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Atlas / Gene / PLA2G10

PLA2G10

gene
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Also known as GXPLA2

Summary

PLA2G10 (phospholipase A2 group X, HGNC:9029) is a protein-coding gene on chromosome 16p13.12, encoding Group 10 secretory phospholipase A2 (O15496). Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids. It is a selective cancer dependency (DepMap: 33.3% of cell lines).

This gene encodes a member of the phospholipase A2 family of proteins. Alternative splicing results in multiple transcript variants, at least one of which encodes a preproprotein that is proteolytically processed to generate the mature enzyme. This calcium-dependent enzyme hydrolyzes glycerophospholipids to produce free fatty acids and lysophospholipids. In one example, this enzyme catalyzes the release of arachidonic acid from cell membrane phospholipids, thus playing a role in the production of various inflammatory lipid mediators, such as prostaglandins. The encoded protein may promote the survival of breast cancer cells through its role in lipid metabolism.

Source: NCBI Gene 8399 — RefSeq curated summary.

At a glance

  • GWAS associations: 1
  • Clinical variants (ClinVar): 10 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • Cancer dependency (DepMap): dependent in 33.3% of screened cell lines
  • MANE Select transcript: NM_003561

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9029
Approved symbolPLA2G10
Namephospholipase A2 group X
Location16p13.12
Locus typegene with protein product
StatusApproved
AliasesGXPLA2
Ensembl geneENSG00000069764
Ensembl biotypeprotein_coding
OMIM603603
Entrez8399

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 1 protein_coding, 1 nonsense_mediated_decay

ENST00000438167, ENST00000567462

RefSeq mRNA: 1 — MANE Select: NM_003561 NM_003561

CCDS: CCDS10555

Canonical transcript exons

ENST00000438167 — 4 exons

ExonStartEnd
ENSE000015941741469049514690645
ENSE000016175361468816514688271
ENSE000017916931469413314694308
ENSE000019259761467254814672749

Expression profiles

Bgee: expression breadth ubiquitous, 129 present calls, max score 95.38.

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
mucosa of transverse colonUBERON:000499195.38gold quality
rectumUBERON:000105290.42gold quality
transverse colonUBERON:000115784.86gold quality
olfactory segment of nasal mucosaUBERON:000538684.76gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047380.10silver quality
duodenumUBERON:000211479.43gold quality
right uterine tubeUBERON:000130278.82gold quality
right lungUBERON:000216778.46gold quality
body of stomachUBERON:000116177.67gold quality
small intestine Peyer’s patchUBERON:000345476.58gold quality
body of pancreasUBERON:000115076.53gold quality
upper lobe of left lungUBERON:000895276.35gold quality
small intestineUBERON:000210874.77gold quality
stomachUBERON:000094574.55gold quality
gall bladderUBERON:000211074.29gold quality
intestineUBERON:000016072.82gold quality
fundus of stomachUBERON:000116072.57gold quality
colonUBERON:000115572.32gold quality
lungUBERON:000204871.59gold quality
pancreasUBERON:000126471.00gold quality
mucosa of stomachUBERON:000119969.21gold quality
vermiform appendixUBERON:000115467.49gold quality
fallopian tubeUBERON:000388966.57gold quality
right testisUBERON:000453466.06gold quality
left testisUBERON:000453365.97gold quality
testisUBERON:000047364.98gold quality
placentaUBERON:000198763.35gold quality
islet of LangerhansUBERON:000000662.32gold quality
putamenUBERON:000187460.12gold quality
smooth muscle tissueUBERON:000113559.68gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes16.63

Regulation

Is transcription factor: no

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 33.3% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 36)

  • circulating human neutrophils express groups V and X sPLA(2) (GV and GX sPLA(2)) mRNA and contain GV and GX sPLA(2) proteins, whereas GIB, GIIA, GIID, GIIE, GIIF, GIII, and GXII sPLA(2)s are undetectable (PMID:11741884)
  • LDL modification by GXPLA2 (PMID:12021277)
  • Expressed in human colorectal adenocarcinomas (PMID:12048163)
  • crystal structure of human group X secreted phospholipase A2 (PMID:12161451)
  • Modifies lipoproteins, which are involved in the pathogenesis of atherosclerosis (review) (PMID:12664556)
  • Group V sPLA2 may play an important role in promoting atherosclerotic lesion development by modifying LDL particles in the arterial wall, thereby enhancing particle aggregation, retention, and macrophage uptake. (PMID:14962950)
  • Stable expression of human groups IIA and X secreted phospholipases A(2) (hGIIA and hGX) in CHO-K1 and HEK293 cells leads to serum- and interleukin-1beta-promoted arachidonate release. (PMID:15007070)
  • group X secreted phospholipase A2 is expressed in neural cells and has neuritogenic action (PMID:15781456)
  • Recombinant hGX sPLA2 can efficiently hydrolyze PAF unlike the others secreted PLA2s; thus hGX sPLA2 may be a novel player in PAF regulation during inflammatory processes. (PMID:16962371)
  • This study showed that GX sPLA2 is present in human atherosclerotic lesions and that the hydrolysis of LDL cholesterol by GX sPLA2 results in a modified particle that induces lipid accumulation in human monocyte-derived macrophages. (PMID:17077289)
  • secretory phospholipase A2 group X enhances anti-inflammatory responses, promotes lipid accumulation, and contributes to aberrant lung pathology (PMID:18511424)
  • rate and specificity of hydrolysis are affected by relative increases in endogenous SM and free cholesterol (FC) during the lipase digestion (PMID:18587072)
  • The T-512C polymorphism located in the 5’ untranslated region of the secreted phospholipase A2 group X gene associated with a decreased risk of recurrent cardiovascular events during follow-up. (PMID:19495570)
  • Group X secreted phospholipase A2 induces production of VEGF-A and VEGF-C from lung macrophages by a receptor-mediated, catalytically independent mechanism and may play an important role in inflammatory and neoplastic angiogenesis and lymphangiogenesis. (PMID:20357262)
  • GX sPLA(2) promotes Ang II-induced pathological responses leading to abdominal aortic aneurysm formation (PMID:20833395)
  • Eosinophil cysteinyl leukotriene synthesis is mediated by exogenous secreted phospholipase A2 group X (PMID:20974857)
  • sPLA(2) -IIA and sPLA(2) -X are the major sPLA(2) s in human airways, and suggest a link between the levels of sPLA(2) -X in the airways and several features of asthma. (PMID:21255140)
  • the use of a highly potent indole-based inhibitor of hGX-sPLA(2), RO061606 (which is ineffective against mGX-sPLA(2)), to assess the potential utility of GX-sPLA(2) blockade as a therapeutic intervention in asthma. (PMID:21652694)
  • Group X secreted phospholipase A2 proenzyme is matured by a furin-like proprotein convertase and releases arachidonic acid inside of human HEK293 cells (PMID:21878635)
  • CONCLUSION: hGX-sPLA(2) secreted in inflamed tissues can contribute to local dendritic cell maturation, resulting in pro-Th1 cells, through the production of various lipid mediators from hydrolysis of either LDL and/or cell plasma membrane. (PMID:22494626)
  • Molecular details of membrane fluidity changes during apoptosis and relationship to phospholipase A(2) activity (PMID:22967861)
  • PLA2G10 expression in bone marrow cells controls a proatherogenic Th1 response and limits the development of atherosclerosis. (PMID:23349189)
  • Secreted phospholipase A2 group X plays a key role in regulating eicosanoid formation and the development of inflammation and airway hyperresponsiveness in murine models. (PMID:23614662)
  • The enzyme activity of sPLA2 is not altered in serum and cerebrospinal fluid of patients with relapsing-remitting multiple sclerosis during the course of the disease. (PMID:23859159)
  • hGX sPLA2 is a novel modulator of lipid metabolism that promotes breast cancer cell growth and survival by stimulating lipid droplet formation and fatty acid oxidation. (PMID:24070020)
  • Data indicate that the expression of genes encoding hGIIA, hGIII and hGX sPLA2s (PLA2G2A, PLA2G3 and PLA2G10, respectively) in breast tumour biopsies differs from that in normal tissues. (PMID:24508801)
  • Studies indicate that the expression of secreted phospholipases A2 (sPLA2s), most notably the group IIA, III and X enzymes, is dysregulated in various malignant tissues. (PMID:25286228)
  • PLA2G10 variants are not significantly associated with plasma sPLA2 activity or with CHD risk. (PMID:25583995)
  • sPLA2GIII expression may be used as a risk factor for lymph node metastasis and a prognostic marker in colorectal cancer. In addition, sPLA2GIII and sPLA2GX may play opposing roles in colorectal carcinogenesis (PMID:25964585)
  • Endogenous secreted phospholipase A2 group X regulates cysteinyl leukotrienes synthesis by human eosinophils (PMID:26139511)
  • Data show that phospholipase A2 group IIA, V and X have different target/function related activity. (PMID:26711221)
  • PLA2G10 releases omega-3 polyunsaturated fatty acids, suppresses colitis, and promotes sperm fertility. (PMID:26828067)
  • This report provides the first demonstration that Phosphatidylcholine-Isoprostanes are readily hydrolyzed by group IIA, V and X Secretory Phospholipases A2. (PMID:28528433)
  • PLA2G10 facilitates the cell-cycle progression of soft tissue leiomyosarcoma cells at least by elevating cyclin E1/CDK2 expression. (PMID:32423798)
  • PLA2G10 incorporated in exosomes could be diagnostic and prognostic biomarker for non-small cell lung cancer. (PMID:35231479)
  • Up-regulated PLA2G10 in cancer impairs T cell infiltration to dampen immunity. (PMID:38669316)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriopla2g10ENSDARG00000099344
mus_musculusPla2g10ENSMUSG00000022683
rattus_norvegicusPla2g10ENSRNOG00000003164

Paralogs (8): PLA2G2D (ENSG00000117215), PLA2G5 (ENSG00000127472), PLA2G2F (ENSG00000158786), PLA2G1B (ENSG00000170890), PLA2G2C (ENSG00000187980), PLA2G2A (ENSG00000188257), PLA2G2E (ENSG00000188784), OC90 (ENSG00000253117)

Protein

Protein identifiers

Group 10 secretory phospholipase A2 — O15496 (reviewed: O15496)

Alternative names: Group X secretory phospholipase A2, Phosphatidylcholine 2-acylhydrolase 10

All UniProt accessions (2): O15496, H3BRW4

UniProt curated annotations — full annotation on UniProt →

Function. Secretory calcium-dependent phospholipase A2 that primarily targets extracellular phospholipids. Hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids with preference for phosphatidylcholines and phosphatidylglycerols over phosphatidylethanolamines. Preferentially releases sn-2 omega-6 and omega-3 polyunsaturated fatty acyl (PUFA) chains over saturated fatty acyls. Contributes to phospholipid remodeling of very low-density lipoprotein (VLDL), low-density lipoprotein (LDL) and high-density lipoprotein (HDL) particles. Hydrolyzes LDL phospholipids releasing unsaturated fatty acids that regulate macrophage differentiation toward foam cells. Efficiently hydrolyzes and inactivates platelet activating factor (PAF), a potent lipid mediator present in oxidized LDL. May act in an autocrine and paracrine manner. Secreted by lung epithelium, targets membrane phospholipids of infiltrating eosinophils, releasing arachidonate and boosting eicosanoid and cysteinyl leukotriene synthesis involved in airway inflammatory response. Secreted by gut epithelium, hydrolyzes dietary and biliary phosphatidylcholines in the gastrointestinal lumen. Plays a stem cell regulator role in colon epithelium. Within intracellular compartment, mediates Paneth-like cell differentiation and its stem cell supporting functions by inhibiting the Wnt signaling pathway in intestinal stem cell (ISC). Secreted in the intestinal lumen upon inflammation, acts in an autocrine way and promotes prostaglandin E2 synthesis that stimulates Wnt signaling pathway in ISCs and tissue regeneration. May participate in hair follicle morphogenesis by regulating phosphatidylethanolamines metabolism at the outermost epithelial layer and facilitating melanin synthesis. By releasing lysophosphatidylcholines (LPCs) at sperm acrosome, controls sperm cell capacitation, acrosome reaction and overall fertility. May promote neurite outgrowth in neuron fibers involved in nociception. Contributes to lipid remodeling of cellular membranes and generation of lipid mediators involved in pathogen clearance. Cleaves sn-2 fatty acyl chains of phosphatidylglycerols and phosphatidylethanolamines, which are major components of membrane phospholipids in bacteria. Displays bactericidal activity against Gram-positive bacteria by directly hydrolyzing phospholipids of the bacterial membrane. In pulmonary epithelium, may contribute to host defense response against adenoviral infection. Prevents adenovirus entry into host cells by hydrolyzing host cell plasma membrane, releasing C16:0 LPCs that inhibit virus-mediated membrane fusion and viral infection. Likely prevents adenoviral entry into the endosomes of host cells. May play a role in maturation and activation of innate immune cells including macrophages, group 2 innate lymphoid cells and mast cells.

Subunit / interactions. Interacts with PLA2R1; this interaction mediates PLA2G10 clearance and inactivation.

Subcellular location. Secreted. Lysosome. Cytoplasmic vesicle. Secretory vesicle. Acrosome.

Tissue specificity. Found in spleen, thymus, peripheral blood leukocytes, pancreas, lung, and colon. Expressed in neuronal fibers in dorsal root ganglia and in peripheral tissues including stomach, white adipose tissue and prostate (at protein level).

Activity regulation. Inhibited by methyl indoxam.

Cofactor. Binds 1 Ca(2+) ion per subunit.

Similarity. Belongs to the phospholipase A2 family.

RefSeq proteins (1): NP_003552* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001211PLA2Family
IPR016090PLA2-like_domDomain
IPR033112PLA2_Asp_ASActive_site
IPR033113PLA2_histidineActive_site
IPR036444PLipase_A2_dom_sfHomologous_superfamily

Pfam: PF00068

Enzyme classification (BRENDA):

  • EC 3.1.1.4 — phospholipase A2 (BRENDA: 129 organisms, 452 substrates, 710 inhibitors, 90 Km, 14 kcat entries)

Substrate kinetics (BRENDA)

58 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
PHOSPHATIDYLCHOLINE0.05–1712
1,2-DIHEXANOYL-SN-GLYCERO-3-PHOSPHOCHOLINE0.94–13.857
PHOSPHATIDYLETHANOLAMINE0.02–10.55
1,2-DIHEPTANOYL-SN-GLYCERO-3-PHOPHORYLCHOLINE1.12–5.133
1,2-DIHEPTANOYL-SN-GLYCERO-3-PHOSPHOCHOLINE3–3.923
1,2-DIOCTANOYL-SN-GLYCERO-3-PHOSPHOCHOLINE0.12–3.23
1-HEXADECYL-2-ACETYL-SN-GLYCEROL-3-PHOSPHOCHOLIN0.0137–0.01422
1-PALMITOYL-2-ARACHIDONYLPHOSPHATIDYLCHOLINE0.0016–0.00332
LECITHIN8.3–8.52
(3E)-3-[(3AS,7AS)-3-METHYL-2-OXO-6-(PROPAN-2-YLI0.7421
(3R,3AS,5AS,8BR)-3,5A,5B-TRIMETHYL-3A,4,5,5A,5B,0.7461
(3R,3AS,5AS,9BR)-3,5A,9-TRIMETHYL-3A,4,5,5A-TETR0.7341
(3R,3AS,6R,8S,9BS)-6,8-DIHYDROXY-3,6,9-TRIMETHYL0.7441
(3R,3AS,6R,8S,9BS)-8-HYDROXY-3,6,9-TRIMETHYL-2-O0.7381
(3R,3AS,6R,9BS)-3,6,9-TRIMETHYL-2,8-DIOXO-2,3,3A0.7421

Catalyzed reactions (Rhea), 10 shown:

  • 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-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:38779)
  • 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine + H2O = 1-O-hexadecyl-sn-glycero-3-phosphocholine + acetate + H(+) (RHEA:40479)
  • 1-octadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphocholine + H2O = 1-octadecanoyl-sn-glycero-3-phosphocholine + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+) (RHEA:40519)
  • 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphoethanolamine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoethanolamine + (9Z,12Z)-octadecadienoate + H(+) (RHEA:40815)
  • 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:41223)
  • 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phospho-L-serine + H2O = 1-hexadecanoyl-sn-glycero-3-phospho-L-serine + (9Z)-octadecenoate + H(+) (RHEA:41752)
  • 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphoglycerol + H2O = 1-hexadecanoyl-sn-glycero-3-phosphoglycerol + (9Z)-octadecenoate + H(+) (RHEA:44524)
  • 1,2-dihexadecanoyl-sn-glycero-3-phospho-(1’-sn-glycerol) + H2O = 1-hexadecanoyl-sn-glycero-3-phospho-(1’-sn-glycerol) + hexadecanoate + H(+) (RHEA:45472)
  • 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphate + H2O = 1-hexadecanoyl-sn-glycero-3-phosphate + (9Z)-octadecenoate + H(+) (RHEA:63996)

UniProt features (32 total): disulfide bond 8, helix 6, strand 5, binding site 4, turn 2, active site 2, signal peptide 1, propeptide 1, mutagenesis site 1, chain 1, glycosylation site 1

Structure

Experimental structures (PDB)

7 structures.

PDBMethodResolution (Å)
5OWCX-RAY DIFFRACTION1.75
5G3MX-RAY DIFFRACTION1.85
6G5JX-RAY DIFFRACTION1.85
5OW8X-RAY DIFFRACTION1.9
1LE6X-RAY DIFFRACTION1.97
1LE7X-RAY DIFFRACTION2.09
4UY1X-RAY DIFFRACTION2.2

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O15496-F188.230.72

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): 88; 133

Ligand- & substrate-binding residues (4): 68; 70; 72; 89

Disulfide bonds (8): 53–111, 67–157, 69–85, 84–139, 90–164, 91–132, 100–125, 118–130

Glycosylation sites (1): 113

Mutagenesis-validated functional residues (1):

PositionPhenotype
88loss of pla2 activity toward paf. impairs anti-adenoviral activity.

Function

Pathways and Gene Ontology

Reactome pathways

6 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-1482922Acyl chain remodelling of PI
R-HSA-1482925Acyl chain remodelling of PG
R-HSA-1483166Synthesis of PA

MSigDB gene sets: 278 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_SINGLE_FERTILIZATION, GOBP_POSITIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, GOBP_REGULATION_OF_LIPID_STORAGE, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_REGULATION_OF_ICOSANOID_SECRETION, GOBP_EPIDERMIS_MORPHOGENESIS, GOBP_MYELOID_CELL_HOMEOSTASIS, GOBP_REGULATION_OF_PROSTAGLANDIN_SECRETION, GOBP_REGULATION_OF_ORGANIC_ACID_TRANSPORT, GOBP_MYELOID_CELL_DEVELOPMENT

GO Biological Process (38): negative regulation of transcription by RNA polymerase II (GO:0000122), prostaglandin biosynthetic process (GO:0001516), production of molecular mediator involved in inflammatory response (GO:0002532), phosphatidylserine metabolic process (GO:0006658), axon guidance (GO:0007411), fertilization (GO:0009566), positive regulation of macrophage derived foam cell differentiation (GO:0010744), positive regulation of lipid storage (GO:0010884), arachidonate metabolic process (GO:0019369), signal transduction involved in regulation of gene expression (GO:0023019), hair follicle morphogenesis (GO:0031069), positive regulation of prostaglandin secretion (GO:0032308), low-density lipoprotein particle remodeling (GO:0034374), phosphatidylcholine catabolic process (GO:0034638), intestinal stem cell homeostasis (GO:0036335), macrophage activation (GO:0042116), cholesterol homeostasis (GO:0042632), regulation of macrophage activation (GO:0043030), erythrocyte maturation (GO:0043249), phosphatidylethanolamine metabolic process (GO:0046337), phosphatidylcholine metabolic process (GO:0046470), phosphatidylglycerol metabolic process (GO:0046471), phosphatidic acid metabolic process (GO:0046473), arachidonate secretion (GO:0050482), negative regulation of inflammatory response (GO:0050728), positive regulation of protein metabolic process (GO:0051247), defense response to virus (GO:0051607), lysophospholipid transport (GO:0051977), platelet activating factor catabolic process (GO:0062234), positive regulation of arachidonate secretion (GO:0090238), negative regulation of cholesterol efflux (GO:0090370), nuclear receptor-mediated signaling pathway (GO:0141193), negative regulation of cytokine production involved in inflammatory response (GO:1900016), cellular response to leukemia inhibitory factor (GO:1990830), positive regulation of acrosome reaction (GO:2000344), lipid metabolic process (GO:0006629), phospholipid metabolic process (GO:0006644), lipid catabolic process (GO:0016042)

GO Molecular Function (9): 1-alkyl-2-acetylglycerophosphocholine esterase activity (GO:0003847), glycerophospholipase activity (GO:0004620), A2-type glycerophospholipase activity (GO:0004623), calcium ion binding (GO:0005509), phospholipid binding (GO:0005543), obsolete calcium-dependent phospholipase A2 activity (GO:0047498), protein binding (GO:0005515), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (5): acrosomal vesicle (GO:0001669), extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), lysosome (GO:0005764), cytoplasmic vesicle (GO:0031410)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
Glycerophospholipid biosynthesis6

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
glycerophospholipid metabolic process2
carboxylic ester hydrolase activity2
regulation of transcription by RNA polymerase II1
transcription by RNA polymerase II1
negative regulation of DNA-templated transcription1
prostaglandin metabolic process1
prostanoid biosynthetic process1
inflammatory response1
multicellular organismal process1
modified amino acid metabolic process1
axonogenesis1
neuron projection guidance1
sexual reproduction1
reproductive process1
macrophage derived foam cell differentiation1
regulation of macrophage derived foam cell differentiation1
positive regulation of cell differentiation1
regulation of lipid storage1
lipid storage1
positive regulation of cellular process1
positive regulation of lipid localization1
long-chain fatty acid metabolic process1
icosanoid metabolic process1
unsaturated fatty acid metabolic process1
olefinic compound metabolic process1
signal transduction1
regulation of gene expression1
hair follicle development1
anatomical structure morphogenesis1
hair cycle process1
epidermis morphogenesis1
positive regulation of icosanoid secretion1
regulation of prostaglandin secretion1
prostaglandin secretion1
positive regulation of secretion by cell1
plasma lipoprotein particle remodeling1
phosphatidylcholine metabolic process1
glycerophospholipid catabolic process1
homeostasis of number of cells1
myeloid leukocyte activation1

Protein interactions and networks

STRING

1028 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PLA2G10PLA2G12AQ9BZM1955
PLA2G10PLA2G3Q9NZ20945
PLA2G10PLA2R1Q13018926
PLA2G10PLA2G12BQ9BX93917
PLA2G10PLA2G4AP47712858
PLA2G10PTGS2P35354801
PLA2G10PLA2G6O60733678
PLA2G10PLA2G7Q13093663
PLA2G10ENPP2Q13822633
PLA2G10ALBP02768591
PLA2G10SELPP16109525
PLA2G10GANABQ14697514
PLA2G10PNPLA8Q9NP80510
PLA2G10PLA2G1BP04054506
PLA2G10IL1BP01584503

IntAct

164 interactions, top by confidence:

ABTypeScore
PLA2G10NTAQ1psi-mi:“MI:0915”(physical association)0.740
LCE2BPLA2G10psi-mi:“MI:0915”(physical association)0.600
PLA2G10LCE2Bpsi-mi:“MI:0915”(physical association)0.600
VGLL3PLA2G10psi-mi:“MI:0915”(physical association)0.560
PLA2G10KRTAP26-1psi-mi:“MI:0915”(physical association)0.560
PLA2G10KRTAP11-1psi-mi:“MI:0915”(physical association)0.560
PLA2G10ATXN1psi-mi:“MI:0915”(physical association)0.560
PLA2G10HSF4psi-mi:“MI:0915”(physical association)0.560
PLA2G10AQP1psi-mi:“MI:0915”(physical association)0.560
PLA2G10STK16psi-mi:“MI:0915”(physical association)0.560
PLA2G10BAG3psi-mi:“MI:0915”(physical association)0.560
PLA2G10TLX3psi-mi:“MI:0915”(physical association)0.560
PLA2G10SNRPCpsi-mi:“MI:0915”(physical association)0.560
PLA2G10TFGpsi-mi:“MI:0915”(physical association)0.560
PLA2G10OTX1psi-mi:“MI:0915”(physical association)0.560
PLA2G10BEX2psi-mi:“MI:0915”(physical association)0.560
PLA2G10LCE1Apsi-mi:“MI:0915”(physical association)0.560
PLA2G10NOXA1psi-mi:“MI:0915”(physical association)0.560
PLA2G10MALpsi-mi:“MI:0915”(physical association)0.560
PLA2G10MAPKBP1psi-mi:“MI:0915”(physical association)0.560
PLA2G10GATA5psi-mi:“MI:0915”(physical association)0.560
PLA2G10CATSPER1psi-mi:“MI:0915”(physical association)0.560
PLA2G10TBX6psi-mi:“MI:0915”(physical association)0.560
PLA2G10CREB5psi-mi:“MI:0915”(physical association)0.560
PLA2G10CCDC120psi-mi:“MI:0915”(physical association)0.560
PLA2G10INCA1psi-mi:“MI:0915”(physical association)0.560
PLA2G10POU4F3psi-mi:“MI:0915”(physical association)0.560
PLA2G10LCE1Cpsi-mi:“MI:0915”(physical association)0.560
PLA2G10LCE2Apsi-mi:“MI:0915”(physical association)0.560
PLA2G10C1orf94psi-mi:“MI:0915”(physical association)0.560

BioGRID (148): GPT2 (Affinity Capture-MS), GSTCD (Affinity Capture-MS), AURKA (Affinity Capture-MS), TDP2 (Affinity Capture-MS), WNT11 (Affinity Capture-MS), NCOA1 (Affinity Capture-MS), EOGT (Affinity Capture-MS), TUBB1 (Affinity Capture-MS), ZSWIM7 (Affinity Capture-MS), UBA52 (Affinity Capture-MS), WDYHV1 (Affinity Capture-MS), SPIDR (Affinity Capture-MS), LONRF2 (Affinity Capture-MS), PRKD2 (Affinity Capture-MS), FIGNL1 (Affinity Capture-MS)

ESM2 similar proteins: A2AE20, A6QQ77, B6VH75, B6VH76, B6VH77, B6VH79, D4ABW7, O08717, O15496, O75173, O75951, O88839, P00716, P01231, P04421, P04651, P09462, P11688, P12068, P30805, P51782, Q05820, Q0V8J4, Q13444, Q29RT1, Q2T9N7, Q32PD6, Q49KI5, Q5E985, Q5RFQ8, Q5U2X4, Q659U0, Q659U1, Q659U5, Q6EV78, Q6MG64, Q8BNJ2, Q8IXA5, Q923K1, Q96KX0

Diamond homologs: A8CG82, A8CG86, A8CG89, A8CG90, C1JAR9, D2X8K2, F8J2D0, F8J2D2, F8QN50, F8QN51, O15496, O42192, P00592, P00593, P00596, P00608, P00612, P00613, P00614, P04054, P04055, P08872, P0C616, P0DKR3, P0DPT7, P0DPT9, P0DUN7, P0DY42, P14419, P14420, P14423, P14555, P15445, P20476, P21789, P24293, P24294, P31482, P31854, P39878

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 56 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Formation of the cornified envelope512.9×4e-03
Keratinization711.5×3e-04

GO biological processes:

GO termPartnersFoldFDR
keratinization522.5×9e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance8
Likely benign2
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

529 predictions. Top by Δscore:

VariantEffectΔscore
16:14688156:GGGAC:Gdonor_loss0.9900
16:14688157:GGAC:Gdonor_loss0.9900
16:14688158:GAC:Gdonor_loss0.9900
16:14688159:ACTC:Adonor_loss0.9900
16:14688160:CT:Cdonor_loss0.9900
16:14688161:T:TGdonor_loss0.9900
16:14688162:C:CGdonor_loss0.9900
16:14688163:A:ACdonor_gain0.9900
16:14688163:A:AGdonor_loss0.9900
16:14688164:C:CCdonor_gain0.9900
16:14688164:CCGCA:Cdonor_gain0.9900
16:14688164:CCG:Cdonor_gain0.9800
16:14688268:GCACC:Gacceptor_loss0.9800
16:14688270:ACCT:Aacceptor_loss0.9800
16:14688273:T:Gacceptor_loss0.9800
16:14690487:GCACT:Gdonor_loss0.9800
16:14690488:CACT:Cdonor_loss0.9800
16:14690489:ACT:Adonor_loss0.9800
16:14690490:C:CGdonor_loss0.9800
16:14690491:T:TAdonor_loss0.9800
16:14690492:C:CCdonor_loss0.9800
16:14690493:A:ACdonor_gain0.9800
16:14690494:C:CCdonor_gain0.9800
16:14690494:C:Tdonor_loss0.9800
16:14690494:CCAGT:Cdonor_gain0.9800
16:14690646:C:CCacceptor_gain0.9800
16:14672750:C:CCacceptor_gain0.9700
16:14672751:T:Gacceptor_loss0.9600
16:14688282:C:CTacceptor_gain0.9600
16:14690486:TGCAC:Tdonor_loss0.9600

AlphaMissense

1047 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
16:14688193:C:AW109C0.993
16:14688193:C:GW109C0.993
16:14690549:T:CY65C0.993
16:14672707:T:AD133V0.992
16:14672707:T:GD133A0.992
16:14690539:A:CF68L0.992
16:14690539:A:TF68L0.992
16:14690541:A:GF68L0.992
16:14672716:C:GC130S0.991
16:14672717:A:TC130S0.991
16:14672710:C:GC132S0.990
16:14672711:A:TC132S0.990
16:14688221:C:GC100S0.989
16:14688222:A:TC100S0.989
16:14690537:C:GC69S0.988
16:14690538:A:TC69S0.988
16:14690547:C:AG66C0.988
16:14688266:C:GC85S0.987
16:14688267:A:TC85S0.987
16:14690499:C:GD82H0.987
16:14690585:C:GC53S0.986
16:14690586:A:TC53S0.986
16:14690498:T:AD82V0.985
16:14688167:C:GC118S0.984
16:14688168:A:TC118S0.984
16:14688188:C:GC111S0.984
16:14688189:A:TC111S0.984
16:14688200:T:CY107C0.984
16:14688269:C:GC84S0.984
16:14688270:A:TC84S0.984

dbSNP variants (sampled 300 via entrez): RS1000193000 (16:14675183 A>C), RS1000203027 (16:14674753 T>C), RS1000400172 (16:14674645 G>A), RS1000468568 (16:14680943 C>A,G), RS1000675982 (16:14686790 C>T), RS1000807353 (16:14684901 G>A), RS1001005423 (16:14687117 A>C,T), RS1001037140 (16:14679392 G>C), RS1001164535 (16:14673767 A>G), RS1001488003 (16:14674035 A>C), RS1001617971 (16:14680258 G>A,T), RS1001693400 (16:14679964 T>C), RS1001719827 (16:14679529 ACATGCCTGTAATCC>A), RS1001846796 (16:14686427 G>C), RS1001932672 (16:14674596 G>A,T)

Disease associations

OMIM: gene MIM:603603 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

StudyTraitp-value
GCST008932_11Cholesteryl ester levels2.000000e-06

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0008589esterified cholesterol measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4342 (SINGLE PROTEIN), CHEMBL4524005 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 272 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL148674VARESPLADIB2272

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Phospholipase A2

Most potent curated ligand interactions (1 total), top 1:

LigandActionAffinityParameter
compound 12e [PMID: 18605714]Inhibition7.7pIC50

ChEMBL bioactivities

138 potent at pChembl≥5 of 160 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.15IC507nMCHEMBL477548
8.00IC5010nMCHEMBL514705
7.96IC5011nMCHEMBL514656
7.85IC5014nMCHEMBL4215835
7.85IC5014nMCHEMBL474874
7.82IC5015nMCHEMBL4210991
7.82IC5015nMCHEMBL514692
7.70IC5020nMCHEMBL515637
7.66IC5022nMCHEMBL148649
7.58IC5026nMCHEMBL4171084
7.54IC5029nMCHEMBL4217510
7.52IC5030nMCHEMBL477549
7.52IC5030nMCHEMBL506485
7.50IC5032nMCHEMBL4214052
7.41IC5039nMCHEMBL4204172
7.39IC5041nMVARESPLADIB
7.38IC5042nMCHEMBL4215835
7.37IC5043nMCHEMBL4176544
7.30IC5050nMCHEMBL504813
7.25IC5056nMCHEMBL4593409
7.19IC5065nMCHEMBL4205511
7.17IC5068nMCHEMBL4160483
7.16IC5070nMCHEMBL477794
7.12IC5075nMCHEMBL208315
7.12IC5075nMVARESPLADIB
7.10IC5080nMCHEMBL477156
7.05IC5090nMCHEMBL4172222
7.05IC5090nMCHEMBL446349
7.03IC5093nMCHEMBL4175583
7.00IC50100nMCHEMBL4214052
7.00IC50100nMCHEMBL5172164
6.97IC50107.2nMVARESPLADIB
6.96IC50110nMCHEMBL4174522
6.96IC50110nMCHEMBL4213094
6.96IC50110nMCHEMBL4210991
6.94IC50114nMVARESPLADIB
6.92IC50120nMCHEMBL152921
6.88IC50131nMVARESPLADIB
6.85IC50140nMCHEMBL4205008
6.85IC50140nMCHEMBL4204172
6.85IC50140nMCHEMBL477157
6.82IC50150nMVARESPLADIB
6.80IC50160nMCHEMBL4173359
6.77IC50170nMCHEMBL4175643
6.77IC50170nMCHEMBL4204172
6.77IC50170nMCHEMBL4203027
6.76IC50173.8nMCHEMBL3337976
6.70IC50200nMCHEMBL4207266
6.70IC50200nMCHEMBL444450
6.64IC50230nMCHEMBL4171797

PubChem BioAssay actives

138 with measured affinity, of 247 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
2-[1-benzyl-4-[2-(methanesulfonamido)-2-oxoethoxy]-2-(2-methylpropyl)indol-3-yl]-2-oxoacetamide1169326: Binding affinity to sPLA2X (unknown origin)ic500.0070uM
2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylbenzo[g]indol-4-yl]oxyacetic acid341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0100uM
2-[1-benzyl-4-[2-[(2-methylphenyl)sulfonylamino]-2-oxoethoxy]-2-(2-methylpropyl)indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0110uM
(2R)-3-[3-(5-benzyl-2-carbamoylphenyl)phenyl]-2-methylpropanoic acid1631141: Inhibition of sPLA2 in human HepG2 cellsic500.0140uM
3-[6-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]butanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0140uM
2-[1-benzyl-4-[2-[(2-chlorophenyl)sulfonylamino]-2-oxoethoxy]-2-(2-methylpropyl)indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0140uM
(3S)-3-[3-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]phenyl]butanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0150uM
2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-ethylindol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0150uM
2-(1-benzyl-2-ethyl-3-oxamoylbenzo[g]indol-4-yl)oxyacetic acid341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0200uM
2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxypropanoic acid341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0220uM
3-[3-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0260uM
3-[6-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]propanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0290uM
2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-(2-methylpropyl)benzo[g]indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0300uM
2-[1-benzyl-2-(2-methylpropyl)-4-[2-oxo-2-(trifluoromethylsulfonylamino)ethoxy]indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0300uM
3-[3-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]phenyl]-2-methylpropanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0320uM
3-[3-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]phenyl]-2-methoxypropanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0390uM
2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0410uM
3-[3-[2-carbamoyl-6-(trifluoromethyl)indol-1-yl]phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0430uM
2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylindol-4-yl]oxyacetic acid341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0500uM
3-(2-methyl-5-propan-2-ylthiophen-3-yl)-1H-pyrazole-5-carboxamide1169327: Inhibition of human sPLA2X using 1,2-bis(heptanoylthio) glycerophosphocholine substrate incubated for 30 minsic500.0513uM
3-[6-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]-2-methylpropanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.0650uM
3-[3-[2-carbamoyl-6-(difluoromethoxy)indol-1-yl]phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0680uM
2-[1-benzyl-2-(2-methylpropyl)-4-[2-oxo-2-[[2-(trifluoromethyl)phenyl]sulfonylamino]ethoxy]indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0700uM
2-(1-benzyl-2-ethyl-6-methyl-3-oxamoylindol-4-yl)oxyacetic acid264372: Inhibition of human recombinant sPLA2 G10ic500.0750uM
N-(benzenesulfonyl)-2-[1-benzyl-2-(2-methylpropyl)-3-oxamoylindol-4-yl]oxypropanamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0800uM
3-[3-(2-carbamoyl-6-chloroindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0900uM
2-[4-[2-(benzenesulfonamido)-2-oxoethoxy]-1-benzyl-2-ethylbenzo[g]indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.0900uM
3-[3-[2-carbamoyl-6-(2,2,2-trifluoroethoxy)indol-1-yl]phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.0930uM
2-[2-methyl-1-oxamoyl-3-[(2-phenylphenyl)methyl]indolizin-8-yl]oxyacetic acid1894729: Inhibition of human group X phospholipase A2 incubated for 10 to 20 mins cells by radiometric assayic500.1000uM
3-[3-(2-carbamoyl-6-cyanoindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.1100uM
3-[2-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-4-pyridinyl]propanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.1100uM
(3S)-4-(4-benzylphenyl)sulfanyl-3-[[(E)-dec-3-enoyl]amino]butanoic acid159083: In vitro activity against porcine pancreatic phospholipase-A2 (PLA2) and micellar substrate with deoxycholate (DOC)ic500.1200uM
3-[2-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-4-pyridinyl]-2-methylpropanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.1400uM
2-[1-benzyl-4-[2-[(3-chlorophenyl)sulfonylamino]-2-oxoethoxy]-2-(2-methylpropyl)indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.1400uM
3-[3-(2-carbamoyl-6-cyclopropylindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.1600uM
3-[3-(2-carbamoyl-6-ethylindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.1700uM
2-[[6-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]methyl]butanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.1700uM
3-(2-methyl-1-benzothiophen-3-yl)-1H-pyrazole-5-carboxamide1169327: Inhibition of human sPLA2X using 1,2-bis(heptanoylthio) glycerophosphocholine substrate incubated for 30 minsic500.1738uM
(3R)-3-[3-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]phenyl]butanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.2000uM
1-[3-dodecanoyl-2,4,6-trihydroxy-5-[7-hydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-4-yl]phenyl]dodecan-1-one389113: Inhibition of sPLA2 group 10ic500.2000uM
3-[3-(2-carbamoyl-6-methylindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.2300uM
3-[4-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]propanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.2400uM
3-[3-(2-carbamoyl-6-fluoroindol-1-yl)phenyl]propanoic acid1356216: Inhibition of recombinant human sPLA2-10 expressed in Escherichia coli BL21(DE3) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 minsic500.2600uM
3-[3-(5-benzyl-2-carbamoylphenyl)phenyl]propanoic acid1631099: Inhibition of recombinant sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by colorimetric methodic500.2800uM
3-(2,5-dimethylthiophen-3-yl)-1H-pyrazole-5-carboxamide1169327: Inhibition of human sPLA2X using 1,2-bis(heptanoylthio) glycerophosphocholine substrate incubated for 30 minsic500.3162uM
3-[6-[2-carbamoyl-6-(trifluoromethoxy)indol-1-yl]-2-pyridinyl]-2,2-dimethylpropanoic acid1384819: Inhibition of sPLA2-10 (unknown origin) using 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine as substrate pretreated for 20 mins followed by substrate addition and measured after 60 mins by NEFA based assayic500.3200uM
2-[1-benzyl-4-[2-[(4-methylphenyl)sulfonylamino]-2-oxoethoxy]-2-(2-methylpropyl)indol-3-yl]-2-oxoacetamide341251: Inhibition of human group2X phospholipase A2 fluorimetric assayic500.3200uM
3-[(2E)-2-[(3-methoxyphenyl)methylidene]hydrazinyl]-1H-quinoxalin-2-one1859295: Inhibition of human PLA2G10ic500.3300uM
3-(2-methyl-5-phenylthiophen-3-yl)-1H-pyrazole-5-carboxamide1169327: Inhibition of human sPLA2X using 1,2-bis(heptanoylthio) glycerophosphocholine substrate incubated for 30 minsic500.3467uM
(4S)-4-[[(E)-dec-3-enoyl]amino]-5-naphthalen-2-ylsulfanylpentanoic acid159083: In vitro activity against porcine pancreatic phospholipase-A2 (PLA2) and micellar substrate with deoxycholate (DOC)ic500.3800uM

CTD chemical–gene interactions

17 total (human), top 17 by PubMed support.

ChemicalActions (top 5)PubMed papers
Estradioldecreases expression, increases expression, increases reaction2
propionaldehydeincreases expression1
2-methyl-4-isothiazolin-3-oneincreases expression1
Grape Seed Proanthocyanidinsaffects cotreatment, decreases expression1
Benzo(a)pyreneincreases expression1
Calcitriolincreases expression1
Catechinaffects cotreatment, decreases expression1
Flavonoidsdecreases expression1
Mustard Gasincreases expression1
Silicon Dioxidedecreases expression1
Tobacco Smoke Pollutiondecreases expression1
Tretinoinincreases expression1
Cyclosporineincreases expression1
Aflatoxin B1increases methylation1
Raloxifene Hydrochlorideincreases expression, increases reaction1
Permethrindecreases expression1
Particulate Matterincreases expression1

ChEMBL screening assays

40 unique, capped per target: 39 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1648032BindingInhibition of human group 10 sPLA2 by fluorescence assayInhibition of secreted phospholipases A₂ by 2-oxoamides based on α-amino acids: Synthesis, in vitro evaluation and molecular docking calculations. — Bioorg Med Chem
CHEMBL6193898FunctionalInhibition of human PLA2G10 in recombinant human protein using Biochemical human PLA2G10 assayData for DCP probe BAY-439

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 80

This page pulls from 80 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_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot