FABP1

gene
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Also known as L-FABP

Summary

FABP1 (fatty acid binding protein 1, HGNC:3555) is a protein-coding gene on chromosome 2p11.2, encoding Fatty acid-binding protein, liver (P07148). Plays a role in lipoprotein-mediated cholesterol uptake in hepatocytes.

This gene encodes the fatty acid binding protein found in liver. Fatty acid binding proteins are a family of small, highly conserved, cytoplasmic proteins that bind long-chain fatty acids and other hydrophobic ligands. This protein and FABP6 (the ileal fatty acid binding protein) are also able to bind bile acids. It is thought that FABPs roles include fatty acid uptake, transport, and metabolism.

Source: NCBI Gene 2168 — RefSeq curated summary.

At a glance

  • GWAS associations: 7
  • Clinical variants (ClinVar): 21 total
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_001443

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:3555
Approved symbolFABP1
Namefatty acid binding protein 1
Location2p11.2
Locus typegene with protein product
StatusApproved
AliasesL-FABP
Ensembl geneENSG00000163586
Ensembl biotypeprotein_coding
OMIM134650
Entrez2168

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 8 protein_coding, 1 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000295834, ENST00000393750, ENST00000472846, ENST00000495375, ENST00000877228, ENST00000877229, ENST00000877230, ENST00000877231, ENST00000945195, ENST00000945196

RefSeq mRNA: 1 — MANE Select: NM_001443 NM_001443

CCDS: CCDS2001

Canonical transcript exons

ENST00000295834 — 4 exons

ExonStartEnd
ENSE000010762788812298288123104
ENSE000010762808812449488124586
ENSE000018768508812795188128062
ENSE000035143978812617688126348

Expression profiles

Bgee: expression breadth ubiquitous, 168 present calls, max score 99.99.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 32.1513 / max 7588.9007, expressed in 157 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter IDTPM avgSamples expressed
2959332.1513157

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
mucosa of transverse colonUBERON:000499199.99gold quality
colonic mucosaUBERON:000031799.97gold quality
jejunal mucosaUBERON:000039999.97gold quality
mucosa of sigmoid colonUBERON:000499399.96gold quality
ileal mucosaUBERON:000033199.95gold quality
rectumUBERON:000105299.94gold quality
right lobe of liverUBERON:000111499.91gold quality
liverUBERON:000210799.73gold quality
caecumUBERON:000115397.85gold quality
adult mammalian kidneyUBERON:000008297.82gold quality
vermiform appendixUBERON:000115497.60gold quality
small intestine Peyer’s patchUBERON:000345497.59gold quality
small intestineUBERON:000210896.91gold quality
transverse colonUBERON:000115796.64gold quality
duodenumUBERON:000211496.25gold quality
adult organismUBERON:000702394.15gold quality
intestineUBERON:000016092.97gold quality
large intestineUBERON:000005991.64gold quality
colonUBERON:000115591.26gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099190.65gold quality
kidneyUBERON:000211388.71gold quality
kidney epitheliumUBERON:000481987.43gold quality
nephron tubuleUBERON:000123187.36gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047387.35gold quality
colonic epitheliumUBERON:000039786.54gold quality
renal glomerulusUBERON:000007483.95gold quality
sigmoid colonUBERON:000115983.30gold quality
metanephric glomerulusUBERON:000473683.17gold quality
jejunumUBERON:000211582.36gold quality
cortex of kidneyUBERON:000122579.95gold quality

Single-cell (SCXA)

Detected in 11 experiment(s), a significant marker in 11.

ExperimentMarker?Max mean expression
E-GEOD-125970yes22574.10
E-MTAB-8410yes21299.01
E-MTAB-7407yes13504.53
E-CURD-46yes8972.04
E-MTAB-10553yes8892.58
E-CURD-122yes6737.35
E-CURD-88yes6219.04
E-HCAD-9yes5206.67
E-MTAB-9906yes3188.21
E-ANND-5yes805.58
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, FOXA1, GATA4, GATA5, GATA6, HNF1A, HNF4A, PDX1, PPARA, PPARG, PPARGC1B, RXRA, TFAP2A

Literature-anchored findings (GeneRIF, showing 40)

