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AGPAT2

gene
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Also known as LPAAT-betaLPLAT2

Summary

AGPAT2 (1-acylglycerol-3-phosphate O-acyltransferase 2, HGNC:325) is a protein-coding gene on chromosome 9q34.3, encoding 1-acyl-sn-glycerol-3-phosphate acyltransferase beta (O15120). Converts 1-acyl-sn-glycerol-3-phosphate (lysophosphatidic acid or LPA) into 1,2-diacyl-sn-glycerol-3-phosphate (phosphatidic acid or PA) by incorporating an acyl moiety at the sn-2 position of the glycerol backbone.

This gene encodes a member of the 1-acylglycerol-3-phosphate O-acyltransferase family. The protein is located within the endoplasmic reticulum membrane and converts lysophosphatidic acid to phosphatidic acid, the second step in de novo phospholipid biosynthesis. Mutations in this gene have been associated with congenital generalized lipodystrophy (CGL), or Berardinelli-Seip syndrome, a disease characterized by a near absence of adipose tissue and severe insulin resistance. Alternate transcriptional splice variants, encoding different isoforms, have been characterized.

Source: NCBI Gene 10555 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): lipodystrophy (Definitive, ClinGen) — +3 more curated relationships
  • Clinical variants (ClinVar): 295 total — 19 pathogenic, 9 likely-pathogenic
  • Phenotypes (HPO): 40
  • Druggable target: yes
  • Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
  • MANE Select transcript: NM_006412

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:325
Approved symbolAGPAT2
Name1-acylglycerol-3-phosphate O-acyltransferase 2
Location9q34.3
Locus typegene with protein product
StatusApproved
AliasesLPAAT-beta, LPLAT2
Ensembl geneENSG00000169692
Ensembl biotypeprotein_coding
OMIM603100
Entrez10555

Gene structure

Transcript identifiers

Ensembl transcripts: 14 — 12 protein_coding, 2 retained_intron

ENST00000371694, ENST00000371696, ENST00000470861, ENST00000472820, ENST00000882832, ENST00000882833, ENST00000882834, ENST00000882835, ENST00000882836, ENST00000882837, ENST00000882838, ENST00000951405, ENST00000951406, ENST00000951407

RefSeq mRNA: 2 — MANE Select: NM_006412 NM_001012727, NM_006412

CCDS: CCDS35181, CCDS7003

Canonical transcript exons

ENST00000371696 — 6 exons

ExonStartEnd
ENSE00001195409136676961136677136
ENSE00001195414136677423136677556
ENSE00001390768136673143136673927
ENSE00001455876136687176136687457
ENSE00003541941136674735136674807
ENSE00003601996136676585136676680

Expression profiles

Bgee: expression breadth ubiquitous, 257 present calls, max score 98.81.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 11.1272 / max 236.6465, expressed in 1748 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
1031907.16651711
1031893.88371163
1031870.077016

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
mucosa of transverse colonUBERON:000499198.81gold quality
ileal mucosaUBERON:000033198.69gold quality
right lobe of liverUBERON:000111498.56gold quality
subcutaneous adipose tissueUBERON:000219097.77gold quality
omental fat padUBERON:001041497.74gold quality
adipose tissueUBERON:000101397.69gold quality
peritoneumUBERON:000235897.69gold quality
adipose tissue of abdominal regionUBERON:000780897.66gold quality
lower esophagus mucosaUBERON:003583496.80gold quality
connective tissueUBERON:000238496.73gold quality
body of pancreasUBERON:000115096.46gold quality
apex of heartUBERON:000209896.33gold quality
transverse colonUBERON:000115795.59gold quality
right atrium auricular regionUBERON:000663195.33gold quality
small intestine Peyer’s patchUBERON:000345495.12gold quality
duodenumUBERON:000211494.77gold quality
right lungUBERON:000216794.64gold quality
cardiac atriumUBERON:000208194.61gold quality
liverUBERON:000210794.50gold quality
esophagus mucosaUBERON:000246994.50gold quality
small intestineUBERON:000210894.27gold quality
upper lobe of left lungUBERON:000895294.24gold quality
olfactory segment of nasal mucosaUBERON:000538694.13gold quality
jejunal mucosaUBERON:000039993.99gold quality
heart left ventricleUBERON:000208493.73gold quality
cardiac ventricleUBERON:000208293.49gold quality
body of stomachUBERON:000116193.44gold quality
upper lobe of lungUBERON:000894893.38gold quality
endometrium epitheliumUBERON:000481193.25gold quality
monocyteCL:000057692.93gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

ExperimentMarker?Max mean expression
E-GEOD-125970yes72.59
E-MTAB-8410yes25.79
E-ANND-3yes20.91
E-GEOD-135922yes20.14
E-MTAB-8142yes17.33

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

7 targeting AGPAT2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-574-5P100.0066.01989
HSA-MIR-7111-5P99.9768.482062
HSA-MIR-449299.8768.253611
HSA-MIR-6752-3P99.7266.711587
HSA-MIR-429098.5165.17907
HSA-MIR-3173-5P97.3565.821282
HSA-MIR-6799-3P97.3565.601302

Functional genomics

ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 25)

