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 Arthritis [ICD9: 710-719; ICD10: M00-M25]
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]
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 [541327]
Clobetasol Drug Info Approved Inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp [551871]
Clocortolone Drug Info Approved Inflammatory and pruritic manifestations of moderate to severe corticosteroid-responsive dermatoses of the scalp [551871]
Diflorasone Drug Info Approved Inflammatory and pruritic manifestations of corticosteroid responsive dermatoses [551871]
Miltefosine Drug Info Approved Leishmaniasis [533123]
AllerB Drug Info Phase 2b Allergy [550258]
MANOALIDE Drug Info Phase 2 Arthritis [531035]
Miltefosine Drug Info Phase 2 Visceral leishmaniasis [537364]
MRX-4 Drug Info Phase 2 Allergic rhinitis [548571]
MRX-6 Drug Info Phase 2 Contact dermatitis [524592]
Rilapladib Drug Info Phase 1 Arteriosclerosis [542396], [547694]
Darapladib Drug Info Discontinued in Phase 3 Arteriosclerosis [541801], [547463]
BMY-30129 Drug Info Discontinued in Phase 2 Pruritus [545846]
EPC-K1 Drug Info Discontinued in Phase 2 Nerve injury [546374]
SC-106 Drug Info Discontinued in Phase 2 Rheumatoid arthritis [546279]
WAY-123641 Drug Info Discontinued in Phase 2 Asthma [545618]
PF-05212372 Drug Info Discontinued in Phase 1 Asthma [523586]
SB-435495 Drug Info Discontinued in Phase 1 Arteriosclerosis [547355]
YM-26734 Drug Info Terminated Rheumatoid arthritis [545954]
Inhibitor 2-Methyl-2,4-Pentanediol Drug Info [551393]
3,9-dihydroxy-2,10-diprenylpterocap-6a-ene Drug Info [551368]
4'-hydroxy-6,3',5'-triprenylisoflavonone Drug Info [551368]
ABYSSINONE V Drug Info [551368]
Acetate Ion Drug Info [551393]
AllerB Drug Info [534658]
Alpha-D-Mannose Drug Info [551393]
BM-162115 Drug Info [534587]
BMY-30129 Drug Info [533821], [551871]
BOLINAQUINONE Drug Info [526069]
CACOSPONGIONOLIDE Drug Info [534672]
CACOSPONGIONOLIDE B Drug Info [534672]
Cacospongionolide E Drug Info [534672]
Cholic Acid Drug Info [551393]
Clobetasol Drug Info [537809]
Diflorasone Drug Info [536938]
EPC-K1 Drug Info [533699], [551871]
HELENAQUINONE Drug Info [531037]
Heptanoic Acid Drug Info [551374]
Hexane-1,6-Diol Drug Info [551393]
HYRTIOSULAWESINE Drug Info [528597]
Lpc-Ether Drug Info [551393]
LY178002 Drug Info [537683]
Mepacrine Drug Info [536930]
Miltefosine Drug Info [537364]
MRX-4 Drug Info [551190]
MRX-6 Drug Info [528718]
N-Tridecanoic Acid Drug Info [551374]
P-Anisic Acid Drug Info [551393]
Petrosaspongiolide M Drug Info [528771]
Petrosaspongiolide P Drug Info [534632]
PF-05212372 Drug Info [533816]
Pyruvoyl Group Drug Info [551393]
SB-435495 Drug Info [532111]
SC-106 Drug Info [550919]
URSOLIC ACID Drug Info [527616]
WAY-123641 Drug Info [533904]
Modulator AGN-190383 Drug Info
Darapladib Drug Info [552985]
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 [537815]
Binder LY256548 Drug Info [537683]
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
Ref 523586ClinicalTrials.gov (NCT01415102) A First In Human Study In Healthy People To Evaluate Safety, Toleration And Time Course Of Plasma Concentration Of Single Inhaled Doses Of PF-05212372.. U.S. NationalInstitutes of Health.
