Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTR34ETM)

DOT Name Fatty acid-binding protein, liver (FABP1)
Synonyms Fatty acid-binding protein 1; Liver-type fatty acid-binding protein; L-FABP
Gene Name FABP1
UniProt ID
FABPL_HUMAN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
PDB ID
2F73 ; 2L67 ; 2L68 ; 2LKK ; 2PY1 ; 3B2H ; 3B2I ; 3B2J ; 3B2K ; 3B2L ; 3STK ; 3STM ; 3STN ; 3VG2 ; 3VG3 ; 3VG4 ; 3VG5 ; 3VG6 ; 3VG7 ; 6DO6 ; 6DO7 ; 6DRG ; 6MP4 ; 7DZE ; 7DZF ; 7DZG ; 7DZH ; 7DZI ; 7DZJ ; 7DZK ; 7DZL ; 7FXO ; 7FY8 ; 7FYA ; 7G00 ; 7G0W ; 7G1X
Pfam ID
PF14651
Sequence
MSFSGKYQLQSQENFEAFMKAIGLPEELIQKGKDIKGVSEIVQNGKHFKFTITAGSKVIQ
NEFTVGEECELETMTGEKVKTVVQLEGDNKLVTTFKNIKSVTELNGDIITNTMTLGDIVF
KRISKRI
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.
KEGG Pathway
PPAR sig.ling pathway (hsa03320 )
Alcoholic liver disease (hsa04936 )
Fat digestion and absorption (hsa04975 )
Reactome Pathway
Heme degradation (R-HSA-189483 )
PPARA activates gene expression (R-HSA-1989781 )
Regulation of lipid metabolism by PPARalpha (R-HSA-400206 )
Cytoprotection by HMOX1 (R-HSA-9707564 )
Triglyceride catabolism (R-HSA-163560 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
54 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate decreases the expression of Fatty acid-binding protein, liver (FABP1). [1]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Fatty acid-binding protein, liver (FABP1). [2]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Fatty acid-binding protein, liver (FABP1). [3]
Cupric Sulfate DMP0NFQ Approved Cupric Sulfate decreases the expression of Fatty acid-binding protein, liver (FABP1). [4]
Cisplatin DMRHGI9 Approved Cisplatin increases the expression of Fatty acid-binding protein, liver (FABP1). [5]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Fatty acid-binding protein, liver (FABP1). [2]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Fatty acid-binding protein, liver (FABP1). [6]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide affects the expression of Fatty acid-binding protein, liver (FABP1). [7]
Methotrexate DM2TEOL Approved Methotrexate increases the expression of Fatty acid-binding protein, liver (FABP1). [8]
Zoledronate DMIXC7G Approved Zoledronate increases the expression of Fatty acid-binding protein, liver (FABP1). [10]
Menadione DMSJDTY Approved Menadione affects the expression of Fatty acid-binding protein, liver (FABP1). [7]
Folic acid DMEMBJC Approved Folic acid increases the expression of Fatty acid-binding protein, liver (FABP1). [11]
Troglitazone DM3VFPD Approved Troglitazone increases the expression of Fatty acid-binding protein, liver (FABP1). [12]
Azathioprine DMMZSXQ Approved Azathioprine decreases the expression of Fatty acid-binding protein, liver (FABP1). [13]
Paclitaxel DMLB81S Approved Paclitaxel decreases the expression of Fatty acid-binding protein, liver (FABP1). [14]
Diclofenac DMPIHLS Approved Diclofenac decreases the expression of Fatty acid-binding protein, liver (FABP1). [12]
Clozapine DMFC71L Approved Clozapine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Fenofibrate DMFKXDY Approved Fenofibrate increases the expression of Fatty acid-binding protein, liver (FABP1). [16]
Fluoxetine DM3PD2C Approved Fluoxetine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Sertraline DM0FB1J Approved Sertraline increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Bosentan DMIOGBU Approved Bosentan decreases the expression of Fatty acid-binding protein, liver (FABP1). [17]
Bezafibrate DMZDCS0 Approved Bezafibrate decreases the expression of Fatty acid-binding protein, liver (FABP1). [18]
Olanzapine DMPFN6Y Approved Olanzapine increases the expression of Fatty acid-binding protein, liver (FABP1). [19]
Orlistat DMRJSP8 Approved Orlistat decreases the expression of Fatty acid-binding protein, liver (FABP1). [14]
Thioridazine DM35M8J Approved Thioridazine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Imipramine DM2NUH3 Approved Imipramine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Clomipramine DMINRKW Approved Clomipramine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Citalopram DM2G9AE Approved Citalopram increases the expression of Fatty acid-binding protein, liver (FABP1). [20]
