Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00025

Target Information
NamePhospholipase A2, membrane associated    
Type of targetClinical trial target    
SynonymsGIIC sPLA2    
Group IIA phospholipase A2    
NPS-PLA2    
Non-pancreatic secretory phospholipase A2    
PLA2B    
PLA2G2A    
PLA2L    
Phosphatidylcholine 2-acylhydrolase    
RASF-A    
DiseaseAtherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[1][2]
Coronary Artery Disease
[ICD9: 410-414, 429.2   ICD10: I20-I25]
[1][2]
Drug(s)VarespladibPhase IICoronary Artery Disease, Atherosclerosis[1][2]
EC NumberEC 3.1.1.4
PathwayArachidonic acid metabolism
Ether lipid metabolism
Fc epsilon RI signaling pathway
Glycerophospholipid metabolism
GnRH signaling pathway
Linoleic acid metabolism
Long-term depression
MAPK signaling pathway
Metabolic pathways
VEGF signaling pathway
Vascular smooth muscle contraction
alpha-Linolenic acid metabolism
UniProt IDP14555
PDB Structure1AYP; 1BBC; 1DB4; 1DB5; 1DCY; 1J1A; 1KQU; 1KVO; 1N28; 1N29; 1POD; 1POE; 2GNY; 3U8B; 3U8D; 3U8H; 3U8I.    
SequenceMKTLLLLAVIMIFGLLQAHGNLVNFHRMIKLTTGKEAALSYGFYGCHCGVGGRGSPKDAT DRCCVTHDCCYKRLEKRGCGTKFLSYKFSNSGSRITCAKQDSCRSQLCECDKAAATCFAR NKTTYNKKYQYYSNKHCRGSTPRC
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,4-Butanediol[3]
2- (4-phenoxyphenoxy)ethanamine[4]
B-Octylglucoside[5]
BOLINAQUINONE[6]
CACOSPONGIONOLIDE[7]
CACOSPONGIONOLIDE B[7]
DIDODECANOYLPHLOROGLUCINOL[8]
DYSIDINE[6]
Elaidoylamide[5]
Isopropyl Alcohol[9]
LUFFARIELLOLIDE[10]
Lauric Acid[5]
MANOALIDE[7]
N-Tridecanoic Acid[9]
OCHNAFLAVONE[11]
Varespladib[1][2]
Varespladib sodium[12]
YM-26734[8]
cacospongionolide E[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Update on patented cholesterol absorption inhibitors. Expert Opin Ther Pat. 2009 Aug;19(8):1083-107. To Reference
Ref 2Effects of 1-H-indole-3-glyoxamide (A-002) on concentration of secretory phospholipase A2 (PLASMA study): a phase II double-blind, randomised, placebo-controlled trial. Lancet. 2009 Feb 21;373(9664):649-58. To Reference
Ref 3Satta R, Dimitrijevic N, Manev H: Drosophila metabolize 1,4-butanediol into gamma-hydroxybutyric acid in vivo. Eur J Pharmacol. 2003 Jul 25;473(2-3):149-52. To Reference
Ref 4J Med Chem. 2008 Dec 25;51(24):7882-8.Discovery of multitarget inhibitors by combining molecular docking with common pharmacophore matching. To Reference
Ref 5Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 6J Nat Prod. 2001 May;64(5):612-5.New sesquiterpene derivatives from the sponge Dysidea species with a selective inhibitor profile against human phospholipase A2 and other leukocyte functions. To Reference
Ref 7J Nat Prod. 1998 Jul;61(7):931-5.A new cacospongionolide inhibitor of human secretory phospholipase A2 from the Tyrrhenian sponge Fasciospongia cavernosa and absolute configuration of cacospongionolides. To Reference
Ref 8Bioorg Med Chem Lett. 2008 Oct 15;18(20):5415-9. Epub 2008 Sep 12.Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA. To Reference
Ref 9Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 10J. Nat. Prod. 55(12):1701-1717 (1992) To Reference
Ref 11Bioorg Med Chem Lett. 2006 May 1;16(9):2373-5. Epub 2006 Feb 28.Synthesis of phospholipase A2 inhibitory biflavonoids. To Reference
Ref 12J Med Chem. 2008 Aug 14;51(15):4708-14. Epub 2008 Jul 8.Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. To Reference



 

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