa01130 )
Reactome Pathway
Synthesis, secretion, and deacylation of Ghrelin (R-HSA-422085 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
GSK2647544 DM3KARJ Alzheimer disease 8A20 Phase 1 [2]
Rilapladib DMB9861 Arteriosclerosis BD40 Phase 1 [1]
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2 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bicyclic pyrimidine derivative 2 DMJP16K N. A. N. A. Patented [3]
Indolizine derivative 1 DM4GZBI N. A. N. A. Patented [3]
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3 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
RPAF-AH DMOVJ60 Sepsis 1G40-1G41 Discontinued in Phase 3 [4]
Goxalapladib DMSGUY9 Arteriosclerosis BD40 Discontinued in Phase 1 [5]
GSK568859 DM6E84O Arteriosclerosis BD40 Discontinued in Phase 1 [2]
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6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(1r)-1,2,2-trimethylpropyl (r)-methylphosphinate DMVE34H Discovery agent N.A. Investigative [6]
(E)-(thiophen-2-ylmethylidene)amino benzoate DMHSJAT Discovery agent N.A. Investigative [7]
3,4-difluorobenzaldehyde O-benzoyloxime DMFV3Y9 Discovery agent N.A. Investigative [8]
4-fluorobenzaldehyde O-benzoyloxime DM2N4BJ Discovery agent N.A. Investigative [8]
Benzaldehyde O-benzoyloxime DMB7DFT Discovery agent N.A. Investigative [8]
SB-381320 DM3BV5S Discovery agent N.A. Investigative [7]
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⏷ Show the Full List of 6 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Neonatal sepsis 1G41 Whole blood 6.70E-02 -0.48 -0.8
Alzheimer's disease 8A00.0 Entorhinal cortex 5.33E-03 0.09 0.23
Coronary artery disease BA80-BA8Z Peripheral blood 2.26E-01 -0.09 -0.29
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References

1 Phospholipase A2 inhibitors. Curr Opin Lipidol. 2009 Aug;20(4):327-32.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1432).
3 Inhibitors of phospholipase A2 and their therapeutic potential: an update on patents (2012-2016).Expert Opin Ther Pat. 2017 Feb;27(2):217-225.
4 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006777)
5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020582)
6 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
7 (E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7.
8 Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9.