  • AGPAT2 is mutated in congenital generalized lipodystrophy linked to chromosome 9q34. (PMID:11967537)
  • Congenital lipodystrophy patients with Seipin mutations have a more severe lack of body fat, which affects both metabolically active and mechanical adipose tissue, compared with patients with mutations in the AGPAT2 gene. (PMID:14602785)
  • mutations in AGPAT2 and Gng3lg are approximately equally represented in congenital generalized lipodystrophy (PMID:15181077)
  • reduction in AGPAT2 enzymatic activity underlies the loss of adipose tissue in congenital generalized lipodystrophy (PMID:15629135)
  • Our study shows that LPAAT-beta is upregulated in ovarian cancer and is more prevalent in poorly differentiated tumours (PMID:15841084)
  • mutations in AGPAT2 or Seipin may have roles in Berardinelli-Seip congenital lipodystrophy (PMID:16435205)
  • Berardinelli-Seip syndrome is a congenital form of generalized lipodystrophy, transmitted as an autosomal recessive trait. It is well documented in medicine and skin. It is a rare disorder caused by mutations of AGPAT2 gene or BSCL2 gene. (PMID:18155601)
  • A new subtype of congenital generalized lipodystrophy is not associated with the AGPAT2 gene. (PMID:18698612)
  • We have demonstrated four novel mutations of the BSCL2 and AGPAT2 genes responsible for Berardinelli-Seip syndrome and Brunzell syndrome (AGPAT2-related syndrome). (PMID:19226263)
  • Study showed that the cellular level of lysophosphatidic acid was increased in AGPAT2 deficient cells. (PMID:19278620)
  • Lysophosphatidic acid acyltransferase beta (LPAATbeta) promotes the tumor growth of human osteosarcoma (PMID:21152068)
  • lpaat beta gene overexpression exists in both AML and CML patients. lpaat beta produced by AML cells probably plays an important role in abnormal proliferation and drug-resistance of AML cells. (PMID:21176343)
  • the role of AGPAT1 or AGPAT2 in liver lipogenesis is minimal and that accumulation of liver fat is primarily a consequence of insulin resistance (PMID:21873652)
  • Data suggest that AGPAT2 regulates adipogenesis through modulation of lipid metabolism/signal transduction, altering normal activation of phosphatidylinositol 3-kinase (PI3K)/protooncogene c-Akt and PPARgamma signaling in early stage of adipogenesis. (PMID:22872237)
  • novel nonsense a missense mutations were found in two patients with congenital generalized lipodystrophy type 1. (PMID:22902344)
  • miR-24 may play an important role in inhibiting osteosarcoma growth through suppression of LPAATbeta. (PMID:23578572)
  • the ability of LPAAT-beta to regulate mTOR function (PMID:24205284)
  • Data show that missense mutation c.299G>A changes serine in the acyltransferase NHX4D motif of AGPAT2, and intronic c.493-1G>C mutation destroy a splicing site that leads to exon 4 skipping and deletion of whole AGPAT2 substrate binding domain. (PMID:24498038)
  • Results show that LPAATbeta had high expression in osteosarcoma patients who received cisplatin treatment and cisplatin-resistant cancer cell lines. In vitro and in vivo studies provide evidence that LPAATB plays an important role in osteosarcoma. (PMID:28035350)
  • The findings demonstrate that AGPAT2, which is mutated in patients with congenital generalized lipodystrophy and over-expressed in different types of cancer, is a direct transcriptional target of HIF-1, suggesting that upregulation of lipid storage by HIF-1 plays an important role in adaptation and survival of cancer cells under low oxygen conditions. (PMID:29908837)
  • Oligomers of the lipodystrophy protein seipin may co-ordinate GPAT3 and AGPAT2 enzymes to facilitate adipocyte differentiation. (PMID:32094408)
  • Congenital Generalized Lipoatrophy (Berardinelli-Seip Syndrome) Type 1: Description of Novel AGPAT2 Homozygous Variants Showing the Highly Heterogeneous Presentation of the Disease. (PMID:32117065)
  • A rare frameshift mutation in the AGPAT2 gene in a family from gaza with congenital generalized lipodystrophy. (PMID:32412105)
  • Circular RNA circ-CHI3L1.2 modulates cisplatin resistance of osteosarcoma cells via the miR-340-5p/LPAATbeta axis. (PMID:34164774)
  • AGPAT2 interaction with CDP-diacylglycerol synthases promotes the flux of fatty acids through the CDP-diacylglycerol pathway. (PMID:34824276)

Cross-species orthologs

7 orthologs

OrganismSymbolGene ID
danio_rerioagpat2ENSDARG00000101139
mus_musculusAgpat2ENSMUSG00000026922
rattus_norvegicusAgpat2ENSRNOG00000019466
drosophila_melanogasterAgpat2FBGN0026718
drosophila_melanogasterAgpat1FBGN0030421
caenorhabditis_elegansWBGENE00010339
caenorhabditis_elegansWBGENE00011543

Paralogs (1): AGPAT1 (ENSG00000204310)

Protein

Protein identifiers

1-acyl-sn-glycerol-3-phosphate acyltransferase beta — O15120 (reviewed: O15120)

Alternative names: 1-acylglycerol-3-phosphate O-acyltransferase 2, Lysophosphatidic acid acyltransferase beta

All UniProt accessions (2): A0A024R8F9, O15120

UniProt curated annotations — full annotation on UniProt →

Function. Converts 1-acyl-sn-glycerol-3-phosphate (lysophosphatidic acid or LPA) into 1,2-diacyl-sn-glycerol-3-phosphate (phosphatidic acid or PA) by incorporating an acyl moiety at the sn-2 position of the glycerol backbone.

Subcellular location. Endoplasmic reticulum membrane.

Tissue specificity. Expressed predominantly in adipose tissue, pancreas and liver.

Disease relevance. Lipodystrophy, congenital generalized, 1 (CGL1) [MIM:608594] A form of congenital generalized lipodystrophy, a metabolic disorder characterized by a near complete absence of adipose tissue, extreme insulin resistance, hypertriglyceridemia, hepatic steatosis and early onset of diabetes. Inheritance is autosomal recessive. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The HXXXXD motif is essential for acyltransferase activity and may constitute the binding site for the phosphate moiety of the glycerol-3-phosphate.

