Target Information

Target General Infomation
Target ID
T19160
Former ID
TTDC00025
Target Name
Phospholipase A2, membrane associated
Gene Name
PLA2G2A
Synonyms
GIIC sPLA2; Group IIA phospholipase A2; NPS-PLA2; Non-pancreatic secretory phospholipase A2; PLA2B; PLA2L; Phosphatidylcholine 2-acylhydrolase; RASF-A; PLA2G2A
Target Type
Clinical Trial
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Function
Thoughtto participate in the regulation of the phospholipid metabolism in biomembranes including eicosanoid biosynthesis. Catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides.
BioChemical Class
Carboxylic ester hydrolase
Target Validation
T19160
UniProt ID
P14555
EC Number
EC 3.1.1.4
Sequence
MKTLLLLAVIMIFGLLQAHGNLVNFHRMIKLTTGKEAALSYGFYGCHCGVGGRGSPKDAT
DRCCVTHDCCYKRLEKRGCGTKFLSYKFSNSGSRITCAKQDSCRSQLCECDKAAATCFAR
NKTTYNKKYQYYSNKHCRGSTPRC
Drugs and Mode of Action
Drug(s) KH064 Drug Info Clinical trial Breast cancer [526563]
Inhibitor 1,4-Butanediol Drug Info [551398]
2-(4-phenoxyphenoxy)ethanamine Drug Info [529868]
B-Octylglucoside Drug Info [551393]
BOLINAQUINONE Drug Info [526069]
CACOSPONGIONOLIDE Drug Info [534672]
CACOSPONGIONOLIDE B Drug Info [534672]
Cacospongionolide E Drug Info [534672]
DIDODECANOYLPHLOROGLUCINOL Drug Info [529718]
DYSIDINE Drug Info [526069]
Elaidoylamide Drug Info [551393]
Isopropyl Alcohol Drug Info [551374]
KH064 Drug Info [526563]
Lauric Acid Drug Info [551393]
LUFFARIELLOLIDE Drug Info [551354]
N-Tridecanoic Acid Drug Info [551374]
OCHNAFLAVONE Drug Info [528052]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Phospholipases
KEGG Pathway Glycerophospholipid metabolism
Ether lipid metabolism
Arachidonic acid metabolism
Linoleic acid metabolism
alpha-Linolenic acid metabolism
Metabolic pathways
Ras signaling pathway
Vascular smooth muscle contraction
Pancreatic secretion
Fat digestion and absorption
Pathway Interaction Database Glypican 1 network
Reactome Acyl chain remodelling of PC
Acyl chain remodelling of PE
Acyl chain remodelling of PI
WikiPathways Cardiac Hypertrophic Response
Glycerophospholipid biosynthesis
Glycerophospholipid Biosynthetic Pathway
Spinal Cord Injury
Eicosanoid Synthesis
MicroRNAs in cardiomyocyte hypertrophy
References
Ref 526563D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem. 2003 Mar 3;4(2-3):181-5.
Ref 526069J 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.
Ref 526563D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem. 2003 Mar 3;4(2-3):181-5.
Ref 528052Bioorg Med Chem Lett. 2006 May 1;16(9):2373-5. Epub 2006 Feb 28.Synthesis of phospholipase A2 inhibitory biflavonoids.
Ref 529718Bioorg Med Chem Lett. 2008 Oct 15;18(20):5415-9. Epub 2008 Sep 12.Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
Ref 529868J Med Chem. 2008 Dec 25;51(24):7882-8.Discovery of multitarget inhibitors by combining molecular docking with common pharmacophore matching.
Ref 534672J 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.
Ref 551354Phospholipase A2 inhibitors from marine organisms. J Nat Prod. 1992 Dec;55(12):1701-17.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551398Drosophila metabolize 1,4-butanediol into gamma-hydroxybutyric acid in vivo. Eur J Pharmacol. 2003 Jul 25;473(2-3):149-52.

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