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sPLA2-1B

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1416

Nomenclature: sPLA2-1B

Family: Phospholipase A2

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 148 12q24.31 PLA2G1B phospholipase A2 group IB
Mouse - 146 5 F Pla2g1b phospholipase A2, group IB, pancreas
Rat - 146 12q16 Pla2g1b phospholipase A2 group IB
Previous and Unofficial Names Click here for help
GIB | pancreatic PLA2 | PLA2 | PLA2A | PPLA2 | group IB phospholipase A2 | phospholipase A2 group IB pancreas | sPLA2IB | phospholipase A2, group IB (pancreas) | phospholipase A2, group IB, pancreas
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.1.1.4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 28xvii [PMID: 8809154] Small molecule or natural product Hs Inhibition 8.9 pIC50 1
pIC50 8.9 (IC50 1.3x10-9 M) [1]
Description: Measured using a chromogenic assay.
compound 12e [PMID: 18605714] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 3
pIC50 7.1 (IC50 8.4x10-8 M) [3]
Immunopharmacology Comments
sPLA2 enzymes catalyze the first step of the arachidonic acid pathway, so are inextricably involved in the production of arachadonic acid for inflammatory mediator synthesis. Excess sPLA2 activity is suggested to contribute to several inflammatory diseases. The sPLA2-1B isozyme has been reported to induce leukotriene B4 (LTB4) production in human neutrophils, using a mechanism independent of arachadonic acid generation [2].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0002227 innate immune response in mucosa IDA
GO:0030593 neutrophil chemotaxis ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050778 positive regulation of immune response ISS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0032637 interleukin-8 production ISS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0030593 neutrophil chemotaxis ISS

References

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1. Hagishita S, Yamada M, Shirahase K, Okada T, Murakami Y, Ito Y, Matsuura T, Wada M, Kato T, Ueno M et al.. (1996) Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives. J. Med. Chem., 39 (19): 3636-58. [PMID:8809154]

2. Lee HY, Kim MK, Park KS, Shin EH, Bae YS. (2005) Group IB secretory phospholipase A2 stimulates leukotriene B4 production by a unique mechanism in human neutrophils. Biochem. Biophys. Res. Commun., 334 (2): 500-8. [PMID:16005851]

3. Oslund RC, Cermak N, Gelb MH. (2008) Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. J. Med. Chem., 51 (15): 4708-14. [PMID:18605714]

How to cite this page

Phospholipase A2: sPLA2-1B. Last modified on 16/02/2017. Accessed on 19/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1416.