Pathway. Phospholipid metabolism; CDP-diacylglycerol biosynthesis; CDP-diacylglycerol from sn-glycerol 3-phosphate: step 2/3.

Similarity. Belongs to the 1-acyl-sn-glycerol-3-phosphate acyltransferase family.

Isoforms (2)

UniProt IDNamesCanonical?
O15120-11yes
O15120-22

RefSeq proteins (2): NP_001012745, NP_006403* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR002123Plipid/glycerol_acylTrfaseDomain
IPR004552AGP_acyltransDomain

Pfam: PF01553

Enzyme classification (BRENDA):

  • EC 2.3.1.51 — 1-acylglycerol-3-phosphate O-acyltransferase (BRENDA: 39 organisms, 381 substrates, 31 inhibitors, 32 Km, 4 kcat entries)

Substrate kinetics (BRENDA)

7 substrates with measured Km, best-characterized 7. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
1-ACYL-SN-GLYCEROL 3-PHOSPHATE0.0053–0.1258
OLEOYL-COA0.0027–0.02158
PALMITOYL-COA0.0014–0.0128
1-OLEOYL-SN-GLYCEROL 3-PHOSPHATE0.0048–0.0185
1-PALMITOYL-SN-GLYCEROL 3-PHOSPHATE0.0031
DOCOSAHEXAENOYL-COA0.01381
PAMITOLEOYL-COA0.03681

Catalyzed reactions (Rhea), 12 shown:

  • a 1-acyl-sn-glycero-3-phosphate + an acyl-CoA = a 1,2-diacyl-sn-glycero-3-phosphate + CoA (RHEA:19709)
  • 1-hexadecanoyl-sn-glycero-3-phosphate + (9Z)-octadecenoyl-CoA = 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphate + CoA (RHEA:33187)
  • 1-hexadecanoyl-sn-glycero-3-phosphate + tetradecanoyl-CoA = 1-hexadecanoyl-2-tetradecanoyl-sn-glycero-3-phosphate + CoA (RHEA:35899)
  • 1-hexadecanoyl-sn-glycero-3-phosphate + hexadecanoyl-CoA = 1,2-dihexadecanoyl-sn-glycero-3-phosphate + CoA (RHEA:35903)
  • 1-hexadecanoyl-sn-glycero-3-phosphate + octadecanoyl-CoA = 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphate + CoA (RHEA:35907)
  • 1-hexadecanoyl-sn-glycero-3-phosphate + (5Z,8Z,11Z,14Z)-eicosatetraenoyl-CoA = 1-hexadecanoyl-2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-sn-glycero-3-phosphate + CoA (RHEA:35915)
  • 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate + (9Z)-octadecenoyl-CoA = 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphate + CoA (RHEA:37131)
  • 1-(9Z,12Z,15Z)-octadecatrienoyl-sn-glycero-3-phosphate + (9Z)-octadecenoyl-CoA = 1-(9Z,12Z,15Z)-octadecatrienoyl-2-(9Z)-octadecenoyl-sn-glycero-3-phosphate + CoA (RHEA:37139)
  • 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate + hexadecanoyl-CoA = 1-(9Z)-octadecenoyl-2-hexadecanoyl-sn-glycero-3-phosphate + CoA (RHEA:37143)
  • heptadecanoyl-CoA + 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate = 1-(9Z)-octadecenoyl-2-heptadecanoyl-sn-glycero-3-phosphate + CoA (RHEA:37155)
  • 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate + (9Z,12Z)-octadecadienoyl-CoA = 1-(9Z)-octadecenoyl-2-(9Z,12Z)-octadecadienoyl-sn-glycero-3-phosphate + CoA (RHEA:37159)
  • 1-(9Z-octadecenoyl)-sn-glycero-3-phosphate + tetradecanoyl-CoA = 1-(9Z)-octadecenoyl-2-tetradecanoyl-sn-glycero-3-phosphate + CoA (RHEA:37171)

UniProt features (16 total): sequence variant 4, topological domain 3, sequence conflict 2, transmembrane region 2, short sequence motif 2, signal peptide 1, chain 1, splice variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O15120-F191.660.80

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

IDPathway
R-HSA-1483166Synthesis of PA
R-HSA-6798695Neutrophil degranulation
R-HSA-9841922MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis

MSigDB gene sets: 257 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, BOYAULT_LIVER_CANCER_SUBCLASS_G56_DN, BERTUCCI_MEDULLARY_VS_DUCTAL_BREAST_CANCER_DN, GOBP_RESPONSE_TO_PEPTIDE, GOCC_SECRETORY_GRANULE, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, DACOSTA_UV_RESPONSE_VIA_ERCC3_UP, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_CYTOKINE_PRODUCTION, MODULE_16, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_PHOSPHOLIPID_BIOSYNTHETIC_PROCESS, SHAFFER_IRF4_TARGETS_IN_PLASMA_CELL_VS_MATURE_B_LYMPHOCYTE, GOBP_GLYCEROLIPID_METABOLIC_PROCESS

GO Biological Process (10): positive regulation of cytokine production (GO:0001819), positive regulation of cytokine-mediated signaling pathway (GO:0001961), phospholipid metabolic process (GO:0006644), phosphatidic acid biosynthetic process (GO:0006654), epidermis development (GO:0008544), response to xenobiotic stimulus (GO:0009410), CDP-diacylglycerol biosynthetic process (GO:0016024), triglyceride biosynthetic process (GO:0019432), lipid metabolic process (GO:0006629), phospholipid biosynthetic process (GO:0008654)