Ref 524592ClinicalTrials.gov (NCT02031445) Double-Blind, Trial to Evaluate the Safety and Efficacy of MRX-6 Cream 2%. U.S. National Institutes of Health.
Ref 531035In situ aquaculture methods for Dysidea avara (Demospongiae, Porifera) in the northwestern Mediterranean. Mar Drugs. 2010 May 26;8(6):1731-42.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 537364Novel 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.
Ref 541327(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 609).
Ref 541801(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6696).
Ref 542396(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7376).
Ref 545618Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003918)
Ref 545846Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005019)
Ref 545954Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005488)
Ref 546279Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007225)
Ref 546374Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007770)
Ref 547355Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015443)
Ref 547463Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016591)
Ref 547694Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018454)
Ref 548571Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026713)
Ref 550258Clinical pipeline report, company report or official report of Anergis SA.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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 527616Bioorg Med Chem Lett. 2005 Sep 15;15(18):4100-4.Synthesis of benzoyl phenyl benzoates as effective inhibitors for phospholipase A2 and hyaluronidase enzymes.
Ref 528597J Nat Prod. 2006 Dec;69(12):1676-9.Hyrtiazepine, an azepino-indole-type alkaloid from the Red Sea marine sponge Hyrtios erectus.
Ref 528718A novel treatment of contact dermatitis by topical application of phospholipase A2 inhibitor: a double-blind placebo-controlled pilot study. Int J Immunopathol Pharmacol. 2007 Jan-Mar;20(1):191-5.
Ref 528771J 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.
Ref 531037Bioorg 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.
Ref 532111The effect of lipoprotein-associated phospholipase A2 deficiency on pulmonary allergic responses in Aspergillus fumigatus sensitized mice. Respir Res. 2012 Nov 12;13:100.
Ref 533699Posttreatment with EPC-K1, an inhibitor of lipid peroxidation and of phospholipase A2 activity, reduces functional deficits after global ischemia in rats. Brain Res Bull. 1995;36(3):257-60.
Ref 533816Phagedena due to leishmaniasis. Immunologic and experimental studies. Ann Dermatol Syphiligr (Paris). 1976;103(1):23-30.
Ref 533821Inhibitor 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.
Ref 533904Phosphodiesterase-IV inhibition, respiratory muscle relaxation and bronchodilation by WAY-PDA-641. J Pharmacol Exp Ther. 1994 Feb;268(2):888-96.
Ref 534587Investigation 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 534632J 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 534658Successful 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 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 536930Involvement of protein kinase C activation in L-leucine-induced stimulation of protein synthesis in l6 myotubes. Cytotechnology. 2003 Nov;43(1-3):97-103.
Ref 536938Structures from powders: diflorasone diacetate. Steroids. 2009 Jan;74(1):102-11. Epub 2008 Oct 18.
Ref 537364Novel 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.
Ref 537683The anti-inflammatory effects of LY178002 and LY256548. Agents Actions. 1989 Jun;27(3-4):300-2.
Ref 537809Utilization of epidermal phospholipase A2 inhibition to monitor topical steroid action. Br J Dermatol. 1984 Jul;111 Suppl 27:195-203.
Ref 537815Clocortolone pivalate: a paired comparison clinical trial of a new topical steroid in eczema/atopic dermatitis. Cutis. 1980 Jan;25(1):96-8.
Ref 550919US patent application no. 6,673,908, Tumor necrosis factor receptor 2.
Ref 551190Phospholipase A2, group IVA (cytosolic, calcium-dependent) (PLA2G4A). SciBX 1(41); doi:10.1038/scibx.2008.999. Nov. 13 2008
Ref 551368Phospholipase A2 Inhibitors from an Erythrina Species from Samoa J. Nat. Prod. 60(6):537-539 (1997).
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 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 552985Darapladib, a reversible lipoprotein-associated phospholipase A2 inhibitor, for the oral treatment of atherosclerosis and coronary artery disease. IDrugs. 2009 Oct;12(10):648-55.

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