Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00065

Target Information
NamePhospholipase A2    
Type of targetSuccessful target    
SynonymsGroup IB phospholipase A2    
Phosphatidylcholine 2-acylhydrolase    
Secreted phospholipase A(2)    
DiseaseArthritis
[ICD9: 710-719   ICD10: M00-M25]
[1]
Eicosanoid-mediated disorders[2]
Inflammation[1]
Drug(s)ClobetasolApprovedInflammation and itching[3]
ClocortoloneApprovedInflammatory skin conditions[4]
DesonideApprovedAtopic dermatitis[5]
DesoximetasoneApprovedInflammatory diseases[6]
DiflorasoneApprovedSkin Allergies[7]
Halobetasol PropionateApprovedInflammatory diseases[8]
HydrocortamateApprovedInflammatory diseases[9]
PrednicarbateApprovedInflammatory diseases[10]
QuinacrineApprovedGiardiasis and cutaneous leishmaniasis[11]
MiltefosinePhase IIVisceral Leishmaniasis, Fungal diseases[12]
BioChemical ClassHydrolases acting on ester bonds    
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 IDP04054
PDB Structure1YSK; 3ELO.    
FunctionPa2 catalyzes the calcium-dependent hydrolysis of the 2-acyl groups in 3-sn-phosphoglycerides.    
SequenceMKLLVLAVLLTVAAADSGISPRAVWQFRKMIKCVIPGSDPFLEYNNYGCYCGLGGSGTPV DELDKCCQTHDNCYDQAKKLDSCKFLLDNPYTHTYSYSCSGSAITCSSKNKECEAFICNC DRNAAICFSKAPYNKAHKNLDTKKYCQS
Related US Patent6,177,426
6,274,578
6,274,616
6,384,041
6,391,908
6,407,104
6,433,001
6,451,839
6,500,853
6,583,177
6,608,099
6,635,670
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-Methyl-2,4-Pentanediol[13]
3,9-dihydroxy-2,10-diprenylpterocap-6a-ene[14]
4'-hydroxy-6,3',5'-triprenylisoflavonone[14]
ABYSSINONE V[14]
Acetate Ion[13]
Alpha-D-Mannose[13]
BOLINAQUINONE[15]
CACOSPONGIONOLIDE[16]
CACOSPONGIONOLIDE B[16]
Cholic Acid[13]
Clobetasol[3]
Desonide[5]
Desoximetasone[6]
Diflorasone[7]
HELENAQUINONE[17]
HYRTIOSULAWESINE[18]
Halobetasol Propionate[8]
Heptanoic Acid[19]
Hexane-1,6-Diol[13]
Hydrocortamate[9]
LY178002[1]
Lpc-Ether[13]
MANOALIDE[18]
Mepacrine[11]
Miltefosine[12]
N-Tridecanoic Acid[19]
P-Anisic Acid[13]
Petrosaspongiolide M[20]
Petrosaspongiolide P[20]
Pyruvoyl Group[13]
Quinacrine[11]
URSOLIC ACID[21]
Varespladib sodium[22]
cacospongionolide E[16]
petrosaspongiolide M[23]
InducerClocortolone[4]
Prednicarbate[10]
BinderLY256548[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The anti-inflammatory effects of LY178002 and LY256548. Agents Actions. 1989 Jun;27(3-4):300-2. To Reference
Ref 2Secreted phospholipase A2 enzymes as therapeutic targets. Expert Opin Ther Targets. 2003 Jun;7(3):427-40. To Reference
Ref 3Utilization of epidermal phospholipase A2 inhibition to monitor topical steroid action. Br J Dermatol. 1984 Jul;111 Suppl 27:195-203. To Reference
Ref 4Clocortolone pivalate: a paired comparison clinical trial of a new topical steroid in eczema/atopic dermatitis. Cutis. 1980 Jan;25(1):96-8. To Reference
Ref 5Desonide foam 0.05%: safety in children as young as 3 months. J Am Acad Dermatol. 2008 Aug;59(2):334-40. To Reference
Ref 6Iatrogenic hyperadrenocorticism and steatohepatitis caused by unapproved medicine. Intern Med. 2008;47(13):1231-6. Epub 2008 Jul 1. To Reference
Ref 7Structures from powders: diflorasone diacetate. Steroids. 2009 Jan;74(1):102-11. Epub 2008 Oct 18. To Reference
Ref 8Topical halobetasol propionate in the treatment of plaque psoriasis: a review. Am J Clin Dermatol. 2005;6(5):311-6. To Reference
Ref 9Hydrocortamate (magnacort) and neomycin-hydrocortamate (neo-magnacort) ointment in dermatology. J Am Med Womens Assoc. 1959 Jan;14(1):54-5. To Reference
Ref 10Small reduction of capsaicin-induced neurogenic inflammation in human forearm skin by the glucocorticoid prednicarbate. Agents Actions. 1993;38 Spec No:C31-4. To Reference
Ref 11Involvement of protein kinase C activation in L-leucine-induced stimulation of protein synthesis in l6 myotubes. Cytotechnology. 2003 Nov;43(1-3):97-103. To Reference
Ref 12Novel antifungal agents, targets or therapeutic strategies for the treatment of invasive fungal diseases: a review of the literature (2005-2009). Rev Iberoam Micol. 2009 Mar 31;26(1):15-22. Epub 2009 May 7. To Reference
Ref 13Overington 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 14J. Nat. Prod. 60(6):537-539 (1997) To Reference
Ref 15J 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 16J 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 17Bioorg Med Chem. 2010 Aug 15;18(16):6006-11. Epub 2010 Jun 25.New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia. To Reference
Ref 18J Nat Prod. 2006 Dec;69(12):1676-9.Hyrtiazepine, an azepino-indole-type alkaloid from the Red Sea marine sponge Hyrtios erectus. To Reference
Ref 19Berman 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 20J Nat Prod. 1998 May;61(5):571-5.Petrosaspongiolides M-R: new potent and selective phospholipase A2 inhibitors from the New Caledonian marine sponge Petrosaspongia nigra. To Reference
Ref 21Bioorg Med Chem Lett. 2005 Sep 15;15(18):4100-4.Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes. To Reference
Ref 22J 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
Ref 23J Med Chem. 2007 May 3;50(9):2176-84. Epub 2007 Apr 4.Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the gamma-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid production through the selective modulation of microsomal prostaglandin E synthase-1 expression. To Reference



 

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