General Information of Drug Transporter (DT)
DT ID DTD0511 Transporter Info
Gene Name KCNJ11
Transporter Name ATP-sensitive inward rectifier potassium channel 11
Gene ID
3767
UniProt ID
Q14654
Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)

Chemical Compound

  DT Modulation1

KCNJ11 mutant form co-treated with ABCC8 mutant form results in decreased susceptibility to Tolbutamide [15]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Tolbutamide inhibits the reaction ABCC8 protein mutant form results in increased activity of KCNJ11 protein [2]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Tolbutamide results in decreased activity of KCNJ11 protein [2]

Regulation Mechanism

Transcription Factor Info

  1-Methyl-4-phenylpyridinium

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

  DT Modulation1

1-Methyl-4-phenylpyridinium results in increased expression of KCNJ11 mRNA [7]

Regulation Mechanism

Transcription Factor Info

  abrine

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

  DT Modulation1

abrine results in decreased expression of KCNJ11 mRNA [12]

Regulation Mechanism

Transcription Factor Info

  Benzo(a)pyrene

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

  DT Modulation1

Benzo(a)pyrene affects the methylation of KCNJ11 3' UTR [13]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Benzo(a)pyrene affects the methylation of KCNJ11 promoter [13]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Benzo(a)pyrene results in increased methylation of KCNJ11 exon [13]

Regulation Mechanism

Transcription Factor Info

  bisphenol A

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

  DT Modulation1

bisphenol A results in decreased expression of KCNJ11 mRNA [10]

Regulation Mechanism

Transcription Factor Info

  bisphenol S

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

  DT Modulation1

bisphenol S results in decreased expression of KCNJ11 mRNA [14]

Regulation Mechanism

Transcription Factor Info

  Chlorpropamide

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

  DT Modulation1

KCNJ11 mutant form co-treated with ABCC8 mutant form results in decreased susceptibility to Chlorpropamide [15]

Regulation Mechanism

Transcription Factor Info

  Cisplatin

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

  DT Modulation1

Cisplatin co-treated with jinfukang results in increased expression of KCNJ11 mRNA [16]

Regulation Mechanism

Transcription Factor Info

  Diazoxide

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

  DT Modulation1

Diazoxide results in decreased expression of KCNJ11 mRNA [17]

Regulation Mechanism

Transcription Factor Info

  ethyl-p-hydroxybenzoate

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

  DT Modulation1

ethyl-p-hydroxybenzoate results in decreased expression of KCNJ11 mRNA [18]

Regulation Mechanism

Transcription Factor Info

  Gliclazide

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

  DT Modulation1

KCNJ11 mutant form co-treated with ABCC8 mutant form results in increased susceptibility to Gliclazide [15]

Regulation Mechanism

Transcription Factor Info

  glimepiride

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

  DT Modulation1

KCNJ11 mutant form co-treated with ABCC8 mutant form results in decreased susceptibility to glimepiride [15]

Regulation Mechanism

Transcription Factor Info

  Lovastatin

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

  DT Modulation1

Lovastatin results in increased expression of KCNJ11 mRNA [19]

Regulation Mechanism

Transcription Factor Info

  Manganese

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

  DT Modulation1

manganese chloride results in increased abundance of Manganese which results in decreased expression of KCNJ11 protein [20]

Regulation Mechanism

Transcription Factor Info

  manganese chloride

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

  DT Modulation1

manganese chloride results in increased abundance of Manganese which results in decreased expression of KCNJ11 protein [20]

Regulation Mechanism

Transcription Factor Info

  mitiglinide

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

  DT Modulation1

KCNJ11 mutant form co-treated with ABCC8 mutant form results in increased susceptibility to mitiglinide [15]

Regulation Mechanism

Transcription Factor Info

  Silicon Dioxide

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

  DT Modulation1

Silicon Dioxide analog results in decreased expression of KCNJ11 mRNA [21]

Regulation Mechanism

Transcription Factor Info

  Valproic Acid

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

  DT Modulation1

Valproic Acid results in increased methylation of KCNJ11 gene [22]

Regulation Mechanism

Transcription Factor Info

Approved Drug

  Glyburide

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

  DT Modulation1

Glibenclamide inhibits the activity of KCNJ11 [1]

Cell System

Chinese hamster ovary (CHO) cells-KCNJ11

  Tolbutamide

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

  DT Modulation1

Tolbutamide inhibits the activity of KCNJ11 [2]

  Folic Acid

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

  DT Modulation1

Folic Acid inhibits the expression of KCNJ11 [3]

  Acetaminophen

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

  DT Modulation1

Acetaminophen inhibits the expression of KCNJ11 [4]

  Sunitinib

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

  DT Modulation1

Sunitinib increases the expression of KCNJ11 [6]

Drug Marketed but not Approved by US FDA

  Rotenone

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

  DT Modulation1

Rotenone increases the expression of KCNJ11 [5]

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 KCNJ11 [9]

Drug in Phase 2 Trial

  Bisphenol A

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

  DT Modulation1

Bisphenol A inhibits the expression of KCNJ11 [10]

Drug in Preclinical Test

  (+)-JQ1

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

  DT Modulation1

(+)-JQ1 inhibits the expression of KCNJ11 [8]

Investigative Drug

  HBR-985

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

  DT Modulation1

HBR-985 inhibits the activity of KCNJ11 [1]

Cell System

Chinese hamster ovary (CHO) cells-KCNJ11

  HMR1883

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

  DT Modulation1

HMR1883 inhibits the activity of KCNJ11 [1]

Cell System

Chinese hamster ovary (CHO) cells-KCNJ11

Acute Toxic Substance

  Acrylamide

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

  DT Modulation1

Acrylamide inhibits the expression of KCNJ11 [11]

Health and Environmental Toxicant

  1-methyl-4-phenylpyridinium

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

  DT Modulation1

1-methyl-4-phenylpyridinium increases the expression of KCNJ11 [7]
References
1 Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98.
2 Increased ATPase activity produced by mutations at arginine-1380 in nucleotide-binding domain 2 of ABCC8 causes neonatal diabetes. Proc Natl Acad Sci U S A. 2007 Nov 27;104(48):18988-92.
3 Folic acid supplementation dysregulates gene expression in lymphoblastoid cells--implications in nutrition. Biochem Biophys Res Commun. 2011 Sep 9;412(4):688-92.
4 Predictive toxicology using systemic biology and liver microfluidic "on chip" approaches: application to acetaminophen injury. Toxicol Appl Pharmacol. 2012 Mar 15;259(3):270-80.
5 Toxicity, recovery, and resilience in a 3D dopaminergic neuronal in vitro model exposed to rotenone. Arch Toxicol. 2018 Aug;92(8):2587-2606.
6 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.
7 ATP-sensitive potassium channel opener iptakalim protected against the cytotoxicity of MPP+ on SH-SY5Y cells by decreasing extracellular glutamate level. J Neurochem. 2005 Sep;94(6):1570-9.
8 Loss of TRIM33 causes resistance to BET bromodomain inhibitors through MYC- and TGF-beta-dependent mechanisms. Proc Natl Acad Sci U S A. 2016 Aug 2;113(31):E4558-66.
9 Transcriptome and DNA Methylome Dynamics during Triclosan-Induced Cardiomyocyte Differentiation Toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
10 Comparison of transcriptome expression alterations by chronic exposure to low-dose bisphenol A in different subtypes of breast cancer cells. Toxicol Appl Pharmacol. 2019 Dec 15;385:114814.
11 Acrylamide exposure represses neuronal differentiation, induces cell apoptosis and promotes tau hyperphosphorylation in hESC-derived 3D cerebral organoids. Food Chem Toxicol. 2020 Oct;144:111643.
12 Integration of transcriptomics, proteomics and metabolomics data to reveal the biological mechanisms of abrin injury in human lung epithelial cells. Toxicol Lett. 2019;312:1-10.
13 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
14 Screening of Relevant Metabolism-Disrupting Chemicals on Pancreatic-Cells: Evaluation of Murine and Human In Vitro Models. Int J Mol Sci. 2022;23(8).
15 Pharmacogenomic analysis of ATP-sensitive potassium channels coexpressing the common type 2 diabetes risk variants E23K and S1369A. Pharmacogenet Genomics. 2012;22(3):206-14.
16 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
17 Combined contributions of over-secreted glucagon-like peptide 1 and suppressed insulin secretion to hyperglycemia induced by gatifloxacin in rats. Toxicol Appl Pharmacol. 2013;266(3):375-84.
18 Risk assessment of parabens in a transcriptomics-based in vitro test. Chem Biol Interact. 2023;384:110699.
19 Lovastatin impairs cellular proliferation and enhances hyaluronic acid production in fibroblast-like synoviocytes. Toxicol In Vitro. 2024;97:105806.
20 Manganese induced nervous injury by a-synuclein accumulation via ATP-sensitive K(+) channels and GABA receptors. Toxicol Lett. 2020;332:164-170.
21 High-throughput, quantitative assessment of the effects of low-dose silica nanoparticles on lung cells: grasping complex toxicity with a great depth of field. BMC Genomics. 2015;16(1):315.
22 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.

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