  • evidence that FABP is a target for tamoxifen and that target proteins are implicated in cell lipid metabolism (PMID:12121132)
  • besides I-FABP, also L-FABP is a useful plasma marker for the detection of intestinal injury, especially in patients undergoing intestinal surgery (PMID:14563446)
  • L-FABP has a significant role in oxidative stress (PMID:16175609)
  • Urinary L-FABP levels appear to be associated with the progression of diabetic nephropathy, and NK 104 may be effective in ameliorating tubulointerstitial damage in early diabetic nephropathy. (PMID:16249547)
  • EPO supplementation may ameliorate renal tubular damage, in part, due to a reduction of oxidative stress in CRF patients with anemia. (PMID:16772708)
  • Renal L-FABP may reduce the oxidative stress in the unilateral ureteral obstruction model, ameliorating tubulointerstitial damage. (PMID:17003471)
  • L-FABP may play a key role in the progress of invasiveness and metastasis in human breast cancer. (PMID:17428383)
  • there is a functional relevance of the FABP1 T94A SNP in hepatic fatty acid and lipid metabolism in humans (PMID:17485234)
  • These results have demonstrated that C. trachomatis can productively infect liver cells and utilize FABP-transported long-chain fatty acids for its own biosynthesis. (PMID:17526850)
  • Intestinal L-FABP expression was investigated by immuno-histochemistry, western blot, ELISA and Northern blot analysis (PMID:17605029)
  • The Ala/Ala(94)-mutation contributed significantly to reduced glycogenolysis and less severe hyperglycemia in lipid-exposed humans and was further associated with reduced body weight in a large cohort. (PMID:17698986)
  • Hypoxia enhances the expression of FABP1 in term human trophoblasts, suggesting that fatty acid binding proteins support fat accumulation in the hypoxic placenta. (PMID:17826730)
  • Urinary L-FABP levels represent a sensitive and predictive early biomarker of acute kidney injury after cardiac surgery. (PMID:18094680)
  • Data show that genotypes for the A–>G (Thr94Ala) polymorphism (rs2241883) of FABP1 was associated (P<0.05) with the prevalence of atherothrombotic cerebral infarction. (PMID:18506375)
  • The results suggest that urinary L-FABP levels are significantly increased in patients with septic shock and that PMX-F treatment is effective in reducing these levels. (PMID:18838948)
  • Urinary fatty acid-binding protein 1: an early predictive biomarker of kidney injury. (Review) (PMID:19019918)
  • study demonstrated the direct, albeit weak, interaction between MES buffer (2-(N-morpholino)ethanesulfonic acid) & liver fatty acid binding protein; finding of buffer-induced changes in protein dynamics offers a clue to how hLFABP accommodates its ligands (PMID:19217864)
  • paradoxically underexpressed in nonalcoholic steatohepatitis (PMID:19330863)
  • renal expression and urinary excretion of hL-FABP significantly reflected the severity of tubulointerstitial damage in FA-induced nephropathy (PMID:19435794)
  • Studies indicate that the members of the FABP family present in mammals that appear to be more closely related to the L-BABPs are the liver FABPs and the ileal BABPs. (PMID:19441025)
  • two FABPs display differences in localization, regulation and developmental pattern. (PMID:19499240)
  • While B-FABP is over expressed in renal cell carcinoma in comparison to normal renal tissues L-FABP appears to be reduced in tumor tissue (PMID:19622156)
  • High levels of the tubular inflammation marker u-LFABP predict the initiation and progression to diabetic nephropathy and all-cause mortality, independent of urinary albumin excretion rate and other established risk factors. (PMID:20185732)
  • the slow dynamics of human liver fatty acid binding protein (hLFABP) that was shown previously to be highly flexible on millisecond timescales was quantitatively characterized in detail (PMID:20550918)
  • The serum level of I-FABP can be used for assessing the gut dysfunction and disease severity of acute pancreatitis. (PMID:20575163)
  • the T94A mutant of L-FABP lowered free fatty acid uptake but had no effect on FFA efflux (PMID:20721681)
  • Our study suggests that L-FABP is a useful biomarker for early detection of acute kidney injury. (PMID:21153750)
  • Renal hL-FABP reduced the oxidative stress in aristolochic acid-induced nephrotoxicity and attenuated tubulointerstitial damage. (PMID:21356355)
  • Review: summarizes the findings on the pathophysiological roles and dynamics of renal human L-FABP in the recent experimental studies performed in a transgenic mouse model. (PMID:21504508)
  • liver fatty acid-binding protein (LFABP) in apo, holo, and intermediate states of palmitic acid engagement;Apo-LFABP undergoes structural remodeling, where the first palmitate ingress creates the atomic environment for placement of the second palmitate. (PMID:21757748)
  • Data show that IL-FABP mRNA was over-expressed in renal tumour tissue. (PMID:21767383)
  • FABP1 gene is highly transcribed in liver-derived cells, and regulated predominantly by liver-enriched transcription factors HNF3B and CEBPA. (PMID:21856370)
  • in kidney allograft recipients, L-FABP may be a potential early marker for impaired kidney function/injury (PMID:21996226)
  • Common variants of the liver fatty acid binding protein genes 1-4 influence the risk of type 2 diabetes and insulin resistance in Spanish population (PMID:22396741)
  • The present study suggests that genetic variations within FABP1 influence susceptibility to non-alcohol fatty liver disease. (PMID:22465531)
  • Studies indicate the most studied biomarkers for acute kidney injury are neutrophil gelatinase-associated lipocalin-2, kidney injury molecule-1, IL-18, cystatin C, N-acetyl-beta-D-glucosaminidase, liver fatty-acid binding protein, and heat shock protein 72. (PMID:22515481)
  • Baicalin was able to enhance both L-FABP expression and activity of intracellular SOD and GSH, and therefore protected hepatocytes from oxidative stress. (PMID:22525507)
  • PDX1 repression of FABP1, LCT, and SI suggests a role for PDX1 in patterning anterior intestinal development. (PMID:22640736)
  • Serum FABP1 correlates positively with obesity and insulin resistance in Chinese young adults. (PMID:23144966)
  • Urinary L-FABP and NGAL increased at an early stage after cardiac surgery. The combination of the two biomarkers enhanced the accuracy of the early detection of postoperative acute kidney injury after cardiac surgery before a rise in serum creatinine. (PMID:23167703)

