General Information of Drug Transporter (DT)
DT ID DTD0004 Transporter Info
Gene Name ABCG2
Transporter Name Breast cancer resistance protein
Gene ID
9429
UniProt ID
Q9UNQ0

Transcriptional Regulation of This DT (TSR)

TF Superclass1: Basic domains

      Class1.1: Basic leucine zipper factors

Click to Show/Hide the Full List of 3 TF(s) Regulating This DT

        FOSL2 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [1]

TF Protein Name

Fos-related antigen 2 Transcription Factor Info

Tissue

Breast; Liver; Lung

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

Fos-related antigen 2 (FOSL2) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

        JUND 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in coronary artery disease condition [2]

TF Protein Name

Transcription factor JunD Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Transcription factor JunD (JUND) has been reported to bind to the transcription of ABCG2 gene in coronary artery disease condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

        NFE2L2 

Click to Show/Hide to Show 3 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in non-small cell lung cancer condition [3]

TF Protein Name

Nuclear factor erythroid 2-related factor 2 Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone; Topotecan

Studied Phenotype

Non-small cell lung cancer [ICD11: 2C25.Y]

Tissue

Lung

Related DT Changes

Up regulating

Experimental Material

Human lung adenocarcinoma cells (A549)

Detailed Description

Nuclear factor erythroid 2-related factor 2 (NFE2L2) has been reported to activate the transcription of ABCG2 gene in non-small cell lung cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in hepatoblastoma condition [4]

TF Protein Name

Nuclear factor erythroid 2-related factor 2 Transcription Factor Info

Studied Phenotype

Hepatoblastoma [ICD11: 2C12.01]

Tissue

Liver

Related DT Changes

up regulating

Experimental Material

Human hepatoblastoma cells (HepG2)

Detailed Description

Nuclear factor erythroid 2-related factor 2 (NFE2L2), influenced by the exogenous bisphenol A, has been reported to activate the transcription of ABCG2 gene in hepatoblastoma condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon3

Activation of ABCG2 gene in health condition [5]

TF Protein Name

Nuclear factor erythroid 2-related factor 2 Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Liver

Related DT Changes

up regulating

Experimental Material

Human fetal liver samples

Detailed Description

Nuclear factor erythroid 2-related factor 2 (NFE2L2), influenced by the exogenous bisphenol A, has been reported to activate the transcription of ABCG2 gene in health condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

      Class1.2: Basic helix-loop-helix factors

Click to Show/Hide the Full List of 3 TF(s) Regulating This DT

        AHR 

Click to Show/Hide to Show 4 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in colon cancer condition [6], [7]

TF Protein Name

Aryl hydrocarbon receptor Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone; Benzo[a]pyrene-3-sulfate

Studied Phenotype

Colon cancer [ICD11: 2B90]

Tissue

Colon

Related DT Changes

Up regulating

Experimental Material

C57BL/6N mice

Detailed Description

Aryl hydrocarbon receptor (AHR) has been reported to activate the transcription of ABCG2 gene in colon cancer condition, which leads to an enhanced function of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in health condition [6]

TF Protein Name

Aryl hydrocarbon receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Aryl hydrocarbon receptor (AHR) has been reported to activate the transcription of ABCG2 gene in health condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon3

Activation of ABCG2 gene in colon cancer condition [8]

TF Protein Name

Aryl hydrocarbon 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

Aryl hydrocarbon receptor (AHR), influenced by the exogenous polychlorinated dibenzodioxin, has been reported to activate the transcription of ABCG2 gene in colon cancer condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon4

Activation of ABCG2 gene in health condition [9]

TF Protein Name

Aryl hydrocarbon receptor Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Placenta

Related DT Changes

up regulating

Experimental Material

Human placental trophoblast cells (TR-S)

Detailed Description

Aryl hydrocarbon receptor (AHR), influenced by the exogenous polychlorinated dibenzodioxin, has been reported to activate the transcription of ABCG2 gene in health condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        EPAS1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [10]

TF Protein Name

Endothelial PAS domain-containing protein 1 Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Heart

Related DT Changes

up regulating

Experimental Material

Human cardiac side population cells

Detailed Description

Endothelial PAS domain-containing protein 1 (EPAS1), influenced by the exogenous hydrogen Peroxide, has been reported to activate the transcription of ABCG2 gene in health condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        MYC 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in AK7 condition [11]

TF Protein Name

Myc proto-oncogene protein Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Myc proto-oncogene protein (MYC) has been reported to bind to the transcription of ABCG2 gene in AK7 condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

      Class1.3: Basic helix-span-helix factors

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

        TFAP2A 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [12]

TF Protein Name

Transcription factor AP-2-alpha Transcription Factor Info

Tissue

Cervix

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

Transcription factor AP-2-alpha (TFAP2A) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

TF Superclass2: Zinc-coordinating DNA-binding domains

      Class2.1: Nuclear receptors with C4 zinc fingers

Click to Show/Hide the Full List of 10 TF(s) Regulating This DT

        AR 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Repression of ABCG2 gene in prostate cancer condition [13]

TF Protein Name

Androgen receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Down regulating

Detailed Description

Androgen receptor (AR) has been reported to repress the transcription of ABCG2 gene in prostate cancer condition, which leads to a decreased expression of the drug transporter Breast cancer resistance protein.

        ESR1 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in breast cancer condition [14]

TF Protein Name

Estrogen receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Estrogen receptor (ESR1) has been reported to bind to the ABCG2 gene in breast cancer condition, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in bone homeostasis condition [15]

TF Protein Name

Estrogen receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Estrogen receptor (ESR1) has been reported to activate the transcription of ABCG2 gene in bone homeostasis condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        HNF4A 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in health condition [16]

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 ABCG2 gene in health condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Binding to ABCG2 gene in health condition [17]

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 ABCG2 gene in health condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

        NR1H4 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in colorectal cancer condition [18]

TF Protein Name

Bile acid receptor Transcription Factor Info

Studied Phenotype

Colorectal cancer [ICD11: 2B91]

Tissue

Colon

Related DT Changes

up regulating

Experimental Material

human colorectal adenocarcinoma cells (LS174T)

Detailed Description

Bile acid receptor (NR1H4), influenced by the exogenous cisplatin, has been reported to activate the transcription of ABCG2 gene in colorectal cancer condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        NR1I2 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [19]

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 hepatocytes

Detailed Description

Nuclear receptor subfamily 1 group I member 2 (NR1I2), influenced by the exogenous rifampin, has been reported to activate the transcription of ABCG2 gene in health condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Repression of ABCG2 gene in breast cancer condition [20]

TF Protein Name

Nuclear receptor subfamily 1 group I member 2 Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone

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 receptor subfamily 1 group I member 2 (NR1I2) has been reported to repress the transcription of ABCG2 gene in breast cancer condition, which leads to a decreased expression of the drug transporter Breast cancer resistance protein.

        NR1I3 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [21]

TF Protein Name

Nuclear receptor subfamily 1 group I member 3 Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Liver

Related DT Changes

up regulating

Experimental Material

Human hepatocytes

Detailed Description

Nuclear receptor subfamily 1 group I member 3 (NR1I3), influenced by the exogenous phenobarbital, has been reported to activate the transcription of ABCG2 gene in health condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        NR3C1 

Click to Show/Hide to Show 3 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in ER(-) breast cancer condition [22]

TF Protein Name

Glucocorticoid receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Glucocorticoid receptor (NR3C1) has been reported to activate the transcription of ABCG2 gene in ER(-) breast cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in brain edema condition [23]

TF Protein Name

Glucocorticoid receptor Transcription Factor Info

Studied Phenotype

Brain edema [ICD11: 8D60.1]

Tissue

Brain

Related DT Changes

Up regulating

Experimental Material

Sprague-Dawley rats

Detailed Description

Glucocorticoid receptor (NR3C1) has been reported to activate the transcription of ABCG2 gene in brain edema condition, which leads to an enhanced function of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon3

Repression of ABCG2 gene in breast cancer condition [20]

TF Protein Name

Glucocorticoid receptor Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone

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

Glucocorticoid receptor (NR3C1) has been reported to repress the transcription of ABCG2 gene in breast cancer condition, which leads to a decreased expression of the drug transporter Breast cancer resistance protein.

        PGR 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in breast cancer condition [20]

TF Protein Name

Progesterone receptor Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone

Studied Phenotype

Breast cancer [ICD11: 2C60-2C6Z]

Tissue

Breast

Related DT Changes

Up regulating

Experimental Material

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

Detailed Description

Progesterone receptor (PGR) has been reported to activate the transcription of ABCG2 gene in breast cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Repression of ABCG2 gene in breast cancer condition [24]

TF Protein Name

Progesterone receptor Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Down regulating

Detailed Description

Progesterone receptor (PGR) has been reported to repress the transcription of ABCG2 gene in breast cancer condition, which leads to a decreased expression of the drug transporter Breast cancer resistance protein.

        PPARA 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [25]

TF Protein Name

Peroxisome proliferator-activated receptor alpha Transcription Factor Info

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Intestine

Related DT Changes

Up regulating

Experimental Material

C57BL/6 mice

Detailed Description

Peroxisome proliferator-activated receptor alpha (PPARA) has been reported to activate the transcription of ABCG2 gene in health condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        PPARG 

Click to Show/Hide to Show 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [26]

TF Protein Name

Peroxisome proliferator-activated receptor gamma Transcription Factor Info

Affected Drug/Substrate

Mitoxantrone

Studied Phenotype

Heallth [ICD11: N.A]

Tissue

Kidney

Related DT Changes

Up regulating

Experimental Material

Green monkey Kidney fibroblast-like cells (COS-1)

Detailed Description

Peroxisome proliferator-activated receptor gamma (PPARG) has been reported to activate the transcription of ABCG2 gene in health condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in colon cancer condition [27]

TF Protein Name

Peroxisome proliferator-activated receptor gamma 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

Peroxisome proliferator-activated receptor gamma (PPARG), influenced by the exogenous troglitazone, has been reported to activate the transcription of ABCG2 gene in colon cancer condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

      Class2.3: C2H2 zinc finger factors

Click to Show/Hide the Full List of 3 TF(s) Regulating This DT

        BCL6 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in health condition [28]

TF Protein Name

B-cell lymphoma 6 protein Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

B-cell lymphoma 6 protein (BCL6) has been reported to activate the transcription of ABCG2 gene in health condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        MAZ 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [1]

TF Protein Name

Myc-associated zinc finger protein Transcription Factor Info

Tissue

Blood; Bone marrow; Lung

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

Myc-associated zinc finger protein (MAZ) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

        SP1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in pancreatic cancer condition [29]

TF Protein Name

Transcription factor Sp1 Transcription Factor Info

Affected Drug/Substrate

Gemcitabine; 5-fluorouracil

Studied Phenotype

Pancreatic cancer [ICD11: 2C10]

Tissue

Pancreas

Related DT Changes

Up regulating

Experimental Material

Human pancreatic ductal adenocarcinoma cells (ASPC-1)

Detailed Description

Transcription factor Sp1 (SP1) has been reported to activate the transcription of ABCG2 gene in pancreatic cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

TF Superclass3: Helix-turn-helix domains

      Class3.1: Homeo domain factors

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

        MSX2 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in pancreatic cancer condition [29]

TF Protein Name

Homeobox protein MSX-2 Transcription Factor Info

Affected Drug/Substrate

Gemcitabine; 5-fluorouracil

Studied Phenotype

Pancreatic cancer [ICD11: 2C10]

Tissue

Pancreas

Related DT Changes

Up regulating

Experimental Material

Human pancreatic ductal adenocarcinoma cells (ASPC-1)

Detailed Description

Homeobox protein MSX-2 (MSX2) has been reported to activate the transcription of ABCG2 gene in pancreatic cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        NANOG 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in health condition [30]

TF Protein Name

Homeobox protein NANOG Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Homeobox protein NANOG (NANOG) has been reported to bind to the transcription of ABCG2 gene in health condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

      Class3.3: Fork head / winged helix factors

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

        FOXA2 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in health condition [17]

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 ABCG2 gene in health condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.

      Class3.5: Tryptophan cluster factors

Click to Show/Hide the Full List of 3 TF(s) Regulating This DT

        FLI1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [31]

TF Protein Name

Friend leukemia integration 1 transcription factor Transcription Factor Info

Tissue

Blood; Mesenchymal; Vein

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

Friend leukemia integration 1 transcription factor (FLI1) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

        GABPA 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [32]

TF Protein Name

GA-binding protein alpha chain Transcription Factor Info

Tissue

Blood; Liver; Lung; Mesenchymal

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

GA-binding protein alpha chain (GABPA) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

        SPI1 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Direct binding to ABCG2 gene [12]

TF Protein Name

Transcription factor PU.1 Transcription Factor Info

Tissue

Adrenal gland; Blood; Brain; Breast; Embryo; Foreskin; Heart; Intestine; Kidney; Lung; Muscle; Penis; Placenta; Renal cortex; Renal pelvis; Skin; Spinal cord; Stomach; Testes; Umbilical cord blood

Related DT Changes

Direct regulating

Experiment method

TF-transporter regulations were collected from ChIP-Seq datasets.

Detailed Description

Transcription factor PU.1 (SPI1) can directly bind to the ABCG2 gene, which in turn affects the expression or function of the drug transporter Breast cancer resistance protein.

TF Superclass4: Other all-alpha-helical DNA-binding domains

      Class4.1: High-mobility group domain factors

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

        SOX2 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in colorectal cancer condition [33]

TF Protein Name

Transcription factor SOX-2 Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Transcription factor SOX-2 (SOX2) has been reported to activate the transcription of ABCG2 gene in colorectal cancer condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

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 2 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in bone homeostasis condition [15]

TF Protein Name

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

Affected Drug/Substrate

17beta-estradiol

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Nuclear factor NF-kappa-B p105 subunit (NFKB1) has been reported to activate the transcription of ABCG2 gene in bone homeostasis condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

       Transcriptional Phenomenon2

Activation of ABCG2 gene in lung adenocarcinoma condition [34]

TF Protein Name

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

Studied Phenotype

Lung adenocarcinoma [ICD11: 2C25.0]

Tissue

Lung

Related DT Changes

up regulating

Experimental Material

Human lung adenocarcinoma cells (A549)

Detailed Description

Nuclear factor NF-kappa-B p105 subunit (NFKB1), influenced by the exogenous arsenic trioxide, has been reported to activate the transcription of ABCG2 gene in lung adenocarcinoma condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

        RELA 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Activation of ABCG2 gene in bone homeostasis condition [15]

TF Protein Name

Transcription factor p65 Transcription Factor Info

Affected Drug/Substrate

17beta-estradiol

Studied Phenotype

.

Related DT Changes

Up regulating

Detailed Description

Transcription factor p65 (RELA) has been reported to activate the transcription of ABCG2 gene in bone homeostasis condition, which leads to an increased expression of the drug transporter Breast cancer resistance protein.

      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

Activation of ABCG2 gene in epithelial ovarian cancer condition [35]

TF Protein Name

Signal transducer and activator of transcription 3 Transcription Factor Info

Affected Drug/Substrate

Doxorubicin

Studied Phenotype

Epithelial ovarian cancer [2B5D.0]

Tissue

Ovary

Related DT Changes

up regulating

Experimental Material

Human doxorubicin-resistant epithelial ovarian cancer cells (A2780-R)

Detailed Description

Signal transducer and activator of transcription 3 (STAT3), influenced by the exogenous paclitaxel, has been reported to activate the transcription of ABCG2 gene in epithelial ovarian cancer condition , which leads to an increased expression of the drug transporter Breast cancer resistance protein.

      Class6.3: p53 domain factors

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

        TP63 

Click to Show/Hide to Show 1 Transcriptional Phenomena      

       Transcriptional Phenomenon1

Binding to ABCG2 gene in epithelial to mesenchymal transition condition [36]

TF Protein Name

Tumor protein 63 Transcription Factor Info

Studied Phenotype

.

Related DT Changes

Direct regulating

Detailed Description

Tumor protein 63 (TP63) has been reported to bind to the transcription of ABCG2 gene in epithelial to mesenchymal transition condition, which leads to an affected expression of the drug transporter Breast cancer resistance protein.
References
1 NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(D1):D991-5.
2 Characterization of TCF21 Downstream Target Regions Identifies a Transcriptional Network Linking Multiple Independent Coronary Artery Disease Loci. PLoS Genet. 2015;11(5):e1005202.
3 Expression of ABCG2 (BCRP) is regulated by Nrf2 in cancer cells that confers side population and chemoresistance phenotype. Mol Cancer Ther. 2010 Aug;9(8):2365-76.
4 Nrf2-dependent and -independent induction of ABC transporters ABCC1, ABCC2, and ABCG2 in HepG2 cells under oxidative stress. J Exp Ther Oncol. 2007;6(4):335-48.
5 Correlation between Conjugated Bisphenol A Concentrations and Efflux Transporter Expression in Human Fetal Livers. Drug Metab Dispos. 2016 Jul;44(7):1061-5.
6 Aryl hydrocarbon receptor is a transcriptional activator of the human breast cancer resistance protein (BCRP/ABCG2). Mol Pharmacol. 2010 Aug;78(2):175-85.
7 Identification of BCRP as transporter of benzo[a]pyrene conjugates metabolically formed in Caco-2 cells and its induction by Ah-receptor agonists. Carcinogenesis. 2005 Oct;26(10):1754-63.
8 Phytochemicals induce breast cancer resistance protein in Caco-2 cells and enhance the transport of benzo[a]pyrene-3-sulfate. Toxicol Sci. 2007 Apr;96(2):227-36.
9 Aryl hydrocarbon receptor and aryl hydrocarbon nuclear translocator expression in human and rat placentas and transcription activity in human trophoblast cultures. Toxicol Sci. 2011 Sep;123(1):26-36.
10 Hypoxia-inducible factor-2alpha transactivates Abcg2 and promotes cytoprotection in cardiac side population cells. Circ Res. 2008 May 9;102(9):1075-81.
11 Gene regulation and epigenetic remodeling in murine embryonic stem cells by c-Myc. PLoS One. 2009;4(11):e7839.
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27 Short-chain fatty acids exert opposite effects on the expression and function of p-glycoprotein and breast cancer resistance protein in rat intestine. Acta Pharmacol Sin. 2021 Mar;42(3):470-481.
28 The transcriptional regulator BCL6 participates in the secondary gene regulatory response to vitamin D. Biochim Biophys Acta. 2015;1849(3):300-8.
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35 CD109 Promotes Drug Resistance in A2780 Ovarian Cancer Cells by Regulating the STAT3-NOTCH1 Signaling Axis. Int J Mol Sci. 2023 Jun 18;24(12):10306.
36 p63 attenuates epithelial to mesenchymal potential in an experimental prostate cell model. PLoS One. 2013;8(5):e62547.

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