Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T19160
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| Former ID |
TTDC00025
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| Target Name |
Phospholipase A2, membrane associated
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| Gene Name |
PLA2G2A
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| Synonyms |
GIIC sPLA2; Group IIA phospholipase A2; NPS-PLA2; Non-pancreatic secretory phospholipase A2; PLA2B; PLA2L; Phosphatidylcholine 2-acylhydrolase; RASF-A; PLA2G2A
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
Carboxylic ester hydrolase
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| Target Validation |
T19160
|
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| UniProt ID | |||||
| EC Number |
EC 3.1.1.4
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| Sequence |
MKTLLLLAVIMIFGLLQAHGNLVNFHRMIKLTTGKEAALSYGFYGCHCGVGGRGSPKDAT
DRCCVTHDCCYKRLEKRGCGTKFLSYKFSNSGSRITCAKQDSCRSQLCECDKAAATCFAR NKTTYNKKYQYYSNKHCRGSTPRC |
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| Drugs and Mode of Action | |||||
| Drug(s) | KH064 | Drug Info | Clinical trial | Breast cancer | [1] |
| Inhibitor | 1,4-Butanediol | Drug Info | [2] | ||
| 2-(4-phenoxyphenoxy)ethanamine | Drug Info | [3] | |||
| B-Octylglucoside | Drug Info | [4] | |||
| BOLINAQUINONE | Drug Info | [5] | |||
| CACOSPONGIONOLIDE | Drug Info | [6] | |||
| CACOSPONGIONOLIDE B | Drug Info | [6] | |||
| Cacospongionolide E | Drug Info | [6] | |||
| DIDODECANOYLPHLOROGLUCINOL | Drug Info | [7] | |||
| DYSIDINE | Drug Info | [5] | |||
| Elaidoylamide | Drug Info | [4] | |||
| Isopropyl Alcohol | Drug Info | [8] | |||
| KH064 | Drug Info | [1] | |||
| Lauric Acid | Drug Info | [4] | |||
| LUFFARIELLOLIDE | Drug Info | [9] | |||
| N-Tridecanoic Acid | Drug Info | [8] | |||
| OCHNAFLAVONE | Drug Info | [10] | |||
| 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 1 | D-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 2 | Drosophila metabolize 1,4-butanediol into gamma-hydroxybutyric acid in vivo. Eur J Pharmacol. 2003 Jul 25;473(2-3):149-52. | ||||
| REF 3 | J Med Chem. 2008 Dec 25;51(24):7882-8.Discovery of multitarget inhibitors by combining molecular docking with common pharmacophore matching. | ||||
| REF 4 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 5 | J 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 6 | J 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 7 | Bioorg 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 8 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 9 | Phospholipase A2 inhibitors from marine organisms. J Nat Prod. 1992 Dec;55(12):1701-17. | ||||
| REF 10 | Bioorg Med Chem Lett. 2006 May 1;16(9):2373-5. Epub 2006 Feb 28.Synthesis of phospholipase A2 inhibitory biflavonoids. | ||||
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