Cross-species orthologs

7 orthologs

OrganismSymbolGene ID
danio_reriofabp1aENSDARG00000019357
danio_reriofabp1b.1ENSDARG00000059227
danio_reriofabp1b.2ENSDARG00000103398
mus_musculusFabp1ENSMUSG00000054422
rattus_norvegicusFabp1ENSRNOG00000006675
caenorhabditis_elegansWBGENE00002259
caenorhabditis_elegansWBGENE00002260

Paralogs (15): RBP2 (ENSG00000114113), RBP1 (ENSG00000114115), FABP3 (ENSG00000121769), RBP5 (ENSG00000139194), CRABP2 (ENSG00000143320), FABP2 (ENSG00000145384), PMP2 (ENSG00000147588), RBP7 (ENSG00000162444), FABP7 (ENSG00000164434), FABP5 (ENSG00000164687), CRABP1 (ENSG00000166426), FABP6 (ENSG00000170231), FABP4 (ENSG00000170323), FABP12 (ENSG00000197416), FABP9 (ENSG00000205186)

Protein

Protein identifiers

Fatty acid-binding protein, liverP07148 (reviewed: P07148)

Alternative names: Fatty acid-binding protein 1, Liver-type fatty acid-binding protein

All UniProt accessions (3): P07148, A8MW49, Q6FGL7

UniProt curated annotations — full annotation on UniProt →

Function. Plays a role in lipoprotein-mediated cholesterol uptake in hepatocytes. Binds cholesterol. Binds free fatty acids and their coenzyme A derivatives, bilirubin, and some other small molecules in the cytoplasm. May be involved in intracellular lipid transport.

Subcellular location. Cytoplasm.

Domain organisation. Forms a beta-barrel structure that accommodates hydrophobic ligands in its interior.

Similarity. Belongs to the calycin superfamily. Fatty-acid binding protein (FABP) family.