GO Molecular Function (3): 1-acylglycerol-3-phosphate O-acyltransferase activity (GO:0003841), transferase activity (GO:0016740), acyltransferase activity (GO:0016746)

GO Cellular Component (5): endoplasmic reticulum (GO:0005783), endoplasmic reticulum membrane (GO:0005789), plasma membrane (GO:0005886), specific granule membrane (GO:0035579), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-3 pathways:

CategoryPathways
Glycerophospholipid biosynthesis1
Innate Immune System1
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
glycerophospholipid biosynthetic process2
cytokine production1
regulation of cytokine production1
positive regulation of gene expression1
positive regulation of multicellular organismal process1
regulation of cytokine-mediated signaling pathway1
positive regulation of signal transduction1
cytokine-mediated signaling pathway1
positive regulation of response to cytokine stimulus1
lipid metabolic process1
organophosphate metabolic process1
phosphatidic acid metabolic process1
tissue development1
response to chemical1
CDP-diacylglycerol metabolic process1
triglyceride metabolic process1
acylglycerol biosynthetic process1
primary metabolic process1
phospholipid metabolic process1
lipid biosynthetic process1
organophosphate biosynthetic process1
acylglycerol O-acyltransferase activity1
lysophosphatidic acid acyltransferase activity1
catalytic activity1
transferase activity1
cytoplasm1
endomembrane system1
intracellular membrane-bounded organelle1
organelle membrane1
nuclear outer membrane-endoplasmic reticulum membrane network1
endoplasmic reticulum subcompartment1
membrane1
cell periphery1
secretory granule membrane1
specific granule1
cellular anatomical structure1

Protein interactions and networks

STRING

1894 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
AGPAT2BSCL2Q96G97988
AGPAT2LPCAT2Q7L5N7878
AGPAT2CAV1Q03135842
AGPAT2CAVIN1Q6NZI2840
AGPAT2LPIN1Q14693804
AGPAT2ZMPSTE24O75844798
AGPAT2GPAT3Q53EU6750
AGPAT2GPAMQ9HCL2723
AGPAT2GPAT4Q86UL3723
AGPAT2LMNAP02545722
AGPAT2AGPAT3Q9NRZ7717
AGPAT2PBX3P40426711
AGPAT2GZMBP10144669
AGPAT2AGPAT4Q9NRZ5667
AGPAT2DGAT1O75907661

IntAct

70 interactions, top by confidence:

ABTypeScore
CFTRESYT2psi-mi:“MI:0914”(association)0.710
SLC1A1AGPAT2psi-mi:“MI:0914”(association)0.640
APLNRSLC33A1psi-mi:“MI:0914”(association)0.530
TMEM184ASLC33A1psi-mi:“MI:0914”(association)0.530
EVA1CSTK25psi-mi:“MI:0914”(association)0.530
SIGMAR1NPC1psi-mi:“MI:0914”(association)0.530
ATP1A3AGPAT2psi-mi:“MI:0914”(association)0.530
AGPAT2GMPSpsi-mi:“MI:0915”(physical association)0.370
AGPAT2SLC23A2psi-mi:“MI:0915”(physical association)0.370
AGPAT2ANKRD28psi-mi:“MI:0915”(physical association)0.370
PHF11AGPAT2psi-mi:“MI:0915”(physical association)0.370
AGPAT2PHRF1psi-mi:“MI:0915”(physical association)0.370
ABCG8AGPAT2psi-mi:“MI:0915”(physical association)0.370
STING1AGPAT2psi-mi:“MI:0914”(association)0.350
MS4A4AMON2psi-mi:“MI:0914”(association)0.350
SLC15A3psi-mi:“MI:0914”(association)0.350
UNC93B1psi-mi:“MI:0914”(association)0.350
P2RY6RAVER1psi-mi:“MI:0914”(association)0.350
ESR1ESYT2psi-mi:“MI:0914”(association)0.350
Mpsi-mi:“MI:0914”(association)0.350
AGPAT2TMEM120Bpsi-mi:“MI:0914”(association)0.350
TTYH1TMEM223psi-mi:“MI:0914”(association)0.350
SLC6A15GPR89Apsi-mi:“MI:0914”(association)0.350
FFAR1SLC12A8psi-mi:“MI:0914”(association)0.350
GPR182SLC12A8psi-mi:“MI:0914”(association)0.350
PCDHB3ESYT2psi-mi:“MI:0914”(association)0.350
CLEC2DESYT2psi-mi:“MI:0914”(association)0.350

BioGRID (84): HIST1H1D (Affinity Capture-MS), HIST1H1D (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), INTU (Affinity Capture-MS), AGPAT2 (Affinity Capture-RNA), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Affinity Capture-MS), AGPAT2 (Proximity Label-MS), AGPAT2 (Proximity Label-MS)

ESM2 similar proteins: A4IFH5, A7MBI7, O15120, O75452, O88587, P22734, P24298, P25409, P97849, Q1HAQ0, Q1LWG4, Q2TBP5, Q3KPP4, Q3SYC2, Q3T0A0, Q3T0R4, Q3TFD2, Q3ZKN0, Q4R3Y4, Q501J2, Q5E9M9, Q5H879, Q5M7F4, Q5M8H5, Q5R7A2, Q5RDY4, Q5RK23, Q60714, Q6P1M0, Q6P2H8, Q6PCB7, Q70VZ8, Q7TSA0, Q80W94, Q8IXI1, Q8JZN7, Q8K3K7, Q8K4X7, Q8NF37, Q8QZR5

