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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

Contents:

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
Alphafold P04054 (Hs), Q9Z0Y2 (Mm), P04055 (Rn)
BRENDA 3.1.1.4
CATH/Gene3D 1.20.90.10
ChEMBL Target CHEMBL4426 (Hs), CHEMBL4378 (Mm), CHEMBL5016 (Rn)
DrugBank Target P04054 (Hs)
Ensembl Gene ENSG00000170890 (Hs), ENSMUSG00000029522 (Mm), ENSRNOG00000001153 (Rn)
Entrez Gene 5319 (Hs), 18778 (Mm), 29526 (Rn)
Human Protein Atlas ENSG00000170890 (Hs)
KEGG Enzyme 3.1.1.4
KEGG Gene hsa:5319 (Hs), mmu:18778 (Mm), rno:29526 (Rn)
OMIM 172410 (Hs)
Pharos P04054 (Hs)
UniProtKB P04054 (Hs), Q9Z0Y2 (Mm), P04055 (Rn)
Wikipedia PLA2G1B (Hs)
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
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration

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 09/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1416.