RefSeq proteins (1): NP_001434* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000463Fatty_acid-bdDomain
IPR012674CalycinHomologous_superfamily
IPR031259ILBPFamily

Pfam: PF14651

UniProt features (30 total): modified residue 13, strand 12, sequence variant 2, helix 2, chain 1

Structure

Experimental structures (PDB)

37 structures, top 30 by resolution.

PDBMethodResolution (Å)
7FXOX-RAY DIFFRACTION1.3
3VG7X-RAY DIFFRACTION1.44
7DZKX-RAY DIFFRACTION1.54
3B2HX-RAY DIFFRACTION1.55
3STKX-RAY DIFFRACTION1.55
7DZEX-RAY DIFFRACTION1.55
7DZGX-RAY DIFFRACTION1.6
7DZJX-RAY DIFFRACTION1.63
7DZLX-RAY DIFFRACTION1.64
7G0WX-RAY DIFFRACTION1.64
7DZHX-RAY DIFFRACTION1.65
7DZIX-RAY DIFFRACTION1.65
7G1XX-RAY DIFFRACTION1.65
7DZFX-RAY DIFFRACTION1.7
3B2KX-RAY DIFFRACTION1.73
3B2IX-RAY DIFFRACTION1.86
7FYAX-RAY DIFFRACTION1.88
3B2JX-RAY DIFFRACTION2
3VG5X-RAY DIFFRACTION2
3STMX-RAY DIFFRACTION2.22
3VG3X-RAY DIFFRACTION2.22
3VG6X-RAY DIFFRACTION2.22
7FY8X-RAY DIFFRACTION2.23
3B2LX-RAY DIFFRACTION2.25
3VG2X-RAY DIFFRACTION2.4
2F73X-RAY DIFFRACTION2.5
3VG4X-RAY DIFFRACTION2.5
6MP4X-RAY DIFFRACTION2.5
3STNX-RAY DIFFRACTION2.6
7G00X-RAY DIFFRACTION2.6

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P07148-F195.250.90

Functional residue map

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

Post-translational modifications (13): 1, 78, 90, 100, 121, 11, 31, 36, 39, 46, 51, 56, 57

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

IDPathway
R-HSA-163560Triglyceride catabolism
R-HSA-189483Heme degradation
R-HSA-1989781PPARA activates gene expression
R-HSA-400206Regulation of lipid metabolism by PPARalpha
R-HSA-9707564Cytoprotection by HMOX1

MSigDB gene sets: 333 (showing top): REACTOME_TRIGLYCERIDE_CATABOLISM, GOBP_LIPID_MODIFICATION, GOBP_ACYLGLYCEROL_HOMEOSTASIS, GOBP_DIGESTION, MODULE_92, SHEPARD_BMYB_MORPHOLINO_UP, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_HEPATICOBILIARY_SYSTEM_DEVELOPMENT, GOBP_FATTY_ACID_CATABOLIC_PROCESS, GOBP_CARBOHYDRATE_TRANSPORT, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_NUCLEOSIDE_DIPHOSPHATE_METABOLIC_PROCESS, GOBP_MUSCLE_TISSUE_DEVELOPMENT, GOBP_ACID_SECRETION, GOBP_BEHAVIOR

GO Biological Process (5): fatty acid transport (GO:0015908), cellular response to hydrogen peroxide (GO:0070301), cellular response to hypoxia (GO:0071456), cellular detoxification (GO:1990748), cellular oxidant detoxification (GO:0098869)

GO Molecular Function (5): chromatin binding (GO:0003682), fatty acid binding (GO:0005504), antioxidant activity (GO:0016209), protein binding (GO:0005515), lipid binding (GO:0008289)

GO Cellular Component (6): nucleus (GO:0005634), nucleoplasm (GO:0005654), peroxisomal matrix (GO:0005782), cytosol (GO:0005829), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-5 pathways:

CategoryPathways
Triglyceride metabolism1
Metabolism of porphyrins1
Regulation of lipid metabolism by PPARalpha1
Metabolism of lipids1
Cellular response to chemical stress1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
binding3
cellular anatomical structure3
lipid transport1
monocarboxylic acid transport1
cellular response to reactive oxygen species1
response to hydrogen peroxide1
response to hypoxia1
cellular response to stress1
cellular response to decreased oxygen levels1
cellular process1
cellular response to toxic substance1
detoxification1
cellular detoxification1
lipid binding1
monocarboxylic acid binding1
molecular_function1
cellular oxidant detoxification1
intracellular membrane-bounded organelle1
nuclear lumen1
peroxisome1
microbody lumen1
cytoplasm1
extracellular vesicle1
intracellular anatomical structure1