Diamond homologs: A8J0J0, D5AQD5, O15120, P0A257, P0A258, P26647, P33333, P75479, Q49402, Q8GXU8, Q8K3K7, Q95JH0, Q95JH2, Q99943, Q9LLY4, Q9US20, O25903, O35083, P44848, Q22267, Q42670, Q42868, Q42870, Q59188, Q93841, Q9I7C1, Q9ZJN8, Q59601, Q9JU41, Q9JZ47, Q41745, Q9SYC8, Q7APG1, A1AF47, A1JPF0, A4TLD3, A6TDH2, A7FFD1, A7ZQU2, A8A3X0

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 87 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
R-HSA-425366517.4×8e-04
SLC-mediated transmembrane transport89.1×6e-04
Transport of small molecules115.3×6e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic19
Likely pathogenic9
Uncertain significance141
Likely benign54
Benign19

Top pathogenic / likely-pathogenic (28)

Variant IDHGVSClassification
1072415NM_006412.4(AGPAT2):c.369_372del (p.Leu124fs)Pathogenic
1334446NM_006412.4(AGPAT2):c.313A>G (p.Met105Val)Pathogenic
1687558NM_006412.4(AGPAT2):c.38T>A (p.Leu13Ter)Pathogenic
210104NM_006412.4(AGPAT2):c.406G>A (p.Gly136Arg)Pathogenic
2506961NM_006412.4(AGPAT2):c.316+1G>TPathogenic
285946NM_006412.4(AGPAT2):c.282del (p.Ile94fs)Pathogenic
3256879NM_006412.4(AGPAT2):c.530_537dup (p.Asp180fs)Pathogenic
372105NM_006412.4(AGPAT2):c.299G>A (p.Ser100Asn)Pathogenic
372107NM_006412.3(AGPAT2):c.(316+1_317-1)_(588+1_589-1)del (p.Leu107AlafsTer279)Pathogenic
374338NM_006412.4(AGPAT2):c.503G>A (p.Trp168Ter)Pathogenic
4848905NM_006412.4(AGPAT2):c.176_178delinsC (p.Asn59fs)Pathogenic
549711NM_006412.4(AGPAT2):c.513del (p.Glu172fs)Pathogenic
549712NM_006412.4(AGPAT2):c.622_626del (p.Ser208fs)Pathogenic
6624NM_006412.4(AGPAT2):c.202C>T (p.Arg68Ter)Pathogenic
6625NM_006412.4(AGPAT2):c.589-2A>GPathogenic
6627NM_006412.4(AGPAT2):c.683T>C (p.Leu228Pro)Pathogenic
6629NM_006412.4(AGPAT2):c.643A>T (p.Lys215Ter)Pathogenic
6631NM_006412.4(AGPAT2):c.570C>A (p.Tyr190Ter)Pathogenic
6632NM_006412.4(AGPAT2):c.366_588+534delPathogenic
1285417NM_006412.4(AGPAT2):c.685G>T (p.Glu229Ter)Likely pathogenic
1806161NM_006412.4(AGPAT2):c.493-2A>GLikely pathogenic
2629060NM_006412.4(AGPAT2):c.656_660del (p.Thr219fs)Likely pathogenic
3065518NM_006412.4(AGPAT2):c.158del (p.Gly53fs)Likely pathogenic
3234919NM_006412.4(AGPAT2):c.254_258dup (p.Gln87fs)Likely pathogenic
3596810NM_006412.4(AGPAT2):c.769del (p.Leu257fs)Likely pathogenic
3596834NM_006412.4(AGPAT2):c.242_245del (p.Arg81fs)Likely pathogenic
3596844NM_006412.4(AGPAT2):c.34del (p.Leu12fs)Likely pathogenic
365928NM_006412.4(AGPAT2):c.335C>T (p.Pro112Leu)Likely pathogenic

SpliceAI

1075 predictions. Top by Δscore:

VariantEffectΔscore
9:136673923:TGTTC:Tacceptor_gain1.0000
9:136673924:GTTC:Gacceptor_gain1.0000
9:136673925:TTC:Tacceptor_gain1.0000
9:136673926:TC:Tacceptor_gain1.0000
9:136673927:CC:Cacceptor_gain1.0000
9:136673928:C:CAacceptor_loss1.0000
9:136673928:C:CCacceptor_gain1.0000
9:136674732:TA:Tdonor_loss1.0000
9:136674733:ACC:Adonor_loss1.0000
9:136674750:T:TAdonor_gain1.0000
9:136674808:C:CCacceptor_gain1.0000
9:136676580:CCTA:Cdonor_loss1.0000
9:136676583:ACCTG:Adonor_loss1.0000
9:136676584:C:Adonor_loss1.0000
9:136676676:TTGAG:Tacceptor_gain1.0000
9:136676677:TGAG:Tacceptor_gain1.0000
9:136676680:GCT:Gacceptor_loss1.0000
9:136676681:C:CCacceptor_gain1.0000
9:136676955:A:ACdonor_gain1.0000
9:136676956:C:CCdonor_gain1.0000
9:136676957:TCA:Tdonor_loss1.0000
9:136676958:CACG:Cdonor_loss1.0000
9:136676959:A:ACdonor_gain1.0000
9:136676959:ACGTT:Adonor_gain1.0000
9:136676960:C:CGdonor_gain1.0000
9:136676960:CG:Cdonor_gain1.0000
9:136676960:CGTT:Cdonor_gain1.0000
9:136676960:CGTTC:Cdonor_gain1.0000
9:136676966:C:CAdonor_gain1.0000
9:136677132:GAGGC:Gacceptor_gain1.0000

