sPLA<sub>2</sub>-1B | Phospholipase A<sub>2</sub> | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

sPLA₂-1B

Target id: 1416

Nomenclature: sPLA₂-1B

Gene and Protein Information
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
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
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

EC Number: 3.1.1.4

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Inhibitors

Key to terms and symbols

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Ligand		Sp.	Action	Value	Parameter	Reference
compound 28xvii [PMID: 8809154]		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]		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].

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]