Erythromycin DM4K7GQ Approved Erythromycin increases the expression of Fatty acid-binding protein, liver (FABP1). [21]
Loratadine DMF3AN7 Approved Loratadine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Pentamidine DMHZJCG Approved Pentamidine decreases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Quinidine DMLPICK Approved Quinidine increases the expression of Fatty acid-binding protein, liver (FABP1). [20]
Flecainide DMSQDLE Approved Flecainide increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Perhexiline DMINO7Z Approved Perhexiline increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Doxepin DMPI98T Approved Doxepin increases the expression of Fatty acid-binding protein, liver (FABP1). [20]
Urethane DM7NSI0 Phase 4 Urethane decreases the expression of Fatty acid-binding protein, liver (FABP1). [22]
SNDX-275 DMH7W9X Phase 3 SNDX-275 decreases the expression of Fatty acid-binding protein, liver (FABP1). [23]
Chlorpromazine DMBGZI3 Phase 3 Trial Chlorpromazine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
TESAGLITAZAR DMGRBN5 Phase 3 TESAGLITAZAR increases the expression of Fatty acid-binding protein, liver (FABP1). [24]
Amiodarone DMUTEX3 Phase 2/3 Trial Amiodarone increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
Belinostat DM6OC53 Phase 2 Belinostat decreases the expression of Fatty acid-binding protein, liver (FABP1). [23]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene increases the mutagenesis of Fatty acid-binding protein, liver (FABP1). [25]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Fatty acid-binding protein, liver (FABP1). [26]
Chlorcyclizine DM3L52Q Phase 1 Chlorcyclizine increases the expression of Fatty acid-binding protein, liver (FABP1). [15]
ZIMELIDINE DMNI3U2 Withdrawn from market ZIMELIDINE increases the expression of Fatty acid-binding protein, liver (FABP1). [21]
PIRINIXIC ACID DM82Y75 Preclinical PIRINIXIC ACID increases the expression of Fatty acid-binding protein, liver (FABP1). [27]
Bisphenol A DM2ZLD7 Investigative Bisphenol A affects the expression of Fatty acid-binding protein, liver (FABP1). [28]
Glyphosate DM0AFY7 Investigative Glyphosate increases the expression of Fatty acid-binding protein, liver (FABP1). [29]
Hexadecanoic acid DMWUXDZ Investigative Hexadecanoic acid increases the expression of Fatty acid-binding protein, liver (FABP1). [30]
D-glucose DMMG2TO Investigative D-glucose increases the expression of Fatty acid-binding protein, liver (FABP1). [31]
Linalool DMGZQ5P Investigative Linalool increases the expression of Fatty acid-binding protein, liver (FABP1). [16]
GW7647 DM9RD0C Investigative GW7647 increases the expression of Fatty acid-binding protein, liver (FABP1). [32]
Farnesol DMV2X1B Investigative Farnesol increases the expression of Fatty acid-binding protein, liver (FABP1). [32]
Linoleic acid DMDGPY9 Investigative Linoleic acid decreases the expression of Fatty acid-binding protein, liver (FABP1). [18]
------------------------------------------------------------------------------------
⏷ Show the Full List of 54 Drug(s)
1 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Marinol DM70IK5 Approved Marinol affects the binding of Fatty acid-binding protein, liver (FABP1). [9]
------------------------------------------------------------------------------------

References

1 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
2 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
3 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
4 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
5 Renal L-type fatty acid-binding protein mediates the bezafibrate reduction of cisplatin-induced acute kidney injury. Kidney Int. 2008 Jun;73(12):1374-84. doi: 10.1038/ki.2008.106. Epub 2008 Mar 26.
6 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
7 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
8 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
9 FABP1 controls hepatic transport and biotransformation of (9)-THC. Sci Rep. 2019 May 20;9(1):7588. doi: 10.1038/s41598-019-44108-3.
10 Zoledronic acid-induced oxidative damage and endoplasmic reticulum stress-mediated apoptosis in human embryonic kidney (HEK-293) cells. J Biochem Mol Toxicol. 2022 Aug;36(8):e23083. doi: 10.1002/jbt.23083. Epub 2022 May 19.
11 Neuronal and cardiac toxicity of pharmacological compounds identified through transcriptomic analysis of human pluripotent stem cell-derived embryoid bodies. Toxicol Appl Pharmacol. 2021 Dec 15;433:115792. doi: 10.1016/j.taap.2021.115792. Epub 2021 Nov 3.
12 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
13 A transcriptomics-based in vitro assay for predicting chemical genotoxicity in vivo. Carcinogenesis. 2012 Jul;33(7):1421-9.
14 Orlistat Displays Antitumor Activity and Enhances the Efficacy of Paclitaxel in Human Hepatoma Hep3B Cells. Chem Res Toxicol. 2019 Feb 18;32(2):255-264. doi: 10.1021/acs.chemrestox.8b00269. Epub 2019 Jan 22.
15 A toxicogenomic approach to drug-induced phospholipidosis: analysis of its induction mechanism and establishment of a novel in vitro screening system. Toxicol Sci. 2005 Feb;83(2):282-92.
16 Linalool is a PPARalpha ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome. J Lipid Res. 2014 Jun;55(6):1098-110.
17 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
18 Expression of cFABP and PPAR in trophoblast cells: effect of PPAR ligands on linoleic acid uptake and differentiation. Biochim Biophys Acta. 2005 Feb 21;1687(1-3):181-94. doi: 10.1016/j.bbalip.2004.11.017.
19 Up-regulation of hepatic fatty acid transporters and inhibition/down-regulation of hepatic OCTN2 contribute to olanzapine-induced liver steatosis. Toxicol Lett. 2019 Nov;316:183-193. doi: 10.1016/j.toxlet.2019.08.013. Epub 2019 Aug 19.
20 In vitro detection of drug-induced phospholipidosis using gene expression and fluorescent phospholipid based methodologies. Toxicol Sci. 2007 Sep;99(1):162-73.
21 Determination of phospholipidosis potential based on gene expression analysis in HepG2 cells. Toxicol Sci. 2007 Mar;96(1):101-14.
22 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
23 Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
24 AZ 242, a novel PPARalpha/gamma agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats. J Lipid Res. 2002 Nov;43(11):1855-63. doi: 10.1194/jlr.m200127-jlr200.
25 Exome-wide mutation profile in benzo[a]pyrene-derived post-stasis and immortal human mammary epithelial cells. Mutat Res Genet Toxicol Environ Mutagen. 2014 Dec;775-776:48-54. doi: 10.1016/j.mrgentox.2014.10.011. Epub 2014 Nov 4.
26 CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
27 Activation of sterol regulatory element-binding proteins in mice exposed to perfluorooctanoic acid for 28?days. Arch Toxicol. 2015 Sep;89(9):1569-78. doi: 10.1007/s00204-014-1322-7. Epub 2014 Aug 6.
28 Comprehensive analysis of transcriptomic changes induced by low and high doses of bisphenol A in HepG2 spheroids in vitro and rat liver in vivo. Environ Res. 2019 Jun;173:124-134. doi: 10.1016/j.envres.2019.03.035. Epub 2019 Mar 18.
29 Alterations in cell viability, reactive oxygen species production, and modulation of gene expression involved in mitogen-activated protein kinase/extracellular regulating kinase signaling pathway by glyphosate and its commercial formulation in hepatocellular carcinoma cells. Toxicol Ind Health. 2023 Feb;39(2):81-93. doi: 10.1177/07482337221149571. Epub 2023 Jan 10.
30 Exendin-4, a glucagon-like peptide-1 receptor agonist, reduces hepatic steatosis and endoplasmic reticulum stress by inducing nuclear factor erythroid-derived 2-related factor 2 nuclear translocation. Toxicol Appl Pharmacol. 2018 Dec 1;360:18-29.
31 Transcriptional Regulation of Human Arylamine N-Acetyltransferase 2 Gene by Glucose and Insulin in Liver Cancer Cell Lines. Toxicol Sci. 2022 Nov 23;190(2):158-172. doi: 10.1093/toxsci/kfac103.
32 Farnesol induces fatty acid oxidation and decreases triglyceride accumulation in steatotic HepaRG cells. Toxicol Appl Pharmacol. 2019 Feb 15;365:61-70.