Target Information

Target General Infomation
Target ID
T69912
Former ID
TTDC00116
Target Name
Lipoprotein-associated phospholipase A2
Gene Name
PLA2G7
Synonyms
1-alkyl-2-acetylglycerophosphocholine esterase; 2-acetyl-1-alkylglycerophosphocholine esterase; LDL-PLA(2); LDL-associated phospholipase A2; Lipoprotein-associated phospholipase A2; PAF 2-acylhydrolase; PAF acetylhydrolase; PLA2G7
Target Type
Clinical Trial
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Arteriosclerosis [ICD9: 440; ICD10: I70]
Cardiovascular disorder [ICD10: I00-I99]
Sepsis [ICD9: 995.91; ICD10: A40, A41]
Function
Modulates the action of platelet-activating factor (PAF) by hydrolyzing the sn-2 ester bond to yield the biologically inactive lyso-PAF. Has a specificity for substrates with a short residue at the sn-2 position. It is inactive against long-chain phospholipids.
BioChemical Class
Carboxylic ester hydrolase
Target Validation
T69912
UniProt ID
Q13093
EC Number
EC 3.1.1.47
Sequence
MVPPKLHVLFCLCGCLAVVYPFDWQYINPVAHMKSSAWVNKIQVLMAAASFGQTKIPRGN
GPYSVGCTDLMFDHTNKGTFLRLYYPSQDNDRLDTLWIPNKEYFWGLSKFLGTHWLMGNI
LRLLFGSMTTPANWNSPLRPGEKYPLVVFSHGLGAFRTLYSAIGIDLASHGFIVAAVEHR
DRSASATYYFKDQSAAEIGDKSWLYLRTLKQEEETHIRNEQVRQRAKECSQALSLILDID
HGKPVKNALDLKFDMEQLKDSIDREKIAVIGHSFGGATVIQTLSEDQRFRCGIALDAWMF
PLGDEVYSRIPQPLFFINSEYFQYPANIIKMKKCYSPDKERKMITIRGSVHQNFADFTFA
TGKIIGHMLKLKGDIDSNVAIDLSNKASLAFLQKHLGLHKDFDQWDCLIEGDDENLIPGT
NINTTNQHIMLQNSSGIEKYN
Structure
3D59; 3D5E; 3F96; 3F97; 3F98; 3F9C
Drugs and Mode of Action
Drug(s) GSK 659032 Drug Info Phase 1 Cardiovascular disorder [547694]
GSK2647544 Drug Info Phase 1 Alzheimer disease [524402]
Rilapladib Drug Info Phase 1 Arteriosclerosis [542396], [547694]
RPAF-AH Drug Info Discontinued in Phase 3 Sepsis [521515]
Goxalapladib Drug Info Discontinued in Phase 1 Arteriosclerosis [547940]
GSK568859 Drug Info Discontinued in Phase 1 Atherosclerosis [548491]
Inhibitor (1R)-1,2,2-TRIMETHYLPROPYL (R)-METHYLPHOSPHINATE Drug Info [551374]
(E)-(thiophen-2-ylmethylidene)amino benzoate Drug Info [527433]
3,4-difluorobenzaldehyde O-benzoyloxime Drug Info [528384]
4-fluorobenzaldehyde O-benzoyloxime Drug Info [528384]
Benzaldehyde O-benzoyloxime Drug Info [528384]
GSK 659032 Drug Info [537512]
Rilapladib Drug Info [1725884]
SB-381320 Drug Info [527433]
Modulator Goxalapladib Drug Info [547941]
GSK2647544 Drug Info [543419]
GSK568859 Drug Info [543419]
RPAF-AH Drug Info [546181]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Ether lipid metabolism
Metabolic pathways
Biosynthesis of antibiotics
Pathway Interaction Database Lissencephaly gene (LIS1) in neuronal migration and development
WikiPathways IL1 and megakaryotyces in obesity
Synthesis, Secretion, and Deacylation of Ghrelin
References
Ref 521515ClinicalTrials.gov (NCT00037687) Safety and Efficacy of Recombinant Human Platelet-Activating Factor Acetylhydrolase for the Treatment of Severe Sepsis. U.S. National Institutes of Health.
Ref 524402ClinicalTrials.gov (NCT01924858) A Positron Emission Tomography (PET) Study to Investigate the Brain Biodistribution of 18F GSK2647544 in Healthy Subjects to Determine Its Ability to Cross the Blood-brain-barrier.. U.S. National Institutes of Health.
Ref 542396(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. (Ligand id: 7376).
Ref 547694Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018454)
Ref 547940Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020582)
Ref 548491Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025982)
Ref 527433Bioorg Med Chem Lett. 2005 Mar 1;15(5):1525-7.(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.
Ref 528384Bioorg Med Chem Lett. 2006 Nov 1;16(21):5576-9. Epub 2006 Aug 21.Potent inhibitors of lipoprotein-associated phospholipase A(2): benzaldehyde O-heterocycle-4-carbonyloxime.
Ref 537512Phospholipase A2 inhibitors. Curr Opin Lipidol. 2009 Aug;20(4):327-32.
Ref 543419(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).
Ref 546181Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006777)
Ref 547941Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020582)
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 1725884THERAPEUTICS: Rilapladib

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