Protein interactions and networks

STRING

1657 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
FABP1GOT2P00505957
FABP1FABP2P12104950
FABP1FABP3P05413927
FABP1PPARAQ07869913
FABP1CD36P16671881
FABP1SCARB1Q8WTV0873
FABP1HAVCR1Q96D42872
FABP1SCARB2Q14108863
FABP1FABP4P15090816
FABP1LCN2P30150814
FABP1CST3P01034771
FABP1APOBP04114734
FABP1CPT1AP50416677
FABP1OGAO60502667
FABP1IGFBP7Q16270644

IntAct

15 interactions, top by confidence:

ABTypeScore
FABP1FLNApsi-mi:“MI:0915”(physical association)0.560
FLNAFABP1psi-mi:“MI:0915”(physical association)0.560
EPHA4FABP1psi-mi:“MI:0915”(physical association)0.560
FABP1GNPNAT1psi-mi:“MI:0915”(physical association)0.560
EPHA4FABP1psi-mi:“MI:0914”(association)0.560
NME4NRDCpsi-mi:“MI:0914”(association)0.350
ADCK5AKR1B10psi-mi:“MI:0914”(association)0.350
FABP1NME2P1psi-mi:“MI:0914”(association)0.350
SHTN1psi-mi:“MI:0914”(association)0.350
FABP1GRB2psi-mi:“MI:0915”(physical association)0.000

BioGRID (19): FLNA (Two-hybrid), FLNA (Two-hybrid), FABP1 (Affinity Capture-MS), GNPNAT1 (Affinity Capture-MS), FABP1 (Two-hybrid), FABP1 (Two-hybrid), NME2P1 (Affinity Capture-MS), GNPNAT1 (Affinity Capture-MS), FABP1 (Affinity Capture-MS), FABP1 (Affinity Capture-MS), FABP1 (Affinity Capture-MS), FABP1 (Affinity Capture-MS), FABP1 (Affinity Capture-MS), DERL1 (Affinity Capture-Western), FABP1 (Affinity Capture-Western)

ESM2 similar proteins: A6NFH5, O01812, O02323, O42494, O45035, P02692, P02693, P07148, P0C241, P0DM59, P10289, P12104, P12710, P29498, P31416, P31417, P41496, P41509, P49924, P50119, P51161, P51162, P55050, P80020, P80226, P80425, P80856, P81399, P81400, P81653, P82289, P83409, Q02970, Q0Z7S8, Q17284, Q1AMT3, Q3T0Z2, Q45KW7, Q4VBT1, Q56JX9

Diamond homologs: A0A0K0MJ13, A0A0K0MJN3, A6NFH5, A6YLM6, A8MUU1, B7SUM8, C4N147, O01812, O01814, O02323, O02324, O02772, O08716, O13008, O15540, O42386, O45035, O76821, O97788, P02689, P02690, P02691, P02694, P02696, P04117, P05413, P06768, P07148, P07483, P09455, P0C6G6, P10790, P11404, P12710, P15090, P22935, P24526, P29373, P29498, P29762

SIGNOR signaling

1 interactions.

AEffectBMechanism
FABP1“up-regulates quantity”“Fatty acid”relocalization

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance18
Likely benign2
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

426 predictions. Top by Δscore:

VariantEffectΔscore
2:88124492:A:ACdonor_gain1.0000
2:88124493:C:CCdonor_gain1.0000
2:88124493:CA:Cdonor_gain1.0000
2:88124583:CTGT:Cacceptor_gain1.0000
2:88124585:GTC:Gacceptor_loss1.0000
2:88124586:TC:Tacceptor_loss1.0000
2:88124587:C:CAacceptor_loss1.0000
2:88124587:C:CCacceptor_gain1.0000
2:88124588:T:Aacceptor_loss1.0000
2:88126246:TTGG:Tdonor_gain1.0000
2:88127949:A:ACdonor_gain1.0000
2:88127950:C:CCdonor_gain1.0000
2:88124493:CATT:Cdonor_gain0.9900
2:88124493:CATTG:Cdonor_gain0.9900
2:88124584:TGT:Tacceptor_gain0.9900
2:88124585:GT:Gacceptor_gain0.9900
2:88127946:CT:Cdonor_loss0.9900
2:88127947:TCA:Tdonor_loss0.9900
2:88127948:CACC:Cdonor_loss0.9900
2:88127950:C:Adonor_loss0.9900
2:88124488:ACT:Adonor_loss0.9800
2:88124489:CT:Cdonor_loss0.9800
2:88124490:T:TCdonor_loss0.9800
2:88124491:TAC:Tdonor_loss0.9800
2:88124492:ACATT:Adonor_loss0.9800
2:88124493:CAT:Cdonor_gain0.9800
2:88126173:TACC:Tdonor_loss0.9800
2:88126175:C:CTdonor_loss0.9800
2:88126240:A:ACdonor_gain0.9800
2:88123150:T:TCacceptor_gain0.9700

AlphaMissense

854 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
2:88127999:A:CY7D0.988
2:88127998:T:GY7S0.985
2:88123066:G:CS124R0.971
2:88123066:G:TS124R0.971
2:88123068:T:GS124R0.971
2:88124555:A:GL91P0.971
2:88126227:G:CF63L0.967
2:88126227:G:TF63L0.967
2:88126229:A:GF63L0.967
2:88126228:A:GF63S0.966
2:88127999:A:TY7N0.965
2:88124579:A:TV83D0.964
2:88127964:G:CF18L0.964
2:88127964:G:TF18L0.964
2:88127966:A:GF18L0.964
2:88128004:C:TG5D0.961
2:88124529:A:GS100P0.960
2:88127999:A:GY7H0.957
2:88123060:T:AR126S0.953
2:88123060:T:GR126S0.953
2:88126273:A:GF48S0.949
2:88127965:A:GF18S0.949
2:88128004:C:AG5V0.943
2:88127998:T:CY7C0.940
2:88128009:G:CF3L0.940
2:88128009:G:TF3L0.940
2:88128011:A:GF3L0.940
2:88128010:A:GF3S0.938
2:88124555:A:CL91R0.933
2:88127957:C:GA21P0.932

dbSNP variants (sampled 300 via entrez): RS1000074723 (2:88124280 T>C,G), RS1000878160 (2:88126006 C>T), RS1001112664 (2:88128486 T>C), RS1001263833 (2:88125177 C>A), RS1002422621 (2:88125572 G>A), RS1002776849 (2:88126154 A>T), RS1003372885 (2:88127398 T>C), RS1003881703 (2:88123854 A>T), RS1004781618 (2:88128291 T>C), RS1004896092 (2:88128030 G>A,C), RS1005720647 (2:88123474 A>G), RS1005829798 (2:88129644 A>C), RS1005901551 (2:88129359 A>G), RS1006018861 (2:88123787 C>T), RS1007038459 (2:88127430 A>G)

Disease associations

OMIM: gene MIM:134650 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

7 associations (top):

StudyTraitp-value
GCST003542_178Night sleep phenotypes3.000000e-08
GCST006585_585Blood protein levels5.000000e-21
GCST007614_37C-reactive protein levels5.000000e-10
GCST008469_17Liver fibrosis in non-alcoholic fatty liver disease8.000000e-08
GCST90011898_98Alanine aminotransferase levels4.000000e-09
GCST90011900_4Serum alkaline phosphatase levels3.000000e-17
GCST90013406_280Liver enzyme levels (alkaline phosphatase)1.000000e-26

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0004458C-reactive protein measurement
EFO:0004533alkaline phosphatase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5421 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 749,198 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL95TACRINE435,360
CHEMBL8659OLEIC ACID2713,838

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

PharmGKB clinical annotations

1 annotations.

VariantTypeLevelDrugsPhenotypes
rs2241883Efficacy4fenofibrateHypertriglyceridemia

PharmGKB variants

1 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs2241883FABP14-1.501fenofibrate

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Fatty acid-binding proteins

Most potent curated ligand interactions (3 total), top 3:

LigandActionAffinityParameter
fenofibrateInhibition7.62pKi
fenofibric acidInhibition6.48pKi
HTS01037Inhibition5.09pKi

Binding affinities (BindingDB)

1 measured of 2 human assays (3 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
3,7,11,15-tetramethylhexadecanoic acidKI38 nM

ChEMBL bioactivities

31 potent at pChembl≥5 of 40 total, top 30 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.70Kd200nMOLEIC ACID
6.05Kd900nMOLEIC ACID
5.93IC501180nMCHEMBL5612524
5.85IC501400nMCHEMBL5394417
5.82IC501500nMCHEMBL5396259
5.74IC501820nMCHEMBL5612235
5.70Kd2000nMCHEMBL471741
5.68IC502110nMCHEMBL5613265
5.61IC502440nMCHEMBL5612678
5.58IC502660nMCHEMBL5614355
5.57IC502700nMCHEMBL5396467
5.57IC502710nMCHEMBL247920
5.54IC502900nMCHEMBL5420532
5.52IC503020nMCHEMBL5613315
5.49IC503240nMCHEMBL5613794
5.48IC503300nMCHEMBL5429880
5.44IC503600nMCHEMBL5420842
5.42IC503800nMCHEMBL5419154
5.40IC504000nMCHEMBL247920
5.38IC504200nMCHEMBL5420029
5.37IC504300nMCHEMBL5436041
5.35IC504460nMCHEMBL5556772
5.25IC505660nMCHEMBL5612128
5.24IC505700nMCHEMBL5439051
5.21IC506110nMCHEMBL5611914
5.14IC507280nMCHEMBL5517962
5.09Ki8170nMCHEMBL1077990
5.07IC508500nMCHEMBL6151098
5.06IC508710nMCHEMBL5558673
5.06IC508630nMCHEMBL5559644

PubChem BioAssay actives

35 with measured affinity, of 314 total; 30 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
Fenofibrate1800412: ANS Fluorescence Displacement Assay from Article 10.1021/bi401014k: “The human liver fatty acid binding protein T94A variant alters the structure, stability, and interaction with fibrates.”ki0.0150uM
3,7,11,15-tetramethylhexadecanoic acid1800412: ANS Fluorescence Displacement Assay from Article 10.1021/bi401014k: “The human liver fatty acid binding protein T94A variant alters the structure, stability, and interaction with fibrates.”ki0.0350uM
(Z)-octadec-9-enoic acid407370: Binding affinity to L-FABP high binding affinity site by titration calorimetry methodkd0.2000uM
Fenofibric Acid1800412: ANS Fluorescence Displacement Assay from Article 10.1021/bi401014k: “The human liver fatty acid binding protein T94A variant alters the structure, stability, and interaction with fibrates.”ki0.2500uM
3-[2-(4-quinolin-8-ylsulfonylpiperazin-1-yl)sulfonylphenyl]phenol2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic501.1800uM
3-[4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]propanoic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic501.4000uM
2-[3-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]-2-methylpropanoic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic501.5000uM
4-[2-(4-quinolin-8-ylsulfonylpiperazin-1-yl)sulfonylphenyl]phenol2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic501.8200uM
(8-anilinonaphthalen-1-yl) hydrogen sulfate407367: Binding affinity to human L-FABPkd2.0000uM
4-[2-(4-quinolin-8-ylsulfonylpiperazin-1-yl)sulfonylphenyl]benzoic acid2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic502.1100uM
8-[4-(quinolin-8-ylsulfonylamino)phenoxy]octanoic acid2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic502.4400uM
4-[2-(4-quinolin-8-ylsulfonylpiperazin-1-yl)sulfonylphenyl]benzonitrile2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic502.6600uM
1-[3-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]cyclopropane-1-carboxylic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic502.7000uM
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic502.7100uM
2-[4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]acetic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic502.9000uM
8-[3-(quinolin-8-ylsulfonylamino)phenoxy]octanoic acid2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic503.0200uM
8-[3-[(4-phenylphenyl)sulfonylamino]phenoxy]octanoic acid2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic503.2400uM
3-[3-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]propanoic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic503.3000uM
2-[4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenoxy]propanoic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic503.6000uM
2-[3-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenoxy]acetic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic503.8000uM
2-[4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenoxy]acetic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic504.2000uM
2-[4-[2-chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenyl]acetic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic504.3000uM
3-[3-(cyclopropylmethoxy)phenyl]-5-[(3-phenoxybenzoyl)amino]benzoic acid2075680: Inhibition of recombinant human FABP1 incubated for 3 mins by fluorescence based analysisic504.4600uM
8-[4-[2-(4-fluorophenyl)phenyl]sulfonylpiperazin-1-yl]sulfonylquinoline2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic505.6600uM
2-[4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]phenoxy]-2-methylpropanoic acid1987909: Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assayic505.7000uM
8-[4-[2-(4-fluoro-2-methylphenyl)phenyl]sulfonylpiperazin-1-yl]sulfonylquinoline2126076: Inhibition of human FABP1 incubated for 3 mins by fluorescence based analysisic506.1100uM
3-(4-tert-butylphenyl)-5-[(3-phenoxybenzoyl)amino]benzoic acid2075680: Inhibition of recombinant human FABP1 incubated for 3 mins by fluorescence based analysisic507.2800uM
(E)-4-[(2-methoxycarbonyl-5-thiophen-2-ylthiophen-3-yl)amino]-4-oxobut-2-enoic acid468322: Displacement of radiolabeled 1-anilinonaphthalene 8-sulfonic acid from LFABP expressed in Escherichia coli BL21 (DE3) by fluorescence spectrophotometryki8.1700uM
3-[(3-phenoxybenzoyl)amino]-5-(3-propoxyphenyl)benzoic acid2075680: Inhibition of recombinant human FABP1 incubated for 3 mins by fluorescence based analysisic508.6300uM
3-(3-ethoxyphenyl)-5-[(3-phenoxybenzoyl)amino]benzoic acid2075680: Inhibition of recombinant human FABP1 incubated for 3 mins by fluorescence based analysisic508.7100uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Benzo(a)pyrenedecreases expression, increases mutagenesis, affects methylation, affects cotreatment, affects expression7
perfluorooctanoic aciddecreases expression, affects cotreatment, increases expression, affects expression5
Aflatoxin B1affects expression, decreases expression, decreases methylation4
Oleic Acidaffects expression, affects cotreatment, increases expression, decreases expression, decreases reaction (+1 more)4
pirinixic acidaffects binding, increases activity, increases expression3
perfluorooctane sulfonic acidaffects cotreatment, increases expression, affects expression, decreases expression3
Acetaminophenaffects cotreatment, decreases expression, increases expression3
Amitriptylineincreases expression3
Ketoconazoleincreases expression3
Tetrachlorodibenzodioxinaffects expression, decreases expression, increases expression3
Valproic Aciddecreases expression3
Cyclosporinedecreases expression, increases expression3
lasiocarpinedecreases expression2
benzo(b)fluoranthenedecreases expression, affects expression, affects cotreatment2
sodium arsenitedecreases methylation, decreases reaction, decreases expression, increases expression2
sulindac sulfidedecreases reaction, increases expression, affects reaction2
perfluorobutyric acidaffects expression, increases expression2
perfluoro-n-nonanoic acidaffects cotreatment, affects expression, increases expression2
GW 7647affects cotreatment, increases expression2
perfluorohexanesulfonic acidincreases expression, affects cotreatment, affects expression2
perfluorododecanoic aciddecreases expression2
Amiodaroneincreases expression2
trans-1,4-Bis(2-chlorobenzaminomethyl)cyclohexane Dihydrochlorideincreases expression2
Bezafibrateaffects cotreatment, affects localization, increases expression, decreases expression, decreases reaction2
Chlorpromazineincreases expression2
Clozapineincreases expression2
Flecainideincreases expression2
Fluoxetineincreases expression2
Imipramineincreases expression2
Perhexilineincreases expression2

ChEMBL screening assays

17 unique, capped per target: 17 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1102423BindingDisplacement of radiolabeled 1-anilinonaphthalene 8-sulfonic acid from LFABP expressed in Escherichia coli BL21 (DE3) by fluorescence spectrophotometryIdentification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. — J Med Chem

Clinical trials (associated diseases)

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