AlphaMissense

1796 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
9:136676606:G:CF189L0.998
9:136676606:G:TF189L0.998
9:136676608:A:GF189L0.998
9:136677447:G:CH98D0.998
9:136677448:G:CN97K0.998
9:136677448:G:TN97K0.998
9:136676661:G:TP171H0.997
9:136677093:C:AK120N0.997
9:136677093:C:GK120N0.997
9:136677461:A:TV93D0.997
9:136676618:C:AK185N0.996
9:136676618:C:GK185N0.996
9:136676656:C:GG173R0.996
9:136676657:C:AE172D0.996
9:136676657:C:GE172D0.996
9:136676671:A:GW168R0.996
9:136676671:A:TW168R0.996
9:136677431:T:AD103V0.996
9:136677431:T:GD103A0.996
9:136677439:G:CS100R0.996
9:136677439:G:TS100R0.996
9:136677441:T:GS100R0.996
9:136677445:G:CH98Q0.996
9:136677445:G:TH98Q0.996
9:136677447:G:TH98N0.996
9:136674800:A:TI199N0.995
9:136676598:G:TA192E0.995
9:136676622:A:GF184S0.995
9:136676650:G:TR175S0.995
9:136676658:T:AE172V0.995

dbSNP variants (sampled 300 via entrez): RS1000080974 (9:136675217 C>G,T), RS1000350217 (9:136689390 G>A), RS1000453959 (9:136684380 C>T), RS1000659746 (9:136680299 T>C), RS1000956046 (9:136688493 G>T), RS1001059960 (9:136683676 G>A), RS1001215760 (9:136675794 G>T), RS1001755560 (9:136680373 C>T), RS1001776620 (9:136685014 G>A,C), RS1002010297 (9:136676292 C>G,T), RS1002385746 (9:136676125 G>A), RS1002394445 (9:136687728 AC>A,ACC), RS1002448412 (9:136687971 C>G), RS1003229436 (9:136673844 G>A,C), RS1003357757 (9:136686098 T>C)

Disease associations

OMIM: gene MIM:603100 | disease phenotypes: MIM:608594

GenCC curated gene-disease

DiseaseClassificationInheritance
congenital generalized lipodystrophy type 1DefinitiveAutosomal recessive
Berardinelli-Seip congenital lipodystrophySupportiveAutosomal recessive
neonatal diabetes mellitusLimitedAutosomal recessive

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

DiseaseClassificationInheritance
lipodystrophyDefinitiveAR

Mondo (6): congenital generalized lipodystrophy type 1 (MONDO:0012071), congenital generalized lipodystrophy (MONDO:0006536), prostate cancer (MONDO:0008315), monogenic diabetes (MONDO:0015967), neonatal diabetes mellitus (MONDO:0016391), Berardinelli-Seip congenital lipodystrophy (MONDO:0018883)

Orphanet (4): Congenital generalized lipodystrophy (Orphanet:528), Congenital generalized lipodystrophy type 1 (Orphanet:696189), Familial prostate cancer (Orphanet:1331), Rare genetic diabetes mellitus (Orphanet:183625)

HPO phenotypes

40 total (30 of 40 shown, HPO-id order):

HPOTerm
HP:0000007Autosomal recessive inheritance
HP:0000065Labial hypertrophy
HP:0000098Tall stature
HP:0000147Polycystic ovaries
HP:0000303Mandibular prognathia
HP:0000325Triangular face
HP:0000400Macrotia
HP:0000787Nephrolithiasis
HP:0000819Diabetes mellitus
HP:0000842Hyperinsulinemia
HP:0000868Decreased fertility in females
HP:0000877Insulin-resistant diabetes mellitus at puberty
HP:0000956Acanthosis nigricans
HP:0001007Hirsutism
HP:0001176Large hands
HP:0001249Intellectual disability
HP:0001394Cirrhosis
HP:0001397Hepatic steatosis
HP:0001537Umbilical hernia
HP:0001544Prominent umbilicus
HP:0001638Cardiomyopathy
HP:0001735Acute pancreatitis
HP:0001744Splenomegaly
HP:0001833Long foot
HP:0002155Hypertriglyceridemia
HP:0002240Hepatomegaly
HP:0002591Polyphagia
HP:0002833Cystic angiomatosis of bone
HP:0002910Elevated circulating hepatic transaminase concentration
HP:0003292Decreased serum leptin

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

DescriptorNameTree numbers
D011471Prostatic NeoplasmsC04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4772 (SINGLE PROTEIN)

