Target Information

Target General Infomation
Target ID
T31479
Former ID
TTDS00065
Target Name
Phospholipase A2
Gene Name
PLA2G1B
Synonyms
Group IB phospholipase A2; Phosphatidylcholine 2-acylhydrolase; Secreted phospholipase A(2); PLA2G1B
Target Type
Successful
Disease Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Asthma [ICD10: J45]
Allergy [ICD9: 995.3; ICD10: T78.4]
Arteriosclerosis [ICD9: 440; ICD10: I70]
Arthritis [ICD9: 710-719; ICD10: M00-M25]
Contact dermatitis [ICD9: 692; ICD10: L23, L24, L25]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp [ICD10: L20-L30]
Inflammatory and pruritic manifestations of corticosteroid responsive dermatoses [ICD10: L20-L30]
Leishmaniasis [ICD10: B55.0]
Nerve injury [ICD10: T14.4]
Pruritus [ICD9: 698; ICD10: L29]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Visceral leishmaniasis [ICD9: 85; ICD10: B55.0]
Unspecified [ICD code not available]
Function
PA2 catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides, this releases glycerophospholipids and arachidonic acid that serve as the precursors of signal molecules.
BioChemical Class
Carboxylic ester hydrolase
Target Validation
T31479
UniProt ID
P04054
EC Number
EC 3.1.1.4
Sequence
MKLLVLAVLLTVAAADSGISPRAVWQFRKMIKCVIPGSDPFLEYNNYGCYCGLGGSGTPV
DELDKCCQTHDNCYDQAKKLDSCKFLLDNPYTHTYSYSCSGSAITCSSKNKECEAFICNC
DRNAAICFSKAPYNKAHKNLDTKKYCQS
Drugs and Mode of Action
Drug(s) Cholic Acid Drug Info Approved Peroxisomal disorders; Synthesis disorders [1]
Clobetasol Drug Info Approved Inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp [2]
Clocortolone Drug Info Approved Inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp [2]
Diflorasone Drug Info Approved Inflammatory and pruritic manifestations of corticosteroid responsive dermatoses [2]
Miltefosine Drug Info Approved Leishmaniasis [3]
AllerB Drug Info Phase 2b Allergy [4]
MANOALIDE Drug Info Phase 2 Arthritis [5]
Miltefosine Drug Info Phase 2 Visceral leishmaniasis [6]
MRX-4 Drug Info Phase 2 Allergic rhinitis [7]
MRX-6 Drug Info Phase 2 Contact dermatitis [8]
Rilapladib Drug Info Phase 1 Arteriosclerosis [9], [10]
Darapladib Drug Info Discontinued in Phase 3 Arteriosclerosis [11], [12]
BMY-30129 Drug Info Discontinued in Phase 2 Pruritus [13]
EPC-K1 Drug Info Discontinued in Phase 2 Nerve injury [14]
SC-106 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [15]
WAY-123641 Drug Info Discontinued in Phase 2 Asthma [16]
PF-05212372 Drug Info Discontinued in Phase 1 Asthma [17]
SB-435495 Drug Info Discontinued in Phase 1 Arteriosclerosis [18]
YM-26734 Drug Info Terminated Rheumatoid arthritis [19]
Inhibitor 2-Methyl-2,4-Pentanediol Drug Info [20]
3,9-dihydroxy-2,10-diprenylpterocap-6a-ene Drug Info [21]
4'-hydroxy-6,3',5'-triprenylisoflavonone Drug Info [21]
ABYSSINONE V Drug Info [21]
Acetate Ion Drug Info [20]
AllerB Drug Info [22]
Alpha-D-Mannose Drug Info [20]
BM-162115 Drug Info [23]
BMY-30129 Drug Info [24], [2]
BOLINAQUINONE Drug Info [25]
CACOSPONGIONOLIDE Drug Info [26]
CACOSPONGIONOLIDE B Drug Info [26]
Cacospongionolide E Drug Info [26]
Cholic Acid Drug Info [20]
Clobetasol Drug Info [27]
Diflorasone Drug Info [28]
EPC-K1 Drug Info [29], [2]
HELENAQUINONE Drug Info [30]
Heptanoic Acid Drug Info [31]
Hexane-1,6-Diol Drug Info [20]
HYRTIOSULAWESINE Drug Info [32]
Lpc-Ether Drug Info [20]
LY178002 Drug Info [33]
Mepacrine Drug Info [34]
Miltefosine Drug Info [6]
MRX-4 Drug Info [35]
MRX-6 Drug Info [36]
N-Tridecanoic Acid Drug Info [31]
P-Anisic Acid Drug Info [20]
Petrosaspongiolide M Drug Info [37]
Petrosaspongiolide P Drug Info [38]
PF-05212372 Drug Info [39]
Pyruvoyl Group Drug Info [20]
SB-435495 Drug Info [40]
SC-106 Drug Info [41]
URSOLIC ACID Drug Info [42]
WAY-123641 Drug Info [43]
Modulator AGN-190383 Drug Info
Darapladib Drug Info [44]
folipastatin Drug Info
MANOALIDE Drug Info
Rilapladib Drug Info
SB-203347 Drug Info
WA-8242-A1 Drug Info
YM-26734 Drug Info
Inducer Clocortolone Drug Info [45]
Binder LY256548 Drug Info [33]
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 Fc-epsilon receptor I signaling in mast cells
Reactome Acyl chain remodelling of PC
Acyl chain remodelling of PE
Acyl chain remodelling of PI
WikiPathways Glycerophospholipid biosynthesis
References
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REF 21Phospholipase A2 Inhibitors from an Erythrina Species from Samoa J. Nat. Prod. 60(6):537-539 (1997).
REF 22Successful immunotherapy with T-cell epitope peptides of bee venom phospholipase A2 induces specific T-cell anergy in patients allergic to bee venom. J Allergy Clin Immunol. 1998 Jun;101(6 Pt 1):747-54.
REF 23Investigation on the effect of experimental phospholipase A2 inhibitors on the formyl-methionyl-leucyl-phenylalanine-stimulated chemotaxis of human leukocytes in vitro. Arzneimittelforschung. 1998 Jan;48(1):77-81.
REF 24Inhibitor of phospholipase A2 blocks eicosanoid and platelet activating factor biosynthesis and has topical anti-inflammatory activity. J Pharmacol Exp Ther. 1994 Nov;271(2):852-9.
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REF 38J 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.
REF 39Phagedena due to leishmaniasis. Immunologic and experimental studies. Ann Dermatol Syphiligr (Paris). 1976;103(1):23-30.
REF 40The effect of lipoprotein-associated phospholipase A2 deficiency on pulmonary allergic responses in Aspergillus fumigatus sensitized mice. Respir Res. 2012 Nov 12;13:100.
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REF 45Clocortolone pivalate: a paired comparison clinical trial of a new topical steroid in eczema/atopic dermatitis. Cutis. 1980 Jan;25(1):96-8.

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