Detail Information of Exogenous Modulation

General Information of Drug Transporter (DT)
DT ID DTD0046 Transporter Info
Gene Name ABCA8
Transporter Name ATP-binding cassette sub-family A member 8
Gene ID
10351
UniProt ID
O94911
Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)

Chemical Compound

  DT Modulation1

 Estradiol co-treated with TGFB1 protein results in decreased expression of ABCA8 mRNA [27]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 Progesterone co-treated with Estradiol results in decreased expression of ABCA8 mRNA [28]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Cyclosporine results in decreased methylation of ABCA8 promoter [10]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Benzo(a)pyrene affects the methylation of ABCA8 5' UTR [24]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 Benzo(a)pyrene affects the methylation of ABCA8 intron [23]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation3

 Benzo(a)pyrene affects the methylation of ABCA8 promoter [24]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation4

 Benzo(a)pyrene results in increased mutagenesis of ABCA8 gene [25]

Regulation Mechanism

 Transcription Factor Info

  2-palmitoylglycerol

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 2-palmitoylglycerol results in increased expression of ABCA8 mRNA [19]

Regulation Mechanism

 Transcription Factor Info

  7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide affects the expression of ABCA8 mRNA [20]

Regulation Mechanism

 Transcription Factor Info

  Adenosine Triphosphate

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Adenosine Triphosphate affects the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  butyraldehyde

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 butyraldehyde results in decreased expression of ABCA8 mRNA [11]

Regulation Mechanism

 Transcription Factor Info

  Digoxin

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Digoxin inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  Docetaxel

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Docetaxel results in decreased susceptibility to Docetaxel which results in increased expression of ABCA8 mRNA [26]

Regulation Mechanism

 Transcription Factor Info

  dofequidar

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 dofequidar inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  estrone sulfate

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 ABCA8 protein affects the transport of estrone sulfate [22]

Regulation Mechanism

 Transcription Factor Info

  Leukotriene C4

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 ABCA8 protein affects the transport of Leukotriene C4 [22]

Regulation Mechanism

 Transcription Factor Info

  licochalcone B

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 licochalcone B results in decreased expression of ABCA8 mRNA [29]

Regulation Mechanism

 Transcription Factor Info

  Okadaic Acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Okadaic Acid results in decreased expression of ABCA8 mRNA [31]

Regulation Mechanism

 Transcription Factor Info

  p-Aminohippuric Acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 ABCA8 protein affects the transport of p-Aminohippuric Acid [22]

Regulation Mechanism

 Transcription Factor Info

  perfluorooctane sulfonic acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 perfluorooctane sulfonic acid results in decreased expression of ABCA8 mRNA [13]

Regulation Mechanism

 Transcription Factor Info

  Probenecid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Probenecid inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  Progesterone

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Progesterone co-treated with Estradiol results in decreased expression of ABCA8 mRNA [28]

Regulation Mechanism

 Transcription Factor Info

  sodium arsenite

            3 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 sodium arsenite affects the methylation of ABCA8 gene [33]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 sodium arsenite results in decreased expression of ABCA8 mRNA [15]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation3

 sodium arsenite results in increased expression of ABCA8 mRNA [34]

Regulation Mechanism

 Transcription Factor Info

  Sodium Selenite

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Sodium Selenite results in decreased expression of ABCA8 mRNA [35]

Regulation Mechanism

 Transcription Factor Info

  Taurocholic Acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 ABCA8 protein affects the transport of Taurocholic Acid [22]

Regulation Mechanism

 Transcription Factor Info

  Verapamil

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Verapamil inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  verlukast

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 verlukast inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

  Vincristine

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Vincristine results in decreased susceptibility to Vincristine which affects the expression of ABCA8 mRNA [26]

Regulation Mechanism

 Transcription Factor Info

Nanoparticle

  perfluoro-n-nonanoic acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 perfluoro-n-nonanoic acid results in decreased expression of ABCA8 mRNA [32]

Regulation Mechanism

 Transcription Factor Info

Approved Drug

  Estradiol

            3 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Estradiol inhibits the expression of ABCA8 [1]

  Acetaminophen

            2 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Acetaminophen inhibits the expression of ABCA8 [2]

  DT Modulation2

 Acetaminophen results in increased expression of ABCA8 mRNA [21]

Regulation Mechanism

 Transcription Factor Info

  Indomethacin

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Indomethacin increases the expression of ABCA8 [3]

  Rosiglitazone

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Rosiglitazone inhibits the expression of ABCA8 [4]

  Valproic Acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Valproic Acid affects the expression of ABCA8 [5]

  Vorinostat

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Vorinostat inhibits the expression of ABCA8 [6]

  Rifampin

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Rifampin inhibits the expression of ABCA8 [7]

  Doxorubicin

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Doxorubicin inhibits the expression of ABCA8 [8]

  Sunitinib

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Sunitinib inhibits the expression of ABCA8 [9]

  Cyclosporine

            2 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Cyclosporine inhibits the expression of ABCA8 [10]

Drug in Phase 3 Trial

  Triclosan

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Triclosan inhibits the expression of ABCA8 [17]

Drug in Phase 1 Trial

  Sodium arsenite

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Sodium arsenite inhibits the expression of ABCA8 [15]

Natural Product

  Particulate Matter

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Particulate Matter inhibits the expression of ABCA8 [16]

Mycotoxins

  Aflatoxin B1

            4 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Aflatoxin B1 inhibits the expression of ABCA8 [12]

  DT Modulation2

 Aflatoxin B1 affects the expression of ABCA8 protein [1]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation3

 Aflatoxin B1 results in decreased methylation of ABCA8 gene [12]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation4

 Aflatoxin B1 results in decreased methylation of ABCA8 intron [23]

Regulation Mechanism

 Transcription Factor Info

  ochratoxin A

            2 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 ABCA8 protein affects the transport of ochratoxin A [22]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 ochratoxin A inhibits the reaction ABCA8 protein results in increased uptake of estradiol-17 beta-glucuronide [22]

Regulation Mechanism

 Transcription Factor Info

Acute Toxic Substance

  Formaldehyde

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Formaldehyde increases the expression of ABCA8 [14]

Carcinogen

  Benzo(a)pyrene

            5 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Benzo(a)pyrene inhibits the expression of ABCA8 [18]

  Nickel

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Nickel results in decreased expression of ABCA8 mRNA [30]

Regulation Mechanism

 Transcription Factor Info

Health and Environmental Toxicant

  Butyraldehyde

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Butyraldehyde inhibits the expression of ABCA8 [11]

  Perfluorooctane sulfonic acid

            1 DT Activity Modulations Related to This Exogenous Factor Click to Show/Hide the Full List

  DT Modulation1

 Perfluorooctane sulfonic acid inhibits the expression of ABCA8 [13]
References
1 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.
2 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
3 Evaluation of developmental toxicity using undifferentiated human embryonic stem cells. J Appl Toxicol. 2015 Feb;35(2):205-18.
4 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
5 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20.
6 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.
7 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
8 Bringing in vitro analysis closer to in vivo: Studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
9 Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761.
10 Integrative "-Omics" Analysis in Primary Human Hepatocytes Unravels Persistent Mechanisms of Cyclosporine A-Induced Cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
11 Integrated analysis of microRNA and mRNA expression profiles highlights aldehyde-induced inflammatory responses in cells relevant for lung toxicity. Toxicology. 2015 Aug 6;334:111-21.
12 Aflatoxin B1 induces persistent epigenomic effects in primary human hepatocytes associated with hepatocellular carcinoma. Toxicology. 2016 Mar 28;350-352:31-9.
13 The role of hepatocyte nuclear factor 4-alpha in perfluorooctanoic acid- and perfluorooctanesulfonic acid-induced hepatocellular dysfunction. Toxicol Appl Pharmacol. 2016 Aug 1;304:18-29.
14 Regulation of Chromatin Assembly and Cell Transformation by Formaldehyde Exposure in Human Cells. Environ Health Perspect. 2017 Sep 21;125(9):097019.
15 Cellular and Molecular Effects of Prolonged Low-Level Sodium Arsenite Exposure on Human Hepatic HepaRG Cells. Toxicol Sci. 2018 Apr 1;162(2):676-687.
16 Transcriptional profiling of human bronchial epithelial cell BEAS-2B exposed to diesel and biomass ultrafine particles. BMC Genomics. 2018 Apr 27;19(1):302.
17 Transcriptome and DNA Methylome Dynamics during Triclosan-Induced Cardiomyocyte Differentiation Toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
18 Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297.
19 Direct effect of 2-palmitoyl glycerol on promotion of gamma aminobutyric acid synthesis in normal human fetal-derived astrocytes. FEBS Open Bio. 2023;13(7):1320-1332.
20 Benzo[a]pyrene diol epoxide stimulates an inflammatory response in normal human lung fibroblasts through a p53 and JNK mediated pathway. Carcinogenesis. 2010;31(6):1149-57.
21 Blood transcript immune signatures distinguish a subset of people with elevated serum ALT from others given acetaminophen. Clin Pharmacol Ther. 2016 Apr;99(4):432-41.
22 Functional analysis of ABCA8, a new drug transporter. Biochem Biophys Res Commun. 2002 Oct 18;298(1):41-5.
23 Effect of aflatoxin B(1), benzo[a]pyrene, and methapyrilene on transcriptomic and epigenetic alterations in human liver HepaRG cells. Food Chem Toxicol. 2018;121:214-223.
24 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
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;775-776:48-54.
26 L-type calcium channel blockers reverse docetaxel and vincristine-induced multidrug resistance independent of ABCB1 expression in human lung cancer cell lines. Toxicol Lett. 2010 Feb 15;192(3):408-18.
27 Transforming growth factor beta1 targets estrogen receptor signaling in bronchial epithelial cells. Respir Res. 2018 Aug 30;19(1):160.
28 Progesterone regulation of implantation-related genes: new insights into the role of oestrogen. Cell Mol Life Sci. 2007 Apr;64(7-8):1009-32.
29 Integrated miRNA and mRNA omics reveal the anti-cancerous mechanism of Licochalcone B on Human Hepatoma Cell HepG2. Food Chem Toxicol. 2021;150:112096.
30 Patients with atopic dermatitis have attenuated and distinct contact hypersensitivity responses to common allergens in skin. J Allergy Clin Immunol. 2015;135(3):712-20.
31 A multi-omics approach to elucidate okadaic acid-induced changes in human HepaRG hepatocarcinoma cells. Arch Toxicol. 2024;98(9):2919-2935.
32 Perfluorooctanoic acid (PFOA), perfluorooctane sulfonic acid (PFOS), and perfluorononanoic acid (PFNA) increase triglyceride levels and decrease cholesterogenic gene expression in human HepaRG liver cells. Arch Toxicol. 2020 Sep;94(9):3137-3155.
33 Microarray dataset of transient and permanent DNA methylation changes in HeLa cells undergoing inorganic arsenic-mediated epithelial-to-mesenchymal transition. Data Brief. 2017;13:6-9.
34 Gene expression changes in human lung cells exposed to arsenic, chromium, nickel or vanadium indicate the first steps in cancer. Metallomics. 2012 Aug;4(8):784-93.
35 Transcriptomic responses of cancerous and noncancerous human colon cells to sulforaphane and selenium. Chem Res Toxicol. 2014;27(3):377-86.

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