General Information of Drug Transporter (DT)
DT ID DTD0029 Transporter Info
Gene Name SLCO1A2
Transporter Name Organic anion transporting polypeptide 1A2
Gene ID
6579
UniProt ID
P46721

Transcriptional Regulation of This DT (TSR)

TF Superclass1: Basic domains

      Class1.1: Basic leucine zipper factors

Click to Show/Hide the Full List of 1 TF(s) Regulating This DT

        BACH1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of SLCO1A2 gene in breast cancer bone metastasis condition [1]

TF Protein Name

Transcription regulator protein BACH1 Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Transcription regulator protein BACH1 (BACH1) has been reported to activate the transcription of SLCO1A2 gene in breast cancer bone metastasis condition, which leads to an increased expression of the drug transporter Organic anion transporting polypeptide 1A2.

      Class1.2: Basic helix-loop-helix factors

Click to Show/Hide the Full List of 1 TF(s) Regulating This DT

        TCF4 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of SLCO1A2 gene in glioblastoma multiforme condition [2]

TF Protein Name

Transcription factor 4 Transcription Factor Info

Affected Drug/Substrate

Temozolomide

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Transcription factor 4 (TCF4) has been reported to activate the transcription of SLCO1A2 gene in glioblastoma multiforme condition, which leads to an increased expression of the drug transporter Organic anion transporting polypeptide 1A2.

TF Superclass2: Zinc-coordinating DNA-binding domains

      Class2.1: Nuclear receptors with C4 zinc fingers

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        AR 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in prostate cancer condition [3]

TF Protein Name

Androgen receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Androgen receptor (AR) has been reported to bind to the transcription of SLCO1A2 gene in prostate cancer condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

        HNF4A 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in health condition [4]

TF Protein Name

Hepatocyte nuclear factor 4-alpha Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Hepatocyte nuclear factor 4-alpha (HNF4A) has been reported to bind to the transcription of SLCO1A2 gene in health condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

        NR1I2 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of SLCO1A2 gene in breast cancer condition [5]

TF Protein Name

Nuclear receptor subfamily 1 group I member 2 Transcription Factor Info

Studied Phenotype

Breast cancer [ICD11: 2C60-2C6Z]

Tissue

Breast

Related DT Changes

Up regulating

Experimental Material

human breast cancer cell isolates

Detailed Description

Nuclear receptor subfamily 1 group I member 2 (NR1I2) has been reported to activate the transcription of SLCO1A2 gene in breast cancer condition, which leads to an increased expression of the drug transporter Organic anion transporting polypeptide 1A2.

       Transcriptional Phenomenon2

Activation of SLCO1A2 gene in health condition [6]

TF Protein Name

Nuclear receptor subfamily 1 group I member 2 Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Liver

Related DT Changes

up regulating

Experimental Material

Human liver samples

Detailed Description

Nuclear receptor subfamily 1 group I member 2 (NR1I2), influenced by the metabolite from Host unspecified microbiota, has been reported to activate the transcription of SLCO1A2 gene in health condition, which leads to an increased expression of the drug transporter Organic anion transporting polypeptide 1A2.

        VDR 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of SLCO1A2 gene in colon cancer condition [7]

TF Protein Name

Vitamin D3 receptor Transcription Factor Info

Studied Phenotype

Colon cancer [ICD11: 2B90]

Tissue

Colon

Related DT Changes

Up regulating

Experimental Material

Human colon adenocarcinoma cells (Caco-2)

Detailed Description

Vitamin D3 receptor (VDR) has been reported to activate the transcription of SLCO1A2 gene in colon cancer condition, which leads to an increased expression of the drug transporter Organic anion transporting polypeptide 1A2.

TF Superclass3: Helix-turn-helix domains

      Class3.3: Fork head / winged helix factors

Click to Show/Hide the Full List of 2 TF(s) Regulating This DT

        FOXA1 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in prostate carcinoma condition [8]

TF Protein Name

Hepatocyte nuclear factor 3-alpha Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Hepatocyte nuclear factor 3-alpha (FOXA1) has been reported to bind to the transcription of SLCO1A2 gene in prostate carcinoma condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

       Transcriptional Phenomenon2

Binding to SLCO1A2 gene in prostate cancer condition [9]

TF Protein Name

Hepatocyte nuclear factor 3-alpha Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Hepatocyte nuclear factor 3-alpha (FOXA1) has been reported to bind to the transcription of SLCO1A2 gene in prostate cancer condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

        FOXA2 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in health condition [4]

TF Protein Name

Hepatocyte nuclear factor 3-beta Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Hepatocyte nuclear factor 3-beta (FOXA2) has been reported to bind to the transcription of SLCO1A2 gene in health condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

TF Superclass6: Immunoglobulin fold

      Class6.1: Rel homology region factors

Click to Show/Hide the Full List of 2 TF(s) Regulating This DT

        NFKB1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Repression of SLCO1A2 gene in breast cancer condition [10]

TF Protein Name

Nuclear factor NF-kappa-B p105 subunit Transcription Factor Info

Studied Phenotype

Breast cancer [ICD11: 2C60-2C6Z]

Tissue

Breast

Related DT Changes

Down regulating

Experimental Material

Human invasive breast carcinoma of no special type cells (MCF-7)

Detailed Description

Nuclear factor NF-kappa-B p105 subunit (NFKB1) has been reported to repress the transcription of SLCO1A2 gene in breast cancer condition, which leads to a decreased expression of the drug transporter Organic anion transporting polypeptide 1A2.

        RELA 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Repression of SLCO1A2 gene in breast cancer condition [10]

TF Protein Name

Transcription factor p65 Transcription Factor Info

Studied Phenotype

Breast cancer [ICD11: 2C60-2C6Z]

Tissue

Breast

Related DT Changes

Down regulating

Experimental Material

Human invasive breast carcinoma of no special type cells (MCF-7)

Detailed Description

Transcription factor p65 (RELA) has been reported to repress the transcription of SLCO1A2 gene in breast cancer condition, which leads to a decreased expression of the drug transporter Organic anion transporting polypeptide 1A2.

      Class6.2: STAT domain factors

Click to Show/Hide the Full List of 1 TF(s) Regulating This DT

        STAT3 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in glioblastoma multiforme condition [2]

TF Protein Name

Signal transducer and activator of transcription 3 Transcription Factor Info

Affected Drug/Substrate

Temozolomide

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Signal transducer and activator of transcription 3 (STAT3) has been reported to bind to the transcription of SLCO1A2 gene in glioblastoma multiforme condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.

      Class6.4: Runt domain factors

Click to Show/Hide the Full List of 1 TF(s) Regulating This DT

        RUNX1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to SLCO1A2 gene in health condition [11]

TF Protein Name

Runt-related transcription factor 1 Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Runt-related transcription factor 1 (RUNX1) has been reported to bind to the transcription of SLCO1A2 gene in health condition, which leads to an affected expression of the drug transporter Organic anion transporting polypeptide 1A2.
References
1 Transcriptional network analysis identifies BACH1 as a master regulator of breast cancer bone metastasis. J Biol Chem. 2012;287(40):33533-44.
2 Unique genome-wide map of TCF4 and STAT3 targets using ChIP-seq reveals their association with new molecular subtypes of glioblastoma. Neuro Oncol. 2013;15(3):279-89.
3 Inhibition of p53 expression modifies the specificity of chromatin binding by the androgen receptor. Oncotarget. 2012;3(2):183-94.
4 Molecular interactions between HNF4a, FOXA2 and GABP identified at regulatory DNA elements through ChIP-sequencing. Nucleic Acids Res. 2009;37(22):7498-508.
5 Interplay between the nuclear receptor pregnane X receptor and the uptake transporter organic anion transporter polypeptide 1A2 selectively enhances estrogen effects in breast cancer. Cancer Res. 2008 Nov 15;68(22):9338-47.
6 Transcriptional profiling of genes induced in the livers of patients treated with carbamazepine. Clin Pharmacol Ther. 2006 Nov;80(5):440-456.
7 The SLCO1A2 gene, encoding human organic anion-transporting polypeptide 1A2, is transactivated by the vitamin D receptor. Mol Pharmacol. 2012 Jul;82(1):37-46.
8 SUMO ligase PIAS1 functions as a target gene selective androgen receptor coregulator on prostate cancer cell chromatin. Nucleic Acids Res. 2015;43(2):848-61.
9 Integrative analysis of FOXP1 function reveals a tumor-suppressive effect in prostate cancer. Mol Endocrinol. 2014;28(12):2012-24.
10 Identification of a NF Kappa B Inhibition Site on the Proximal Promoter Region of Human Organic Anion Transporting Polypeptide 1A2 Coding Gene SLCO1A2. Drug Metab Dispos. 2018 May;46(5):643-651.
11 Genome-wide analyses reveal properties of redundant and specific promoter occupancy within the ETS gene family. Genes Dev. 2007;21(15):1882-94.

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