Detail Information of Exogenous Modulation

General Information of Drug Transporter (DT)
DT ID DTD0544 Transporter Info
Gene Name KCNA5
Transporter Name Voltage-gated potassium channel subunit Kv1.5
Gene ID
3741
UniProt ID
P22460
Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)

Chemical Compound

  DT Modulation1

 Ketoconazole results in decreased activity of KCNA5 protein [2]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Bepridil results in decreased activity of KCNA5 protein [3]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Progesterone results in decreased activity of KCNA5 protein [5]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 KCNA5 protein results in increased susceptibility to Cisplatin [19]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Eugenol results in decreased activity of KCNA5 protein [11]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Rotenone inhibits the reaction Acrolein results in increased expression of KCNA5 mRNA [13]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 Rotenone inhibits the reaction Acrolein results in increased expression of KCNA5 protein [13]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of KCNA5 mRNA [17]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Terfenadine results in decreased activity of KCNA5 protein [24]

Regulation Mechanism

 Transcription Factor Info

  4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide

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

  DT Modulation1

 NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of KCNA5 mRNA [17]

Regulation Mechanism

 Transcription Factor Info

  Benzo(a)pyrene

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

  DT Modulation1

 Benzo(a)pyrene affects the methylation of KCNA5 exon [18]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 Benzo(a)pyrene results in decreased methylation of KCNA5 promoter [18]

Regulation Mechanism

 Transcription Factor Info

  diallyl trisulfide

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

  DT Modulation1

 diallyl trisulfide results in decreased activity of KCNA5 protein [20]

Regulation Mechanism

 Transcription Factor Info

  dorsomorphin

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

  DT Modulation1

 NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of KCNA5 mRNA [17]

Regulation Mechanism

 Transcription Factor Info

  Doxorubicin

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

  DT Modulation1

 KCNA5 protein results in increased susceptibility to Doxorubicin [19]

Regulation Mechanism

 Transcription Factor Info

  ebastine

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

  DT Modulation1

 ebastine results in decreased activity of KCNA5 protein [1]

Regulation Mechanism

 Transcription Factor Info

  Fluorouracil

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

  DT Modulation1

 KCNA5 protein results in increased susceptibility to Fluorouracil [19]

Regulation Mechanism

 Transcription Factor Info

  Fonofos

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

  DT Modulation1

 Fonofos results in increased methylation of KCNA5 promoter [21]

Regulation Mechanism

 Transcription Factor Info

  Parathion

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

  DT Modulation1

 Parathion results in increased methylation of KCNA5 promoter [21]

Regulation Mechanism

 Transcription Factor Info

  Pergolide

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

  DT Modulation1

 Pergolide results in decreased activity of KCNA5 protein [22]

Regulation Mechanism

 Transcription Factor Info

  Potassium

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

  DT Modulation1

 KCNA5 protein results in increased transport of Potassium [19]

Regulation Mechanism

 Transcription Factor Info

  Rotenone

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

  DT Modulation1

 Rotenone inhibits the reaction Acrolein results in increased expression of KCNA5 mRNA [13]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 Rotenone inhibits the reaction Acrolein results in increased expression of KCNA5 protein [13]

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 KCNA5 mRNA [23]

Regulation Mechanism

 Transcription Factor Info

  terbufos

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

  DT Modulation1

 terbufos results in increased methylation of KCNA5 promoter [21]

Regulation Mechanism

 Transcription Factor Info

  trichostatin A

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

  DT Modulation1

 trichostatin A results in decreased expression of KCNA5 mRNA [14]

Regulation Mechanism

 Transcription Factor Info

  vernakalant

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

  DT Modulation1

 vernakalant binds to and results in decreased activity of KCNA5 protein [25]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation2

 vernakalant binds to KCNA5 protein [26]

Regulation Mechanism

 Transcription Factor Info

  Vincristine

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

  DT Modulation1

 KCNA5 protein results in increased susceptibility to Vincristine [19]

Regulation Mechanism

 Transcription Factor Info

Approved Drug

  Ketoconazole

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

  DT Modulation1

 Ketoconazole inhibits the activity of KCNA5 [2]

  Bepridil

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

  DT Modulation1

 Bepridil inhibits the activity of KCNA5 [3]

  Tamoxifen

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

  DT Modulation1

 Tamoxifen inhibits the expression of KCNA5 [4]

  Progesterone

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

  DT Modulation1

 Progesterone inhibits the activity of KCNA5 [5]

  Cisplatin

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

  DT Modulation1

 Cisplatin affects the expression of KCNA5 [6]

  Decitabine

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

  DT Modulation1

 Decitabine affects the expression of KCNA5 [6]

  Carbamazepine

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

  DT Modulation1

 Carbamazepine affects the expression of KCNA5 [7]

  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 KCNA5 [7]

  Sunitinib

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

  DT Modulation1

 Sunitinib increases the expression of KCNA5 [8]

  Tretinoin

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

  DT Modulation1

 Tretinoin increases the expression of KCNA5 [9]

  Propafenone

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

  DT Modulation1

 Propafenone inhibits the activity of KCNA5 [10]

Drug Marketed but not Approved by US FDA

  Ebastine

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

  DT Modulation1

 Ebastine inhibits the activity of KCNA5 [1]

Drug in Phase 1 Trial

  Trichostatin A

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

  DT Modulation1

 Trichostatin A inhibits the expression of KCNA5 [14]

Investigative Drug

  Phenylmercuric Acetate

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

  DT Modulation1

 Phenylmercuric Acetate inhibits the expression of KCNA5 [15]

Patented Pharmaceutical Agent

  Eugenol

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

  DT Modulation1

 Eugenol inhibits the activity of KCNA5 [11]

Drug Withdrawn

  Terfenadine

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

  DT Modulation1

 Terfenadine inhibits the activity of KCNA5 [1]

Environmental toxicant

  Zinc

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

  DT Modulation1

 Zinc inhibits the expression of KCNA5 [12]

Acute Toxic Substance

  Acrolein

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

  DT Modulation1

 Acrolein increases the expression of KCNA5 [13]

Health and Environmental Toxicant

  Diethylhexyl Phthalate

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

  DT Modulation1

 Diethylhexyl Phthalate inhibits the expression of KCNA5 [16]
References
1 Comparative effects of nonsedating histamine H1 receptor antagonists, ebastine and terfenadine, on human Kv1.5 channels. Eur J Pharmacol. 1997 May 20;326(2-3):257-63.
2 Blockade of HERG and Kv1.5 by ketoconazole. J Pharmacol Exp Ther. 1998 Aug;286(2):727-35.
3 Inhibitory effect of bepridil on hKv1.5 channel current: comparison with amiodarone and E-4031. Eur J Pharmacol. 2001 Nov 2;430(2-3):149-57.
4 Gene expression changes induced by estrogen and selective estrogen receptor modulators in primary-cultured human endometrial cells: signals that distinguish the human carcinogen tamoxifen. Toxicology. 2005 Jan 5;206(1):91-109.
5 Differential effects of estrogen and progesterone on potassium channels expressed in Xenopus oocytes. Steroids. 2008 Mar;73(3):272-9.
6 Acute hypersensitivity of pluripotent testicular cancer-derived embryonal carcinoma to low-dose 5-aza deoxycytidine is associated with global DNA Damage-associated p53 activation, anti-pluripotency and DNA demethylation. PLoS One. 2012;7(12):e53003.
7 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.
8 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.
9 Atrial-like Engineered Heart Tissue: An In Vitro Model of the Human Atrium. Stem Cell Reports. 2018 Dec 11;11(6):1378-1390.
10 Optimization of propafenone analogues as antimalarial leads. J Med Chem. 2011 Nov 10;54(21):7477-85.
11 Eugenol inhibits K+ currents in trigeminal ganglion neurons. J Dent Res. 2007 Sep;86(9):898-902.
12 Zinc deficiency alters DNA damage response genes in normal human prostate epithelial cells. J Nutr. 2008 Apr;138(4):667-73.
13 Mitochondrial ROS-K+ channel signaling pathway regulated secretion of human pulmonary artery endothelial cells. Free Radic Res. 2012 Dec;46(12):1437-45.
14 From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
15 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
16 Di-(2-ethylhexyl)-phthalate induces apoptosis via the PPAR Gamma/PTEN/AKT pathway in differentiated human embryonic stem cells. Food Chem Toxicol. 2019 Sep;131:110552.
17 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.
18 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
19 Detection of potassium currents and regulation of multidrug resistance by potassium channels in human gastric cancer cells. Cell Biol Int. 2007;31(7):741-7.
20 Allitridi inhibits multiple cardiac potassium channels expressed in HEK 293 cells. PLoS One. 2012;7(12):e51550.
21 DNA methylation alterations in response to pesticide exposure in vitro. Environ Mol Mutagen. 2012;53(7):542-9.
22 Pergolide is an inhibitor of voltage-gated potassium channels, including Kv1.5, and causes pulmonary vasoconstriction. Circulation. 2005;112(10):1494-9.
23 Supplementation of healthy volunteers with nutritionally relevant amounts of selenium increases the expression of lymphocyte protein biosynthesis genes. Am J Clin Nutr. 2008;87(1):181-9.
24 HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine. Circulation. 1996;94(4):817-23.
25 The molecular basis of high-affinity binding of the antiarrhythmic compound vernakalant (RSD1235) to Kv1.5 channels. Mol Pharmacol. 2007;72(6):1522-34.
26 Modeling of high-affinity binding of the novel atrial anti-arrhythmic agent, vernakalant, to Kv1.5 channels. J Mol Graph Model. 2009;28(3):226-35.

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