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

ChEMBL bioactivities

111 potent at pChembl≥5 of 122 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.22IC506nMCHEMBL34896
8.08IC508.4nMCHEMBL5219455
8.00IC5010nMCHEMBL75167
7.82IC5015nMCHEMBL5219496
7.82IC5015nMCHEMBL35508
7.82IC5015nMCHEMBL286394
7.82IC5015nMCHEMBL35388
7.80IC5016nMCHEMBL310136
7.77IC5017nMCHEMBL308945
7.77IC5017nMCHEMBL77883
7.75IC5018nMCHEMBL74548
7.70IC5020nMCHEMBL307716
7.66IC5022nMCHEMBL311379
7.62IC5024nMCHEMBL74492
7.57IC5027nMCHEMBL422579
7.55IC5028nMCHEMBL424605
7.55IC5028nMCHEMBL74708
7.51IC5031nMCHEMBL74549
7.47IC5034nMCHEMBL73376
7.47IC5034nMCHEMBL72618
7.46IC5035nMCHEMBL32894
7.40IC5040nMCHEMBL193874
7.40IC5040nMCHEMBL284111
7.35IC5045nMCHEMBL195457
7.30IC5050nMCHEMBL194604
7.30IC5050nMCHEMBL193911
7.30IC5050nMCHEMBL35564
7.30IC5050nMCHEMBL35165
7.27IC5054nMCHEMBL306107
7.22IC5060nMCHEMBL36501
7.22IC5060nMCHEMBL418604
7.16IC5070nMCHEMBL195457
7.16IC5070nMCHEMBL32731
7.12IC5075nMCHEMBL32553
7.12IC5075nMCHEMBL286639
7.12IC5075nMCHEMBL75522
7.10IC5080nMCHEMBL76274
7.08IC5084nMCHEMBL72992
7.06IC5088nMCHEMBL73574
7.04IC5091nMCHEMBL74932
7.00IC5099nMCHEMBL193588
7.00IC50100nMCHEMBL35006
7.00IC50100nMCHEMBL35967
7.00IC50100nMCHEMBL418404
7.00IC50100nMCHEMBL33773
6.92IC50120nMCHEMBL34938
6.92IC50120nMCHEMBL309911
6.85IC50140nMCHEMBL193589
6.85IC50140nMCHEMBL35051
6.85IC50140nMCHEMBL422414

PubChem BioAssay actives

110 with measured affinity, of 137 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
prop-2-ynyl N-[4-chloro-3-(5-chloro-1,3-benzothiazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0060uM
6-(3-ethyl-1-benzofuran-2-yl)-2-N-(4-methylphenyl)-1,3,5-triazine-2,4-diamine1917061: Inhibition of LPAAT-beta (unknown origin) expressed in Xenopus laevis oocytes incubated for 3 minsic500.0084uM
6-(5-chloro-2-ethoxyphenyl)-4-N-(4-nitrophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0100uM
prop-2-ynyl N-[4-chloro-3-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0150uM
prop-2-ynyl N-[3-(5-chloro-1,3-benzothiazol-2-yl)-4-methylphenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0150uM
2-N-(4-ethylphenyl)-6-(3-methyl-1-benzofuran-2-yl)-1,3,5-triazine-2,4-diamine1917061: Inhibition of LPAAT-beta (unknown origin) expressed in Xenopus laevis oocytes incubated for 3 minsic500.0150uM
N-[4-chloro-3-(5-chloro-1,3-benzothiazol-2-yl)phenyl]-2-cyanoacetamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0150uM
6-(5-bromo-2-ethoxyphenyl)-4-N-(4-chlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0160uM
6-(5-chloro-2-ethoxyphenyl)-4-N-(4-chlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0170uM
4-[[2-amino-6-(5-bromo-2-ethoxyphenyl)pyrimidin-4-yl]amino]benzonitrile102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0170uM
6-(5-bromo-2-methylphenyl)-4-N-(4-bromophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0180uM
4-N-(4-chlorophenyl)-6-(2,5-dichlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0200uM
6-(5-chloro-2-methylphenyl)-4-N-(4-chlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0220uM
6-(5-chloro-2-ethoxyphenyl)-4-N-(1H-indazol-6-yl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0240uM
N-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-2-cyanoacetamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0270uM
4-N-(4-bromophenyl)-6-(5-chloro-2-methoxyphenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0280uM
2-[4-[[2-amino-6-(5-chloro-2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]ethanol102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0280uM
6-(5-bromo-2-methylphenyl)-4-N-(4-chlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0310uM
4-N-(4-bromophenyl)-6-(5-chloro-2-methylphenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0340uM
1-[4-[[2-amino-6-(5-bromo-2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]ethanone102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0340uM
prop-2-ynyl N-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0350uM
4-(5-chloro-2-methoxyphenyl)-6-N-(4-chlorophenyl)pyridine-2,6-diamine254997: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membraneic500.0400uM
methyl N-[4-chloro-3-(5-chloro-1,3-benzothiazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0400uM
6-(5-chloro-2-methoxyphenyl)-2-N-(4-chlorophenyl)-1,3,5-triazine-2,4-diamine254997: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membraneic500.0450uM
4-[[6-amino-4-(5-chloro-2-ethoxyphenyl)-2-pyridinyl]amino]benzaldehyde254997: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membraneic500.0500uM
4-(5-chloro-2-ethoxyphenyl)-6-N-(4-chlorophenyl)pyridine-2,6-diamine254997: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membraneic500.0500uM
N-[4-chloro-3-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]phenyl]-2-cyanoacetamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0500uM
prop-2-ynyl N-[3-(1,3-benzoxazol-2-yl)-4-chlorophenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0500uM
6-(5-chloro-2-methoxyphenyl)-4-N-(4-chlorophenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0540uM
prop-2-ynyl N-[4-chloro-3-(5-chloro-1-methylbenzimidazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0600uM
2-N-(4-bromophenyl)-6-(5-chloro-2-methylphenyl)-1,3,5-triazine-2,4-diamine102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0600uM
N-[3-(1,3-benzothiazol-2-yl)-4-methylphenyl]-2-cyanoacetamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0700uM
[4-[[2-amino-6-(5-chloro-2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]methanol102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0750uM
but-2-ynyl N-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0750uM
but-3-ynyl N-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.0750uM
6-(5-chloro-2-methoxyphenyl)-4-N-(1H-indazol-6-yl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0800uM
(NZ)-N-[1-[4-[[2-amino-6-(5-bromo-2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]ethylidene]hydroxylamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0840uM
4-[[2-amino-6-(5-bromo-2-ethoxyphenyl)pyrimidin-4-yl]amino]-N-hydroxybenzamide102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0880uM
[4-[[2-amino-6-(5-bromo-2-ethoxyphenyl)pyrimidin-4-yl]amino]phenyl]boronic acid102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.0910uM
[4-[[6-amino-4-(5-chloro-2-ethoxyphenyl)-2-pyridinyl]amino]phenyl]methanol254997: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta enzyme over-expressed in Sf9 insect cell membraneic500.0990uM
1-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]-3-prop-2-ynylurea102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1000uM
prop-2-ynyl N-[3-(5-chloro-1,3-benzoxazol-2-yl)-4-methylphenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1000uM
N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-cyanoacetamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1000uM
N-[4-chloro-3-(5-chloro-1,3-benzoxazol-2-yl)phenyl]pent-4-ynamide102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1000uM
prop-2-ynyl N-[4-chloro-3-[1-methyl-5-(trifluoromethyl)benzimidazol-2-yl]phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1200uM
6-(5-bromo-2-ethoxyphenyl)-4-N-phenylpyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.1200uM
6-(5-chloro-2-methylphenyl)-4-N-[4-(trifluoromethyl)phenyl]pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.1400uM
6-(5-chloro-2-ethoxyphenyl)-2-N-(4-chlorophenyl)-1,3,5-triazine-2,4-diamine1917048: Inhibition of human LPAAT-beta by cell-free colorimetric assayic500.1400uM
prop-2-ynyl N-[4-chloro-3-[5-(trifluoromethyl)-1,3-benzoxazol-2-yl]phenyl]carbamate102975: Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranesic500.1400uM
4-N-(4-chlorophenyl)-6-(5-fluoro-2-methylphenyl)pyrimidine-2,4-diamine102974: Inhibitory activity against Lysophosphatidic acid acyltransferase-beta expressed in Sf9 insect cell membranesic500.1500uM

CTD chemical–gene interactions

62 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyrenedecreases expression, affects methylation4
Tetrachlorodibenzodioxinaffects expression, increases expression3
entinostatincreases expression, affects cotreatment2
Acetaminophendecreases expression2
Valproic Acidaffects cotreatment, decreases expression, affects expression2
Cyclosporinedecreases expression, increases expression2
Aflatoxin B1affects expression, increases methylation2
Cadmium Chlorideincreases abundance, increases expression2
Oleic Acidaffects cotreatment, increases expression, affects expression2
methyleugenoldecreases expression1
triphenyl phosphateaffects expression1
bisphenol Aincreases expression1
O,O-diethyl O-3,5,6-trichloro-2-pyridyl phosphateaffects expression, affects reaction, increases expression1
tris(2-butoxyethyl) phosphateaffects expression1
sodium arseniteincreases expression1
anandamideaffects expression, affects reaction1
GW 4064increases expression1
GW 7647affects cotreatment, increases expression1
2-chloro-5-nitrobenzanilideaffects expression, affects cotreatment1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, increases expression1
obeticholic aciddecreases expression1
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oximeaffects cotreatment, increases expression1
oleoylethanolamideaffects expression, affects reaction1
bisphenol Bincreases expression1
abrinedecreases expression1
dorsomorphinaffects cotreatment, increases expression1
(+)-JQ1 compounddecreases expression1
MT19c compounddecreases expression1
bisphenol AFincreases expression1
Capecitabineincreases response to substance1

ChEMBL screening assays

6 unique, capped per target: 6 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL5216570BindingInhibition of human LPAAT-beta by cell-free colorimetric assayA closer look at N2,6-substituted 1,3,5-triazine-2,4-diamines: Advances in synthesis and biological activities. — Eur J Med Chem

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00029224PHASE4COMPLETEDTreatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997PHASE4COMPLETEDOpen-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609PHASE4COMPLETEDThe Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623PHASE4SUSPENDEDThe Plenaxis® Experience Study
NCT00106392PHASE4COMPLETEDA Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029PHASE4UNKNOWNMR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485PHASE4COMPLETEDAngelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219PHASE4COMPLETEDZoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271PHASE4COMPLETEDEffect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146PHASE4COMPLETEDStudy to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554PHASE4COMPLETEDOpen-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098PHASE4COMPLETEDDocetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696PHASE4COMPLETEDCasodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139PHASE4COMPLETEDEffect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765PHASE4COMPLETEDEffects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690PHASE4COMPLETEDEvaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708PHASE4COMPLETEDLocal Anesthesia for Prostate Biopsy
NCT00526331PHASE4COMPLETEDEvaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213PHASE4COMPLETEDCompare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330PHASE4TERMINATEDDissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966PHASE4COMPLETEDRadical Prostatectomy and Perioperative Fluid Therapy
NCT00805701PHASE4COMPLETEDStudy Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027PHASE4COMPLETEDEffect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269PHASE4UNKNOWNCan Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277PHASE4COMPLETEDStudy of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800PHASE4COMPLETEDDoes Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199PHASE4COMPLETEDGlobal Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226PHASE4COMPLETEDEvaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563PHASE4COMPLETEDRandomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905PHASE4COMPLETEDStudy to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672PHASE4COMPLETED3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143PHASE4TERMINATEDProspective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742PHASE4UNKNOWNComparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563PHASE4COMPLETEDHydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874PHASE4COMPLETEDEfficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472PHASE4TERMINATEDFirmagon (Degarelix) Intermittent Therapy
NCT01547416PHASE4COMPLETEDThe Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544PHASE4COMPLETEDThe Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749PHASE4UNKNOWNEvaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635PHASE4COMPLETEDStudy of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer

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
v1.1.2
BioBTree
v2.0.2

Sources 78

This page pulls from 78 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot