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PLA2G4B

gene
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Also known as cPLA2-betaHsT16992

Summary

PLA2G4B (phospholipase A2 group IVB, HGNC:9036) is a protein-coding gene on chromosome 15q15.1, encoding Cytosolic phospholipase A2 beta (P0C869). Calcium-dependent phospholipase A1 and A2 and lysophospholipase that may play a role in membrane phospholipid remodeling.

This gene encodes a member of the cytosolic phospholipase A2 protein family. Phospholipase A2 enzymes hydrolyze the sn-2 bond of phospholipids, releasing lysophospholipids and fatty acids. This enzyme may be associated with mitochondria and early endosomes. Most tissues also express read-through transcripts from the upstream gene into this gene, some of which may encode fusion proteins combining the N-terminus of the upstream gene including its JmjC domain with the almost complete coding region of this gene, including the C2 and cytoplasmic phospholipase A2 domains.

Source: NCBI Gene 100137049 — RefSeq curated summary.

At a glance

  • GWAS associations: 5
  • Clinical variants (ClinVar): 1 total
  • Druggable target: yes
  • MANE Select transcript: NM_001114633

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9036
Approved symbolPLA2G4B
Namephospholipase A2 group IVB
Location15q15.1
Locus typegene with protein product
StatusApproved
AliasescPLA2-beta, HsT16992
Ensembl geneENSG00000243708
Ensembl biotypeprotein_coding
OMIM606088
Entrez100137049

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 4 protein_coding, 3 retained_intron

ENST00000452633, ENST00000458483, ENST00000461382, ENST00000483748, ENST00000566076, ENST00000569354, ENST00000880478

RefSeq mRNA: 1 — MANE Select: NM_001114633 NM_001114633

CCDS: CCDS45241

Canonical transcript exons

ENST00000458483 — 20 exons

ExonStartEnd
ENSE000035787004183884741838922
ENSE000037026754184447141844607
ENSE000037037094184105541841095
ENSE000037037724184181941841949
ENSE000037050254184052441840660
ENSE000037050454184733741847523
ENSE000037052304184123141841273
ENSE000037056044184255441842591
ENSE000037059284184484841845070
ENSE000037059564184620341846382
ENSE000037059954184666941846835
ENSE000037060384184563841845775
ENSE000037069154184015841840230
ENSE000037089584184077441840905
ENSE000037090694184594341846047
ENSE000037091054184367641843811
ENSE000037094594184151741841571
ENSE000037095384184219341842276
ENSE000037096004184520341845320
ENSE000039104814184764941848143

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 95.95.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1544 / max 27.8128, expressed in 42 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
14621410.08231763
1462150.117538
1462160.036918

Top tissues by expression

134 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
lower esophagus mucosaUBERON:003583495.95gold quality
right hemisphere of cerebellumUBERON:001489095.50gold quality
cerebellar cortexUBERON:000212995.38gold quality
cerebellar hemisphereUBERON:000224595.34gold quality
cerebellumUBERON:000203795.26gold quality
skin of abdomenUBERON:000141692.91gold quality
zone of skinUBERON:000001492.15gold quality
skin of legUBERON:000151191.75gold quality
esophagus mucosaUBERON:000246990.57gold quality
vaginaUBERON:000099689.12gold quality
ectocervixUBERON:001224987.54gold quality
granulocyteCL:000009486.77gold quality
primary visual cortexUBERON:000243686.57gold quality
right lobe of thyroid glandUBERON:000111986.22gold quality
thyroid glandUBERON:000204686.15gold quality
left lobe of thyroid glandUBERON:000112085.98gold quality
apex of heartUBERON:000209885.91gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099185.82gold quality
pituitary glandUBERON:000000785.62gold quality
left ovaryUBERON:000211985.55gold quality
uterine cervixUBERON:000000284.83gold quality
esophagusUBERON:000104384.74gold quality
adenohypophysisUBERON:000219684.51gold quality
right frontal lobeUBERON:000281084.48gold quality
right ovaryUBERON:000211884.31gold quality
prostate glandUBERON:000236784.28gold quality
ovaryUBERON:000099283.93gold quality
endocervixUBERON:000045883.79gold quality
right uterine tubeUBERON:000130283.78gold quality
minor salivary glandUBERON:000183083.68gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no0.69

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

12 targeting PLA2G4B, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-467999.7669.191229
HSA-MIR-6716-5P99.5668.621244
HSA-MIR-317199.4969.06776
HSA-MIR-314998.7767.131639
HSA-MIR-126298.1766.52757
HSA-MIR-4701-3P98.1766.25788
HSA-MIR-6736-5P98.1766.43760
HSA-MIR-7113-5P97.8867.331735
HSA-MIR-92497.7866.21681
HSA-MIR-627-5P95.5166.80509
HSA-MIR-319794.0263.4785
HSA-MIR-4520-5P93.5465.23140

Literature-anchored findings (GeneRIF, showing 2)

  • TLR2 cooperates with MyD88, PI3K, and Rac1 in lipoteichoic acid-induced cPLA2/COX-2-dependent airway inflammatory responses (PMID:20167866)
  • JMJD7-PLA2G4B may serve as an important therapeutic target and prognostic marker for head and neck squamous cell carcinoma development and progression. (PMID:28030848)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriopla2g4f.1ENSDARG00000056535
danio_reriopla2g4f.2ENSDARG00000070953
mus_musculusPla2g4bENSMUSG00000098488
rattus_norvegicusPla2g4bENSRNOG00000007447

Paralogs (5): PLA2G4C (ENSG00000105499), PLA2G4A (ENSG00000116711), PLA2G4D (ENSG00000159337), PLA2G4F (ENSG00000168907), PLA2G4E (ENSG00000188089)

Protein

Protein identifiers

Cytosolic phospholipase A2 beta — P0C869 (reviewed: P0C869)

Alternative names: Lysophospholipase A1 group IVB, Phospholipase A2 group IVB

All UniProt accessions (2): P0C869, H3BSX5

UniProt curated annotations — full annotation on UniProt →

Function. Calcium-dependent phospholipase A1 and A2 and lysophospholipase that may play a role in membrane phospholipid remodeling. Calcium-dependent phospholipase A2 and lysophospholipase. Cleaves the ester bond of the fatty acyl group attached to the sn-2 position of phosphatidylethanolamines, producing lysophospholipids that may be used in deacylation-reacylation cycles. Hydrolyzes lysophosphatidylcholines with low efficiency but is inefficient toward phosphatidylcholines. Calcium-dependent phospholipase A1 and A2 and lysophospholipase. Cleaves the ester bond of the fatty acyl group attached to the sn-1 or sn-2 position of diacyl phospholipids (phospholipase A1 and A2 activity, respectively), producing lysophospholipids that may be used in deacylation-reacylation cycles. Can further hydrolyze lysophospholipids enabling complete deacylation. Has no activity toward alkylacyl phospholipids.

Subcellular location. Cytoplasm. Cytosol. Mitochondrion membrane. Early endosome membrane Cytoplasm.

Tissue specificity. Widely expressed. Expressed at higher level in brain, heart, liver, cerebellum and pancreas.

Activity regulation. Stimulated by cytosolic Ca(2+).

Domain organisation. The N-terminal C2 domain associates with lipid membranes upon calcium binding. It modulates enzyme activity by presenting the active site to its substrate in response to elevations of cytosolic Ca(2+).

Miscellaneous. Based on a naturally occurring readthrough transcript which produces a JMJD7-PLA2G4B fusion protein. Based on a naturally occurring readthrough transcript which produces a JMJD7-PLA2G4B fusion protein. Based on a naturally occurring readthrough transcript which produces a JMJD7-PLA2G4B fusion protein.

Isoforms (5)

UniProt IDNamesCanonical?
P0C869-11yes
P0C869-72, beta2
P0C869-83, beta3
P0C869-44
P0C869-65, Beta1

RefSeq proteins (1): NP_001108105* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000008C2_domDomain
IPR002642LysoPLipase_cat_domDomain
IPR016035Acyl_Trfase/lysoPLipaseHomologous_superfamily
IPR035892C2_domain_sfHomologous_superfamily
IPR040723cPLA2_C2Domain
IPR041847C2_cPLA2Domain

Pfam: PF00168, PF01735, PF18695

Catalyzed reactions (Rhea), 7 shown:

  • a 1-acyl-sn-glycero-3-phosphocholine + H2O = sn-glycerol 3-phosphocholine + a fatty acid + H(+) (RHEA:15177)
  • a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 1-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:15801)
  • 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40427)
  • 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40431)
  • 1-hexadecanoyl-sn-glycero-3-phosphocholine + H2O = sn-glycerol 3-phosphocholine + hexadecanoate + H(+) (RHEA:40435)
  • 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphocholine + H2O = 2-(5Z,8Z,11Z,14Z)-eicosatetraenoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:40571)
  • 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (9Z,12Z)-octadecadienoate + H(+) (RHEA:40815)

UniProt features (32 total): binding site 8, sequence conflict 6, splice variant 5, sequence variant 4, mutagenesis site 4, domain 2, active site 2, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P0C869-F187.390.63

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (2): 335 (nucleophile); 615 (proton acceptor)

Ligand- & substrate-binding residues (8): 84; 84; 90; 26; 26; 32; 82; 82

Mutagenesis-validated functional residues (4):

PositionPhenotype
335abolishes enzyme activity.
417no effect.
615abolishes enzyme activity.
632abolishes enzyme activity.

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

IDPathway
R-HSA-1482788Acyl chain remodelling of PC
R-HSA-1482801Acyl chain remodelling of PS
R-HSA-1482839Acyl chain remodelling of PE
R-HSA-1482925Acyl chain remodelling of PG
R-HSA-1483115Hydrolysis of LPC
R-HSA-1483166Synthesis of PA
R-HSA-381038XBP1(S) activates chaperone genes

MSigDB gene sets: 100 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, REACTOME_UNFOLDED_PROTEIN_RESPONSE_UPR, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_INFLAMMATORY_RESPONSE, KEGG_MAPK_SIGNALING_PATHWAY, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_LONG_CHAIN_FATTY_ACID_METABOLIC_PROCESS, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLGLYCEROL_METABOLIC_PROCESS, KEGG_FC_EPSILON_RI_SIGNALING_PATHWAY, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_PARTURITION, GOCC_MITOCHONDRIAL_ENVELOPE, GOBP_ORGANOPHOSPHATE_CATABOLIC_PROCESS, GOBP_GLYCEROPHOSPHOLIPID_METABOLIC_PROCESS

GO Biological Process (12): inflammatory response (GO:0006954), parturition (GO:0007567), arachidonate metabolic process (GO:0019369), calcium-mediated signaling (GO:0019722), phosphatidylglycerol acyl-chain remodeling (GO:0036148), phosphatidylcholine acyl-chain remodeling (GO:0036151), phosphatidylethanolamine acyl-chain remodeling (GO:0036152), glycerophospholipid catabolic process (GO:0046475), lipid metabolic process (GO:0006629), glycerophospholipid metabolic process (GO:0006650), phospholipid catabolic process (GO:0009395), lipid catabolic process (GO:0016042)

GO Molecular Function (9): phosphatidylcholine lysophospholipase A1 activity (GO:0004622), A2-type glycerophospholipase activity (GO:0004623), calcium ion binding (GO:0005509), calcium-dependent phospholipid binding (GO:0005544), glycerophospholipid phospholipase A1 activity (GO:0008970), obsolete calcium-dependent phospholipase A2 activity (GO:0047498), glycerophospholipase activity (GO:0004620), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (9): extracellular region (GO:0005576), mitochondrial inner membrane (GO:0005743), cytosol (GO:0005829), early endosome membrane (GO:0031901), cytoplasm (GO:0005737), mitochondrion (GO:0005739), endosome (GO:0005768), membrane (GO:0016020), mitochondrial membrane (GO:0031966)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Glycerophospholipid biosynthesis6
IRE1alpha activates chaperones1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
phosphatidylcholine metabolic process2
phospholipid metabolic process2
cytoplasm2
defense response1
multi-organism reproductive process1
multi-multicellular organism process1
long-chain fatty acid metabolic process1
icosanoid metabolic process1
unsaturated fatty acid metabolic process1
olefinic compound metabolic process1
intracellular signaling cassette1
phosphatidylglycerol metabolic process1
glycerophospholipid metabolic process1
phospholipid catabolic process1
glycerolipid catabolic process1
primary metabolic process1
glycerolipid metabolic process1
lipid catabolic process1
organophosphate catabolic process1
lipid metabolic process1
catabolic process1
lysophospholipase A1 activity1
glycerophospholipase activity1
carboxylic ester hydrolase activity1
metal ion binding1
phospholipid binding1
A1-type glycerophospholipase activity1
phospholipase activity1
catalytic activity1
cation binding1
organelle inner membrane1
mitochondrial membrane1
early endosome1
endosome membrane1
intracellular anatomical structure1
intracellular membrane-bounded organelle1
endomembrane system1
cytoplasmic vesicle1
mitochondrion1

Protein interactions and networks

STRING

616 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PLA2G4BPLA2G5P39877849
PLA2G4BYIF1AO95070465
PLA2G4BPLA2G3Q9NZ20427
PLA2G4BPLA2G2FQ9BZM2424
PLA2G4BJMJD7P0C870411
PLA2G4BANKRD31Q8N7Z5403
PLA2G4BPLA2G12AQ9BZM1380
PLA2G4BCDIPTO14735373
PLA2G4BPLA2G2AP14555370
PLA2G4BPLA2G6O60733358
PLA2G4BPDZD9Q8IXQ8346
PLA2G4BCYP4F22Q6NT55343
PLA2G4BPLA2G4CQ9UP65342
PLA2G4BPLA2G10O15496340
PLA2G4BA0A087WUM3A0A087WUM3336

IntAct

19 interactions, top by confidence:

ABTypeScore
PLA2G4BTFAP2Apsi-mi:“MI:0915”(physical association)0.370
PLEKHG3psi-mi:“MI:0914”(association)0.350
SRRTA2ML1psi-mi:“MI:0914”(association)0.350
STX17A2ML1psi-mi:“MI:0914”(association)0.350
OR2A4A2ML1psi-mi:“MI:0914”(association)0.350
GOT1A2ML1psi-mi:“MI:0914”(association)0.350
PPP2R2BA2ML1psi-mi:“MI:0914”(association)0.350
CCR1UBA6psi-mi:“MI:0914”(association)0.350
SSUH2IGLC7psi-mi:“MI:0914”(association)0.350
FNDC5A2ML1psi-mi:“MI:0914”(association)0.350
AGPAT1A2ML1psi-mi:“MI:0914”(association)0.350
MBNL1A2ML1psi-mi:“MI:0914”(association)0.350
MYCBPA2ML1psi-mi:“MI:0914”(association)0.350
SMPD2A2ML1psi-mi:“MI:0914”(association)0.350
DISC1PLA2G4Bpsi-mi:“MI:0915”(physical association)0.000
PLA2G4BuvrBpsi-mi:“MI:0915”(physical association)0.000
sdhAPLA2G4Bpsi-mi:“MI:0915”(physical association)0.000
LCORPLA2G4Bpsi-mi:“MI:0915”(physical association)0.000

BioGRID (26): JMJD7-PLA2G4B (Two-hybrid), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), PLA2G4B (Reconstituted Complex), PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS), JMJD7-PLA2G4B (Affinity Capture-MS)

ESM2 similar proteins: A0A8C2MDK8, A0PJX2, A2ACG1, B3DLB3, D3ZBP4, F1MH07, O75038, P0C869, P0DPD7, P0DPE1, P10688, P10895, P21671, P21709, P51178, Q0IID2, Q1LWV7, Q2KJ24, Q3U2A8, Q4KM32, Q4R380, Q4R6L3, Q5RET0, Q5RKI3, Q5ST30, Q5TM74, Q60750, Q684M2, Q68DD2, Q6MG21, Q6NVG1, Q6ZSI9, Q767M3, Q86U10, Q86XP0, Q8C9V1, Q8K3R3, Q8NFF5, Q8R3B1, Q8SPR7

Diamond homologs: A0JJX5, A1CQG2, A1ZBD6, A2QQ28, A3KGK3, A4IFJ5, A6QQP7, A8KBH6, B1WAZ6, B8N7E5, G0S9J5, O14065, O14795, O43581, O75131, O75923, O94812, P04409, P05126, P05128, P05129, P05696, P05771, P05772, P0C869, P0C871, P10102, P10829, P13677, P17252, P20444, P21521, P27715, P29101, P41823, P41885, P46097, P46935, P49147, P63318

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

1 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance0
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

3441 predictions. Top by Δscore:

VariantEffectΔscore
15:41840837:G:GGdonor_gain1.0000
15:41840869:G:GTdonor_gain1.0000
15:41840869:G:Tdonor_gain1.0000
15:41841092:GTCT:Gdonor_gain1.0000
15:41841096:G:GGdonor_gain1.0000
15:41842188:TGCA:Tacceptor_loss1.0000
15:41842189:GCA:Gacceptor_loss1.0000
15:41842190:CAG:Cacceptor_loss1.0000
15:41842191:A:ACacceptor_loss1.0000
15:41842191:A:AGacceptor_gain1.0000
15:41842191:AG:Aacceptor_gain1.0000
15:41842192:G:GGacceptor_gain1.0000
15:41842192:G:GTacceptor_loss1.0000
15:41842192:GG:Gacceptor_gain1.0000
15:41842192:GGAT:Gacceptor_gain1.0000
15:41842243:TC:Tdonor_gain1.0000
15:41842247:GTG:Gdonor_gain1.0000
15:41843669:C:Aacceptor_gain1.0000
15:41843669:C:CAacceptor_gain1.0000
15:41843671:GCCAG:Gacceptor_loss1.0000
15:41843672:CCAGA:Cacceptor_loss1.0000
15:41843673:CAGAC:Cacceptor_loss1.0000
15:41843674:A:AGacceptor_gain1.0000
15:41843674:AG:Aacceptor_loss1.0000
15:41843675:G:GGacceptor_gain1.0000
15:41843675:GA:Gacceptor_gain1.0000
15:41843675:GACT:Gacceptor_gain1.0000
15:41843803:GAGGA:Gdonor_gain1.0000
15:41843806:G:GTdonor_gain1.0000
15:41843809:G:GTdonor_gain1.0000

AlphaMissense

5058 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
15:41846755:A:CS623R0.993
15:41846757:C:AS623R0.993
15:41846757:C:GS623R0.993
15:41843745:G:CR271S0.989
15:41843745:G:TR271S0.989
15:41844879:T:AW350R0.989
15:41844879:T:CW350R0.989
15:41845649:T:CF457L0.987
15:41845651:C:AF457L0.987
15:41845651:C:GF457L0.987
15:41845948:T:AW501R0.987
15:41845948:T:CW501R0.987
15:41840619:T:AW60R0.985
15:41840619:T:CW60R0.985
15:41843744:G:TR271M0.985
15:41845718:T:CF480L0.985
15:41845720:C:AF480L0.985
15:41845720:C:GF480L0.985
15:41843744:G:CR271T0.984
15:41845640:T:AW454R0.983
15:41845640:T:CW454R0.983
15:41846732:A:TD615V0.983
15:41840621:G:CW60C0.981
15:41840621:G:TW60C0.981
15:41844606:T:AW339R0.979
15:41844606:T:CW339R0.979
15:41844881:G:CW350C0.979
15:41844881:G:TW350C0.979
15:41845650:T:CF457S0.977
15:41845035:T:AW402R0.976

dbSNP variants (sampled 300 via entrez): RS1000139128 (15:41846914 G>A), RS1000200930 (15:41841488 G>A,C), RS1000379775 (15:41846602 T>C), RS1000581476 (15:41843583 A>G), RS1000655610 (15:41842684 C>A,T), RS1000693798 (15:41847808 T>G), RS1000874167 (15:41839246 G>T), RS1001213298 (15:41840466 G>A), RS1001355946 (15:41846179 A>C,G), RS1001382280 (15:41844702 A>G), RS1001808219 (15:41846053 T>C,G), RS1002095040 (15:41843406 G>GCCTGGGGGCCTGTCTGCA), RS1002156036 (15:41838073 C>T), RS1002255325 (15:41844486 A>C,G), RS1002437258 (15:41848346 A>G)

Disease associations

OMIM: gene MIM:606088 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

5 associations (top):

StudyTraitp-value
GCST90020024_483A body shape index3.000000e-09
GCST90020025_142Waist-to-hip ratio adjusted for BMI2.000000e-08
GCST90020025_450Waist-to-hip ratio adjusted for BMI1.000000e-09
GCST90020027_628Waist-hip index1.000000e-09
GCST90020027_629Waist-hip index1.000000e-08

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0007789BMI-adjusted waist circumference
EFO:0007788BMI-adjusted waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4136 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Phospholipase A2

ChEMBL bioactivities

51 potent at pChembl≥5 of 59 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.40IC504nMCHEMBL29838
8.10IC508nMCHEMBL30108
7.77IC5017nMCHEMBL26200
7.70IC5020nMCHEMBL286067
7.58IC5026nMCHEMBL418207
7.52IC5030nMCHEMBL30108
7.52IC5030nMCHEMBL29515
7.46IC5035nMCHEMBL286068
7.40IC5040nMCHEMBL29353
7.34IC5046nMCHEMBL282164
7.32IC5048nMCHEMBL30130
7.30IC5050nMCHEMBL30107
7.22IC5060nMCHEMBL29247
7.22IC5060nMCHEMBL29246
7.16IC5070nMCHEMBL285344
7.13IC5074nMCHEMBL25900
7.10IC5080nMCHEMBL29838
6.92IC50120nMCHEMBL286067
6.82IC50150nMCHEMBL27479
6.82IC50150nMCHEMBL286068
6.82IC50150nMCHEMBL26200
6.70IC50200nMCHEMBL29246
6.62IC50240nMCHEMBL27245
6.57IC50270nMCHEMBL25853
6.55IC50280nMCHEMBL413539
6.40IC50400nMCHEMBL283294
6.39IC50410nMCHEMBL282164
6.34IC50460nMCHEMBL30130
6.30IC50500nMCHEMBL29807
6.18IC50660nMCHEMBL281320
6.16IC50690nMCHEMBL27531
6.16IC50700nMCHEMBL282634
6.10IC50800nMARACHIDONYL TRIFLUOROMETHYLKETONE
6.00IC501000nMCHEMBL27534
5.92IC501200nMCHEMBL29859
5.92IC501200nMCHEMBL442099
5.89IC501300nMCHEMBL416027
5.85IC501400nMCHEMBL29552
5.85IC501400nMCHEMBL284224
5.72IC501900nMCHEMBL27478
5.70IC502000nMCHEMBL27531
5.66IC502200nMCHEMBL30198
5.66IC502200nMCHEMBL25853
5.64IC502300nMCHEMBL29674
5.48IC503300nMCHEMBL281320
5.44IC503600nMCHEMBL29393
5.37IC504300nMCHEMBL29707
5.34IC504600nMCHEMBL413539
5.28IC505300nMCHEMBL29987
5.19IC506500nMCHEMBL442099

PubChem BioAssay actives

102 with measured affinity, of 142 total; 37 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
4-[2-oxo-3-[4-(5-phenylpentylsulfanyl)phenoxy]propoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0040uM
4-[3-(4-decoxyphenoxy)-2-oxopropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0080uM
2-[4-[3-(4-decoxyphenoxy)-2-oxopropoxy]phenyl]acetic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0170uM
4-[3-(4-decoxyphenoxy)-2-oxopropoxy]-3-nitrobenzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0200uM
4-[3-(4-dodecoxyphenoxy)-2-oxopropoxy]benzoic acid158952: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by soluble assayic500.0260uM
5-[3-(4-decoxyphenoxy)-2-oxopropoxy]pentanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0300uM
3-[[3-(4-decoxyphenoxy)-2-oxopropoxy]methyl]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0350uM
4-[[3-(4-decoxyphenoxy)-2-oxopropoxy]methyl]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0400uM
4-[3-(4-octoxyphenoxy)-2-oxopropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0460uM
4-[2-oxo-3-[4-(5-phenylpentoxy)phenoxy]propoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0480uM
3-[3-(4-decoxyphenoxy)-2-oxopropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0500uM
2-[3-[3-(4-decoxyphenoxy)-2-oxopropoxy]phenoxy]acetic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0600uM
2-[3-[3-(4-decoxyphenoxy)-2-oxopropoxy]phenyl]acetic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0600uM
5-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfanylpentanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0700uM
4-[3-(4-decoxyphenoxy)-2-oxopropoxy]-3-methoxybenzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.0740uM
4-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfanylbutanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.1500uM
4-[3-(4-decoxyphenoxy)-2-oxopropoxy]butanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.2400uM
3-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.2700uM
4-[3-(4-hexoxyphenoxy)-2-oxopropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.2800uM
3-[2-oxo-3-(4-tetradecoxyphenoxy)propyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.4000uM
3-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfonylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.5000uM
2-[3-[3-[(4-decoxyphenyl)methoxy]-2-oxopropoxy]phenyl]acetic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.6600uM
3-[4-(4-decoxyphenyl)-2-oxobutoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.6900uM
3-[3-(3-decoxyphenoxy)-2-oxopropyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic500.7000uM
(6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one158952: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by soluble assayic500.8000uM
3-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfinylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.0000uM
3-[3-(4-decoxyphenoxy)-2-oxopropoxy]propanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.2000uM
4-[3-oxo-4-[4-(5-phenylpentylsulfanyl)phenoxy]butyl]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.2000uM
4-[3-(4-decoxyphenoxy)-2-hydroxypropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.3000uM
2-[3-(4-decoxyphenoxy)-2-oxopropyl]sulfanylacetic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.4000uM
3-[3-(2-decoxyphenoxy)-2-oxopropyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.4000uM
3-[3-(4-decoxyphenoxy)propylsulfanyl]propanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic501.9000uM
4-[2-oxo-3-(4-phenylmethoxyphenoxy)propoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic502.2000uM
3-[3-[4-(naphthalen-2-ylmethoxy)phenoxy]-2-oxopropyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic502.3000uM
3-[3-(4-decoxyphenoxy)-2-hydroxypropyl]sulfanylpropanoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic503.6000uM
4-[3-(4-butoxyphenoxy)-2-oxopropoxy]benzoic acid158951: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assayic504.3000uM
4-[3-[4-[(4-nitrophenyl)methoxy]phenoxy]-2-oxopropoxy]benzoic acid158952: Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by soluble assayic505.3000uM

CTD chemical–gene interactions

22 total (human), top 22 by PubMed support.

ChemicalActions (top 5)PubMed papers
Tobacco Smoke Pollutiondecreases expression, decreases methylation2
2,5,2’,5’-tetrachlorobiphenyldecreases expression1
cypermethrinincreases expression1
beta-methylcholineaffects expression1
ICG 001increases expression1
jinfukangaffects cotreatment, increases expression1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acidincreases expression1
Atrazineincreases expression1
Cisplatinaffects cotreatment, increases expression1
Gasolineaffects cotreatment, increases abundance, increases expression1
Polycyclic Aromatic Hydrocarbonsaffects cotreatment, increases abundance, increases expression1
Smokedecreases expression1
Tunicamycinincreases expression1
Urethanedecreases expression1
Valproic Acidincreases methylation1
Sodium Seleniteincreases expression1
Cadmium Chlorideincreases expression1
Okadaic Aciddecreases expression1
1-Butanolaffects cotreatment, increases abundance, increases expression1
Acrylamidedecreases expression1
S-Nitrosoglutathioneincreases expression1
Particulate Matteraffects cotreatment, increases abundance, increases expression1

ChEMBL screening assays

5 unique, capped per target: 5 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4626965BindingInhibition of human PLA2G4B expressed in HEK293T cell lysates at 10 uM preincubated for 30 mins followed by FP-TAMRA addition and measured after 20 mins by SDS-PAGE based competitive ABPP analysisStructure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family. — J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_TE12HAP1 PLA2G4B (-) 1Cancer cell lineMale
CVCL_TE13HAP1 PLA2G4B (-) 2Cancer cell lineMale

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 79

This page pulls from 79 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot