PLAAT3
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Also known as HREV107H-REV107-1HREV107-3MGC118754.AdPLAPLAAT-3
Summary
PLAAT3 (phospholipase A and acyltransferase 3, HGNC:17825) is a protein-coding gene on chromosome 11q12.3-q13.1, encoding Phospholipase A and acyltransferase 3 (P53816). Exhibits both phospholipase A1/2 and acyltransferase activities.
Enables N-acyltransferase activity; lipid binding activity; and phospholipase activity. Involved in N-acylphosphatidylethanolamine metabolic process. Predicted to be located in several cellular components, including lysosome; nuclear envelope; and peroxisome. Predicted to be active in cytoplasm. Biomarker of seminoma.
Source: NCBI Gene 11145 — RefSeq curated summary.
At a glance
- Gene–disease (curated): lipodystrophy, familial partial, type 9 (Strong, GenCC)
- Clinical variants (ClinVar): 51 total — 3 pathogenic, 1 likely-pathogenic
- Phenotypes (HPO): 49
- Druggable target: yes
- MANE Select transcript:
NM_001128203
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:17825 |
| Approved symbol | PLAAT3 |
| Name | phospholipase A and acyltransferase 3 |
| Location | 11q12.3-q13.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | HREV107, H-REV107-1, HREV107-3, MGC118754., AdPLA, PLAAT-3 |
| Ensembl gene | ENSG00000176485 |
| Ensembl biotype | protein_coding |
| OMIM | 613867 |
| Entrez | 11145 |
Gene structure
Transcript identifiers
Ensembl transcripts: 16 — 14 protein_coding, 2 protein_coding_CDS_not_defined
ENST00000323646, ENST00000394613, ENST00000415826, ENST00000540943, ENST00000544269, ENST00000873643, ENST00000873644, ENST00000873645, ENST00000873646, ENST00000873647, ENST00000873648, ENST00000911543, ENST00000911544, ENST00000911545, ENST00000911546, ENST00000911547
RefSeq mRNA: 2 — MANE Select: NM_001128203
NM_001128203, NM_007069
CCDS: CCDS8047
Canonical transcript exons
ENST00000415826 — 5 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001671551 | 63614385 | 63614433 |
| ENSE00001712076 | 63614000 | 63614068 |
| ENSE00003575548 | 63598061 | 63598163 |
| ENSE00003601992 | 63590100 | 63590368 |
| ENSE00003909622 | 63574462 | 63575046 |
Expression profiles
Bgee: expression breadth ubiquitous, 287 present calls, max score 99.33.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.9610 / max 709.3708, expressed in 1545 samples.
FANTOM5 promoters (15 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 120318 | 11.0631 | 1457 |
| 120317 | 8.6588 | 1035 |
| 120319 | 1.8765 | 941 |
| 120312 | 1.4697 | 621 |
| 120313 | 0.9424 | 381 |
| 120314 | 0.7158 | 258 |
| 120311 | 0.6362 | 253 |
| 120316 | 0.4155 | 252 |
| 120309 | 0.2824 | 123 |
| 120310 | 0.2707 | 61 |
Top tissues by expression
293 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| C1 segment of cervical spinal cord | UBERON:0006469 | 99.33 | gold quality |
| spinal cord | UBERON:0002240 | 99.01 | gold quality |
| corpus callosum | UBERON:0002336 | 98.76 | gold quality |
| adipose tissue | UBERON:0001013 | 98.51 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 98.47 | gold quality |
| tibial nerve | UBERON:0001323 | 98.44 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 98.43 | gold quality |
| omental fat pad | UBERON:0010414 | 98.43 | gold quality |
| left testis | UBERON:0004533 | 98.41 | gold quality |
| peritoneum | UBERON:0002358 | 98.40 | gold quality |
| right testis | UBERON:0004534 | 98.32 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 98.21 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 98.16 | gold quality |
| middle frontal gyrus | UBERON:0002702 | 98.10 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 97.93 | gold quality |
| apex of heart | UBERON:0002098 | 97.79 | gold quality |
| putamen | UBERON:0001874 | 97.59 | gold quality |
| globus pallidus | UBERON:0001875 | 97.59 | gold quality |
| substantia nigra | UBERON:0002038 | 97.59 | gold quality |
| connective tissue | UBERON:0002384 | 97.53 | gold quality |
| midbrain | UBERON:0001891 | 97.49 | gold quality |
| inferior olivary complex | UBERON:0002127 | 97.47 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 97.46 | gold quality |
| amygdala | UBERON:0001876 | 97.40 | gold quality |
| medial globus pallidus | UBERON:0002477 | 97.39 | gold quality |
| heart left ventricle | UBERON:0002084 | 97.29 | gold quality |
| hypothalamus | UBERON:0001898 | 97.23 | gold quality |
| cardiac ventricle | UBERON:0002082 | 97.21 | gold quality |
| right atrium auricular region | UBERON:0006631 | 97.13 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 97.12 | gold quality |
Single-cell (SCXA)
Detected in 11 experiment(s), a significant marker in 10.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-11121 | yes | 709.62 |
| E-GEOD-134144 | yes | 34.64 |
| E-MTAB-10287 | yes | 30.25 |
| E-MTAB-8410 | yes | 21.90 |
| E-MTAB-6701 | yes | 18.15 |
| E-HCAD-1 | yes | 15.60 |
| E-GEOD-84465 | yes | 12.13 |
| E-MTAB-9388 | yes | 11.46 |
| E-MTAB-6678 | yes | 9.17 |
| E-MTAB-6524 | no | 286.05 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): ETS2, FOXC1, IRF1, PPARG, SP1, SP3, TP53
miRNA regulators (miRDB)
18 targeting PLAAT3, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
| HSA-MIR-1305 | 99.91 | 71.43 | 3443 |
| HSA-MIR-345-3P | 99.89 | 70.23 | 1421 |
| HSA-MIR-6885-3P | 99.75 | 70.36 | 3187 |
| HSA-MIR-670-5P | 99.67 | 69.94 | 1565 |
| HSA-MIR-4743-3P | 99.62 | 68.12 | 2095 |
| HSA-MIR-3171 | 99.49 | 69.06 | 776 |
| HSA-MIR-4652-3P | 99.33 | 70.02 | 2742 |
| HSA-MIR-223-5P | 99.24 | 68.82 | 1206 |
| HSA-MIR-26B-3P | 98.71 | 67.49 | 1102 |
| HSA-MIR-6830-3P | 98.62 | 68.07 | 1760 |
| HSA-MIR-581 | 98.39 | 67.42 | 835 |
| HSA-MIR-4778-5P | 97.96 | 68.06 | 1634 |
| HSA-MIR-6787-3P | 97.75 | 66.17 | 1233 |
| HSA-MIR-6859-3P | 97.26 | 64.69 | 428 |
| HSA-MIR-1251-5P | 95.78 | 64.10 | 374 |
| HSA-MIR-4655-3P | 82.43 | 62.92 | 60 |
Literature-anchored findings (GeneRIF, showing 20)
- Contact inhibition of growth and growth arrest caused by histone deacetylase inhibitors probably use the same mechanism to stimulate H-rev107 expression via histone acetylation in NIH3T3 cells (PMID:12054741)
- H-REV107-1 is deficient in its function as a tumor suppressor in non-small cell lung carcinomas. (PMID:17003497)
- Identification and functional characterization of adipose-specific phospholipase A2 (AdPLA) (PMID:18614531)
- AdPLA ablation increases lipolysis and prevents obesity induced by high-fat feeding or leptin deficiency. (PMID:19136964)
- role of PKC isoenzymes in PP2A and HRSL3(H-REV107-1) tumor suppressor-dependent cell death induction in ovarian carcinoma cell line; verified contribution to PP2A- and HRLS3-dependent apoptosis for PKCzeta suggesting a proapoptotic function of this kinase (PMID:20501645)
- Data show that acyl-modified forms of HRAS-like tumor suppressors HRASLS2 and HRASLS3 mimicking lipolytic activity of lecithin retinol acyltransferase LRAT. (PMID:22605381)
- an alternate mechanism for AdPLA in promoting adipose tissue lipolysis that is not contingent on the release of arachidonic acid and that is compatible with its combined PLA(1)/A(2) activity (PMID:22923616)
- Our study further suggests that the PLA/AT activity of H-rev107 may play an important role in H-rev107-mediated RAS suppression. (PMID:24884338)
- several mutant p53 proteins bind the Pla2g16 promoter at E26 transformation-specific (ETS) binding motifs and knockdown of ETS2 suppressed mutant p53 induction of Pla2g16. (PMID:25024203)
- crystal structure of the HRASLS3-LRAT chimeric enzyme in a thioester catalytic intermediate state revealed a major structural rearrangement accompanied by three-dimensional domain swapping dimerization not observed in native HRASLS (PMID:25383759)
- the flexible main loop of H-REV107, but not that of TIG3, is critical for its NTD to modulate its CTD in inducing cell death. (PMID:25871522)
- Results show that osteosarcoma patients with metastasis showed higher expression of PLA2G16 at both the mRNA and protein levels and shorter overall survival suggesting it as significant prognostic factor for poor outcome. (PMID:25993412)
- suggest a novel regulatory mechanism for peroxisome biogenesis through the interaction between Pex19p and PLA/AT-3 (PMID:26018079)
- our results revealed that H-rev107 is also involved in lipid accumulation in liver cells through the POR pathway via its PLA2 activity. (PMID:26381418)
- Demonstrate increased PLA2G16 expression activates the MAPK pathway to enhance osteosarcoma metastasis. (PMID:26933804)
- study uncovers two competing processes triggered by Picornaviridae virus entry: activation of a pore-activated clearance pathway and recruitment of a PLA2G16 phospholipase to enable genome release (PMID:28077878)
- PLA2G16 SNPs are associated with the colorectal cancer risk in the Chinese population. (PMID:30343388)
- PLA2G16 methylation defines an extensive field defect in histologically normal prostate tissue associated with PC. (PMID:31233548)
- Skeletal muscle expression of adipose-specific phospholipase in peripheral artery disease. (PMID:32853041)
- PLA2G16 is a mutant p53/KLF5 transcriptional target and promotes glycolysis of pancreatic cancer. (PMID:32985124)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | lratb.2 | ENSDARG00000077652 |
| mus_musculus | Plaat3 | ENSMUSG00000060675 |
| rattus_norvegicus | Plaat3 | ENSRNOG00000021206 |
Paralogs (7): LRAT (ENSG00000121207), PLAAT1 (ENSG00000127252), PLAAT4 (ENSG00000133321), PLAAT2 (ENSG00000133328), LRATD1 (ENSG00000162981), PLAAT5 (ENSG00000168004), LRATD2 (ENSG00000168672)
Protein
Protein identifiers
Phospholipase A and acyltransferase 3 — P53816 (reviewed: P53816)
Alternative names: Adipose-specific phospholipase A2, Group XVI phospholipase A1/A2, H-rev 107 protein homolog, HRAS-like suppressor 1, HRAS-like suppressor 3, HREV107-3, Renal carcinoma antigen NY-REN-65
All UniProt accessions (2): P53816, F5H7E5
UniProt curated annotations — full annotation on UniProt →
Function. Exhibits both phospholipase A1/2 and acyltransferase activities. Shows phospholipase A1 (PLA1) and A2 (PLA2) activity, catalyzing the calcium-independent release of fatty acids from the sn-1 or sn-2 position of glycerophospholipids. For most substrates, PLA1 activity is much higher than PLA2 activity. Shows O-acyltransferase activity,catalyzing the transfer of a fatty acyl group from glycerophospholipid to the hydroxyl group of lysophospholipid. Shows N-acyltransferase activity, catalyzing the calcium-independent transfer of a fatty acyl group at the sn-1 position of phosphatidylcholine (PC) and other glycerophospholipids to the primary amine of phosphatidylethanolamine (PE), forming N-acylphosphatidylethanolamine (NAPE), which serves as precursor for N-acylethanolamines (NAEs). Exhibits high N-acyltransferase activity and low phospholipase A1/2 activity. Required for complete organelle rupture and degradation that occur during eye lens terminal differentiation, when fiber cells that compose the lens degrade all membrane-bound organelles in order to provide lens with transparency to allow the passage of light. Organelle membrane degradation is probably catalyzed by the phospholipase activity. (Microbial infection) Acts as a host factor for picornaviruses: required during early infection to promote viral genome release into the cytoplasm. May act as a cellular sensor of membrane damage at sites of virus entry, which relocalizes to sites of membrane rupture upon virus unfection. Facilitates safe passage of the RNA away from LGALS8, enabling viral genome translation by host ribosome. May also be involved in initiating pore formation, increasing pore size or in maintaining pores for genome delivery. The lipid-modifying enzyme activity is required for this process.
Subunit / interactions. Interacts with PPP2R1A; this interaction might decrease PP2A activity.
Subcellular location. Cell membrane. Cytoplasm. Cytosol. Perinuclear region. Peroxisome membrane. Mitochondrion membrane. Nucleus envelope. Lysosome membrane. Endoplasmic reticulum membrane.
Tissue specificity. Widely expressed. Low expression, if any, in hematopoietic cells and thymus. In testis, confined to round spermatids. Expressed in normal ovarian epithelial cells. Down-regulated in some ovarian carcinomas and testicular germ cell tumors. Highly expressed in white adipose tissue.
Disease relevance. Lipodystrophy, familial partial, 9 (FPLD9) [MIM:620683] An autosomal recessive form of partial lipodystrophy, a disorder characterized by abnormal subcutaneous fat distribution. FPLD9 patients are lean and show muscular hypertrophy, insulin-resistant diabetes with hyperinsulinemia, hypertriglyceridemia with low high-density lipoprotein (HDL) cholesterol, liver steatosis, and polycystic ovary syndrome with hirsutism. Some patients have more generalized lipoatrophy, whereas others have abnormal fat accumulation in the face and neck regions and show cushingoid or acromegalic facial features. Most patients also have neurologic features, including demyelinating polyneuropathy, developmental delay and intellectual disability. The disease is caused by variants affecting the gene represented in this entry.
Domain organisation. The C-terminal transmembrane domain is required for the targeting of the protein to damaged organelles.
Induction. By IFNG and IRF1.
Similarity. Belongs to the H-rev107 family.
RefSeq proteins (2): NP_001121675, NP_009000 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR007053 | LRAT_dom | Domain |
| IPR051496 | H-rev107_PLA/AT | Family |
Pfam: PF04970
Catalyzed reactions (Rhea), 12 shown:
- a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 1-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:15801)
- a 1,2-diacyl-sn-glycero-3-phosphocholine + H2O = a 2-acyl-sn-glycero-3-phosphocholine + a fatty acid + H(+) (RHEA:18689)
- 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 1-hexadecanoyl-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:38779)
- 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:38783)
- 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)
- 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine + H2O = 2-hexadecanoyl-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:40487)
- 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-phosphocholine + H2O = (9Z,12Z)-octadecadienoate + 1-hexadecanoyl-sn-glycero-3-phosphocholine + H(+) (RHEA:40811)
- 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-di-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + H2O = 1-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine + (9Z)-octadecenoate + H(+) (RHEA:40923)
- 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine + H2O = 2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine + hexadecanoate + H(+) (RHEA:40971)
UniProt features (27 total): strand 8, helix 4, mutagenesis site 3, active site 3, topological domain 2, turn 2, chain 1, sequence conflict 1, transmembrane region 1, domain 1, sequence variant 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7ZOM | X-RAY DIFFRACTION | 1.6 |
| 7C3Z | X-RAY DIFFRACTION | 1.96 |
| 4DOT | X-RAY DIFFRACTION | 1.96 |
| 4Q95 | X-RAY DIFFRACTION | 2.2 |
| 7C41 | X-RAY DIFFRACTION | 2.28 |
| 4FA0 | X-RAY DIFFRACTION | 2.65 |
| 2KYT | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P53816-F1 | 77.12 | 0.56 |
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 (3): 23; 35; 113 (acyl-thioester intermediate)
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 39–57 | induces a major structural rearrangement accompanied by domain-swapping dimerization and changes in substrate-specificit |
| 113 | no effect on ppp2r1a-binding. impaired ability to act as a host factor for picornaviruses. |
| 23 | no effect on ppp2r1a-binding. |
Function
Pathways and Gene Ontology
Reactome pathways
4 pathways
| ID | Pathway |
|---|---|
| R-HSA-1482788 | Acyl chain remodelling of PC |
| R-HSA-1482801 | Acyl chain remodelling of PS |
| R-HSA-1482839 | Acyl chain remodelling of PE |
| R-HSA-1482922 | Acyl chain remodelling of PI |
MSigDB gene sets: 451 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_UP, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_UP, GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_DN, GOBP_LENS_FIBER_CELL_DIFFERENTIATION, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOCC_VACUOLAR_MEMBRANE, GOBP_MEMBRANE_DISASSEMBLY, GOZGIT_ESR1_TARGETS_DN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, chr11q13
GO Biological Process (14): triglyceride metabolic process (GO:0006641), phospholipid metabolic process (GO:0006644), peroxisome organization (GO:0007031), phospholipid biosynthetic process (GO:0008654), response to bacterium (GO:0009617), lipid catabolic process (GO:0016042), membrane disassembly (GO:0030397), phosphatidylethanolamine acyl-chain remodeling (GO:0036152), ether lipid metabolic process (GO:0046485), N-acylphosphatidylethanolamine metabolic process (GO:0070292), lens fiber cell differentiation (GO:0070306), organelle disassembly (GO:1903008), regulation of adipose tissue development (GO:1904177), lipid metabolic process (GO:0006629)
GO Molecular Function (9): A2-type glycerophospholipase activity (GO:0004623), lipid binding (GO:0008289), glycerophospholipid phospholipase A1 activity (GO:0008970), obsolete N-acyltransferase activity (GO:0016410), acyltransferase activity (GO:0016746), glycerophospholipase activity (GO:0004620), protein binding (GO:0005515), transferase activity (GO:0016740), hydrolase activity (GO:0016787)
GO Cellular Component (15): nuclear envelope (GO:0005635), cytoplasm (GO:0005737), mitochondrion (GO:0005739), lysosome (GO:0005764), lysosomal membrane (GO:0005765), peroxisome (GO:0005777), peroxisomal membrane (GO:0005778), endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), cytosol (GO:0005829), plasma membrane (GO:0005886), mitochondrial membrane (GO:0031966), perinuclear region of cytoplasm (GO:0048471), nucleus (GO:0005634), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Glycerophospholipid biosynthesis | 4 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 4 |
| cytoplasm | 4 |
| lipid metabolic process | 3 |
| intracellular membrane-bounded organelle | 3 |
| organelle organization | 2 |
| cellular component disassembly | 2 |
| binding | 2 |
| catalytic activity | 2 |
| endomembrane system | 2 |
| organelle membrane | 2 |
| acylglycerol metabolic process | 1 |
| organophosphate metabolic process | 1 |
| phospholipid metabolic process | 1 |
| lipid biosynthetic process | 1 |
| organophosphate biosynthetic process | 1 |
| response to other organism | 1 |
| catabolic process | 1 |
| membrane organization | 1 |
| phosphatidylcholine metabolic process | 1 |
| phosphatidylethanolamine metabolic process | 1 |
| lens development in camera-type eye | 1 |
| epithelial cell differentiation | 1 |
| regulation of developmental process | 1 |
| adipose tissue development | 1 |
| primary metabolic process | 1 |
| glycerophospholipase activity | 1 |
| carboxylic ester hydrolase activity | 1 |
| A1-type glycerophospholipase activity | 1 |
| transferase activity | 1 |
| phospholipase activity | 1 |
| nucleus | 1 |
| organelle envelope | 1 |
| intracellular anatomical structure | 1 |
| lytic vacuole | 1 |
| lysosome | 1 |
| lytic vacuole membrane | 1 |
| microbody | 1 |
| peroxisome | 1 |
| microbody membrane | 1 |
| nuclear outer membrane-endoplasmic reticulum membrane network | 1 |
Protein interactions and networks
STRING
2908 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PLAAT3 | CRABP2 | P29373 | 747 |
| PLAAT3 | RARG | P13631 | 642 |
| PLAAT3 | PLA2G15 | Q8NCC3 | 640 |
| PLAAT3 | PLA2G2A | P14555 | 582 |
| PLAAT3 | SETD3 | Q86TU7 | 563 |
| PLAAT3 | RARB | P10826 | 553 |
| PLAAT3 | PEX19 | P40855 | 543 |
| PLAAT3 | PLA2G4A | P47712 | 528 |
| PLAAT3 | PLA2G3 | Q9NZ20 | 499 |
| PLAAT3 | PLA2G2D | Q9UNK4 | 496 |
| PLAAT3 | PLA2G10 | O15496 | 490 |
| PLAAT3 | PLA2G6 | O60733 | 488 |
| PLAAT3 | KRAS | P01116 | 485 |
| PLAAT3 | PLA2G5 | P39877 | 483 |
| PLAAT3 | ENPP2 | Q13822 | 472 |
IntAct
26 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| UBQLN1 | PLAAT3 | psi-mi:“MI:0915”(physical association) | 0.780 |
| PLAAT3 | UBQLN1 | psi-mi:“MI:0915”(physical association) | 0.780 |
| PPP2R1A | PLAAT3 | psi-mi:“MI:0915”(physical association) | 0.640 |
| PLAAT3 | PPP2R1A | psi-mi:“MI:0915”(physical association) | 0.640 |
| PLAAT3 | PPP2R1A | psi-mi:“MI:0403”(colocalization) | 0.640 |
| PLAAT3 | UBQLN1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| UBQLN1 | PLAAT3 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PLAAT3 | UBQLN2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PLAAT3 | OCLN | psi-mi:“MI:0914”(association) | 0.350 |
| PRKCSH | KLRG2 | psi-mi:“MI:0914”(association) | 0.350 |
| MFSD14A | FAM171A2 | psi-mi:“MI:0914”(association) | 0.350 |
| PLAAT3 | UBQLN2 | psi-mi:“MI:0915”(physical association) | 0.000 |
| PLAAT3 | UBQLN1 | psi-mi:“MI:0915”(physical association) | 0.000 |
| NRIP1 | PLAAT3 | psi-mi:“MI:0915”(physical association) | 0.000 |
| PLAAT3 | UBQLN4 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (19): UBQLN1 (Two-hybrid), UBQLN1 (Two-hybrid), HRAS (Affinity Capture-Western), PLA2G16 (Affinity Capture-Western), PLA2G16 (Affinity Capture-MS), PLA2G16 (Two-hybrid), UBQLN2 (Two-hybrid), OCLN (Affinity Capture-MS), MIB2 (Affinity Capture-MS), PLA2G16 (Affinity Capture-MS), PLA2G16 (Two-hybrid), PLA2G16 (Affinity Capture-MS), PLA2G16 (Affinity Capture-MS), PLA2G16 (Affinity Capture-RNA), PLA2G16 (Two-hybrid)
ESM2 similar proteins: A0A0R4IY06, B8BKI7, D2KX21, D3ZLY0, E0CSI1, O54909, O75452, O88451, P00860, P09057, P11926, P14019, P17516, P27117, P27118, P27119, P27120, P50170, P53816, P53817, P55006, P70694, P97872, Q04799, Q1XAA8, Q2R483, Q3T067, Q3UFY7, Q571F8, Q5R611, Q6AY30, Q6AYP7, Q6P4H8, Q86TW2, Q86V88, Q8R127, Q8R2J9, Q8R3U1, Q8VDG3, Q93V51
Diamond homologs: A0A0R4IY06, D2KX21, P53816, P53817, Q4KLN5, Q5R611, Q8R3U1, Q96KN8, Q9BGL2, Q9CPX5, Q9HDD0, Q9JI61, Q9NWW9, Q9QZU4, Q9UL19, O95237, Q9JI60, Q3ZCA1, Q96KN1, Q96KN4, Q9D650
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PLAAT3 | down-regulates | PPP2CA | |
| PLAAT3 | down-regulates | PPP2CB |
Disease & clinical
Clinical variants and AI predictions
ClinVar
51 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 3 |
| Likely pathogenic | 1 |
| Uncertain significance | 38 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (4)
| Variant ID | HGVS | Classification |
|---|---|---|
| 2691740 | NM_001128203.2(PLAAT3):c.16-4823_118+167del | Pathogenic |
| 2691741 | NM_001128203.2(PLAAT3):c.286dup (p.Ala96fs) | Pathogenic |
| 2691742 | NM_001128203.2(PLAAT3):c.339C>A (p.Cys113Ter) | Pathogenic |
| 4845839 | NM_001128203.2(PLAAT3):c.387+2T>C | Likely pathogenic |
SpliceAI
655 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 11:63575044:GACCT:G | acceptor_loss | 1.0000 |
| 11:63575046:CCT:C | acceptor_loss | 1.0000 |
| 11:63575047:CT:C | acceptor_loss | 1.0000 |
| 11:63575048:T:A | acceptor_loss | 1.0000 |
| 11:63590095:CGCA:C | donor_loss | 1.0000 |
| 11:63590096:GCACC:G | donor_loss | 1.0000 |
| 11:63590097:CAC:C | donor_loss | 1.0000 |
| 11:63590378:C:CT | acceptor_gain | 1.0000 |
| 11:63598059:A:AC | donor_gain | 1.0000 |
| 11:63598060:C:CC | donor_gain | 1.0000 |
| 11:63613998:A:AC | donor_gain | 1.0000 |
| 11:63613999:C:CC | donor_gain | 1.0000 |
| 11:63614018:C:A | donor_gain | 1.0000 |
| 11:63574901:C:CA | donor_gain | 0.9900 |
| 11:63590157:A:AC | donor_gain | 0.9900 |
| 11:63590158:C:CC | donor_gain | 0.9900 |
| 11:63590364:CTCAC:C | acceptor_gain | 0.9900 |
| 11:63590365:TCAC:T | acceptor_gain | 0.9900 |
| 11:63590366:CAC:C | acceptor_gain | 0.9900 |
| 11:63590366:CACC:C | acceptor_gain | 0.9900 |
| 11:63590369:C:CA | acceptor_loss | 0.9900 |
| 11:63590369:C:CC | acceptor_gain | 0.9900 |
| 11:63590370:T:C | acceptor_loss | 0.9900 |
| 11:63590378:C:T | acceptor_gain | 0.9900 |
| 11:63597628:AGATC:A | donor_gain | 0.9900 |
| 11:63598160:CTGG:C | acceptor_gain | 0.9900 |
| 11:63598164:C:CC | acceptor_gain | 0.9900 |
| 11:63613999:CA:C | donor_gain | 0.9900 |
| 11:63613999:CAA:C | donor_gain | 0.9900 |
| 11:63613999:CAAT:C | donor_gain | 0.9900 |
AlphaMissense
1058 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 11:63590126:G:T | R121S | 0.994 |
| 11:63590151:G:C | N112K | 0.991 |
| 11:63590151:G:T | N112K | 0.991 |
| 11:63598107:C:A | W24C | 0.991 |
| 11:63598107:C:G | W24C | 0.991 |
| 11:63598109:A:G | W24R | 0.991 |
| 11:63598109:A:T | W24R | 0.991 |
| 11:63590139:A:C | F116L | 0.990 |
| 11:63590139:A:T | F116L | 0.990 |
| 11:63590141:A:G | F116L | 0.990 |
| 11:63598141:A:G | L13P | 0.990 |
| 11:63590106:A:C | S127R | 0.989 |
| 11:63590106:A:T | S127R | 0.989 |
| 11:63590108:T:G | S127R | 0.989 |
| 11:63590128:A:G | L120P | 0.989 |
| 11:63598078:A:T | V34D | 0.989 |
| 11:63590149:C:T | C113Y | 0.988 |
| 11:63590308:A:T | V60E | 0.987 |
| 11:63590125:C:G | R121P | 0.986 |
| 11:63590140:A:G | F116S | 0.985 |
| 11:63590146:T:A | E114V | 0.985 |
| 11:63590150:A:G | C113R | 0.985 |
| 11:63598106:C:G | A25P | 0.985 |
| 11:63590145:C:A | E114D | 0.984 |
| 11:63590145:C:G | E114D | 0.984 |
| 11:63590148:G:C | C113W | 0.984 |
| 11:63598074:A:C | H35Q | 0.984 |
| 11:63598074:A:T | H35Q | 0.984 |
| 11:63590126:G:C | R121G | 0.983 |
| 11:63598081:A:T | V33E | 0.982 |
dbSNP variants (sampled 300 via entrez): RS1000036247 (11:63614172 CG>C), RS1000073148 (11:63604260 T>A), RS1000227954 (11:63587678 A>C), RS1000357723 (11:63600804 A>G), RS1000429992 (11:63613913 G>C), RS1000450898 (11:63593125 G>T), RS1000474695 (11:63606153 A>C), RS1000618823 (11:63594676 G>A,C), RS1000813685 (11:63601131 T>C), RS1000816281 (11:63594556 T>C), RS1000845492 (11:63575813 T>TA), RS1000911442 (11:63582372 G>A), RS1000931269 (11:63582578 C>T), RS1000932068 (11:63618759 A>G), RS1001106721 (11:63582639 A>G)
Disease associations
OMIM: gene MIM:613867 | disease phenotypes: MIM:620683
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| lipodystrophy, familial partial, type 9 | Strong | Autosomal recessive |
Mondo (1): lipodystrophy, familial partial, type 9 (MONDO:0958034)
Orphanet (1): Lipodystrophy-demyelinating peripheral sensory-motor neuropathy syndrome (Orphanet:686999)
HPO phenotypes
49 total (30 of 49 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000007 | Autosomal recessive inheritance |
| HP:0000147 | Polycystic ovaries |
| HP:0000303 | Mandibular prognathia |
| HP:0000369 | Low-set ears |
| HP:0000444 | Convex nasal ridge |
| HP:0000448 | Prominent nose |
| HP:0000470 | Short neck |
| HP:0000490 | Deeply set eye |
| HP:0000771 | Gynecomastia |
| HP:0000821 | Hypothyroidism |
| HP:0000822 | Hypertension |
| HP:0000826 | Precocious puberty |
| HP:0000831 | Insulin-resistant diabetes mellitus |
| HP:0000842 | Hyperinsulinemia |
| HP:0000956 | Acanthosis nigricans |
| HP:0001007 | Hirsutism |
| HP:0001249 | Intellectual disability |
| HP:0001263 | Global developmental delay |
| HP:0001284 | Areflexia |
| HP:0001397 | Hepatic steatosis |
| HP:0001761 | Pes cavus |
| HP:0001771 | Achilles tendon contracture |
| HP:0002064 | Spastic gait |
| HP:0002076 | Migraine |
| HP:0002155 | Hypertriglyceridemia |
| HP:0002240 | Hepatomegaly |
| HP:0002650 | Scoliosis |
| HP:0002808 | Kyphosis |
| HP:0002829 | Arthralgia |
| HP:0002857 | Genu valgum |
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3831244 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
33 potent at pChembl≥5 of 33 total, top 33 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.00 | IC50 | 100 | nM | CHEMBL4633449 |
| 7.00 | IC50 | 100 | nM | CHEMBL4639199 |
| 6.90 | IC50 | 125.9 | nM | CHEMBL4639242 |
| 6.80 | IC50 | 158.5 | nM | CHEMBL4639478 |
| 6.80 | IC50 | 158.5 | nM | CHEMBL4649677 |
| 6.70 | IC50 | 199.5 | nM | CHEMBL4641977 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL4643099 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL4643782 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL4644464 |
| 6.60 | IC50 | 251.2 | nM | CHEMBL4636806 |
| 6.40 | IC50 | 398.1 | nM | CHEMBL4645342 |
| 6.10 | IC50 | 794.3 | nM | CHEMBL4636379 |
| 6.00 | IC50 | 1000 | nM | CHEMBL4643675 |
| 6.00 | IC50 | 1000 | nM | CHEMBL4636463 |
| 6.00 | IC50 | 1000 | nM | CHEMBL4640863 |
| 6.00 | IC50 | 1000 | nM | CHEMBL4643908 |
| 5.90 | IC50 | 1259 | nM | CHEMBL4642795 |
| 5.80 | IC50 | 1585 | nM | CHEMBL4646350 |
| 5.80 | IC50 | 1585 | nM | CHEMBL4632512 |
| 5.80 | IC50 | 1585 | nM | CHEMBL4634598 |
| 5.80 | IC50 | 1585 | nM | CHEMBL4645578 |
| 5.70 | IC50 | 1995 | nM | CHEMBL4640676 |
| 5.70 | IC50 | 1995 | nM | CHEMBL4639235 |
| 5.70 | IC50 | 1995 | nM | CHEMBL4644324 |
| 5.60 | IC50 | 2512 | nM | CHEMBL4645552 |
| 5.60 | IC50 | 2512 | nM | CHEMBL4636625 |
| 5.50 | IC50 | 3162 | nM | CHEMBL4641818 |
| 5.50 | IC50 | 3162 | nM | CHEMBL4636282 |
| 5.40 | IC50 | 3981 | nM | CHEMBL4648272 |
| 5.30 | IC50 | 5012 | nM | CHEMBL4641304 |
| 5.30 | IC50 | 5012 | nM | CHEMBL4646429 |
| 5.10 | IC50 | 7943 | nM | CHEMBL4638043 |
| 5.10 | IC50 | 7943 | nM | CHEMBL4649884 |
PubChem BioAssay actives
33 with measured affinity, of 57 total; 33 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-(3,4-dichlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1000 | uM |
| 2-oxo-5-phenyl-N-[2-[4-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]ethyl]pentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1000 | uM |
| N-[2-(4-methylphenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1259 | uM |
| N-[2-(4-bromophenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1585 | uM |
| 2-oxo-5-phenyl-N-[2-[4-[[6-(trifluoromethyl)-3-pyridinyl]oxy]phenyl]ethyl]pentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1585 | uM |
| N-[2-(3-chlorophenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.1995 | uM |
| N-[2-[4-(2-chloropyrimidin-4-yl)oxyphenyl]ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.2512 | uM |
| 2-oxo-5-phenyl-N-[2-(4-pyrazin-2-yloxyphenyl)ethyl]pentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.2512 | uM |
| N-[2-(2,4-dichlorophenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.2512 | uM |
| 2-oxo-N-[2-(4-phenoxyphenyl)ethyl]-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.2512 | uM |
| 2-oxo-5-phenyl-N-(2-phenylethyl)pentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.3981 | uM |
| N-[2-(4-methoxyphenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 0.7943 | uM |
| 4-(4-chlorophenyl)-2-oxo-N-(4-phenylbutyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.0000 | uM |
| 2-oxo-6-phenyl-N-(2-phenylethyl)hexanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.0000 | uM |
| 4-(4-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.0000 | uM |
| N-[2-(3,4-dimethoxyphenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.0000 | uM |
| N-[2-(2-chlorophenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.2589 | uM |
| (E)-2-oxo-4-phenyl-N-(2-phenylethyl)but-3-enamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.5849 | uM |
| 4-(3-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.5849 | uM |
| N-[2-(4-hydroxyphenyl)ethyl]-2-oxo-5-phenylpentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.5849 | uM |
| N-benzyl-4-(4-chlorophenyl)-2-oxobutanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.5849 | uM |
| 4-(2-chlorophenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.9953 | uM |
| 4-(4-methylphenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.9953 | uM |
| 2-oxo-5-phenyl-N-[2-(4-pyrimidin-2-yloxyphenyl)ethyl]pentanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 1.9953 | uM |
| (E)-4-(4-bromophenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 2.5119 | uM |
| (E)-4-(4-chlorophenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 2.5119 | uM |
| (E)-2-oxo-N-(2-phenylethyl)-4-(3-phenylphenyl)but-3-enamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 3.1623 | uM |
| 4-(4-methoxyphenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 3.1623 | uM |
| 2-oxo-4-(4-phenoxyphenyl)-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 3.9811 | uM |
| 4-(4-fluorophenyl)-2-oxo-N-(2-phenylethyl)butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 5.0119 | uM |
| (E)-4-(4-methoxyphenyl)-2-oxo-N-(2-phenylethyl)but-3-enamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 5.0119 | uM |
| 4-(4-chlorophenyl)-N-ethyl-2-oxobutanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 7.9433 | uM |
| 2-oxo-N-(2-phenylethyl)-4-[4-(trifluoromethyl)phenyl]butanamide | 1666052: Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | ic50 | 7.9433 | uM |
CTD chemical–gene interactions
48 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, increases expression | 6 |
| sodium arsenite | affects expression, decreases expression, increases expression | 5 |
| Tetrachlorodibenzodioxin | increases expression | 3 |
| Cadmium Chloride | decreases expression, increases abundance, increases expression | 3 |
| nickel sulfate | increases expression | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| Benzo(a)pyrene | decreases expression, increases expression | 2 |
| Cisplatin | affects expression, affects cotreatment, increases expression | 2 |
| Dexamethasone | increases expression, affects cotreatment | 2 |
| Quercetin | affects cotreatment, increases expression | 2 |
| Cyclosporine | decreases expression | 2 |
| 3,19-(2-bromobenzylidene)andrographolide | decreases response to substance, increases expression | 1 |
| bisphenol F | affects cotreatment, increases expression | 1 |
| dicrotophos | decreases expression | 1 |
| potassium perchlorate | decreases expression | 1 |
| sodium arsenate | decreases expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| mono-(2-ethylhexyl)phthalate | increases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | decreases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | increases expression, affects cotreatment | 1 |
| belinostat | affects cotreatment, increases expression | 1 |
| ICG 001 | increases expression | 1 |
| Grape Seed Proanthocyanidins | decreases expression, affects cotreatment | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| Temozolomide | increases expression | 1 |
| Decitabine | affects expression | 1 |
| Acetaminophen | decreases expression | 1 |
| Ascorbic Acid | affects cotreatment, increases expression | 1 |
ChEMBL screening assays
2 unique, capped per target: 2 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4626913 | Binding | Inhibition of full-length C-terminal FLAG-tagged human PLAAT3 expressed in HEK293T cell lysate preincubated for 30 mins followed by MB064 addition and measured after 20 mins by SDS-PAGE based ABPP analysis | Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family. — J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Associated diseases: lipodystrophy, familial partial, type 9
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): lipodystrophy, familial partial, type 9