Detail Information of Exogenous Modulation

General Information of Drug Transporter (DT)
DT ID DTD0422 Transporter Info
Gene Name SLC5A2
Transporter Name Sodium/glucose cotransporter 2
Gene ID
6524
UniProt ID
P31639
Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)

Chemical Compound

  DT Modulation1

 Canagliflozin results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  DT Modulation1

 Cisplatin co-treated with jinfukang results in decreased expression of SLC5A2 mRNA [10]

Regulation Mechanism

 Transcription Factor Info

  aristolochic acid I

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

  DT Modulation1

 aristolochic acid I results in increased expression of SLC5A2 mRNA [20]

Regulation Mechanism

 Transcription Factor Info

  Benzo(a)pyrene

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

  DT Modulation1

 Benzo(a)pyrene affects the methylation of SLC5A2 exon [21]

Regulation Mechanism

 Transcription Factor Info

  bexagliflozin

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

  DT Modulation1

 bexagliflozin results in decreased activity of SLC5A2 protein [22]

Regulation Mechanism

 Transcription Factor Info

  CGP 52608

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

  DT Modulation1

 CGP 52608 promotes the reaction RORA protein binds to SLC5A2 gene [23]

Regulation Mechanism

 Transcription Factor Info

  dapagliflozin

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

  DT Modulation1

 dapagliflozin results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  ertugliflozin

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

  DT Modulation1

 ertugliflozin results in decreased activity of SLC5A2 protein [24]

Regulation Mechanism

 Transcription Factor Info

  methyleugenol

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

  DT Modulation1

 methyleugenol results in decreased expression of SLC5A2 mRNA [18]

Regulation Mechanism

 Transcription Factor Info

  N-Nitrosopyrrolidine

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

  DT Modulation1

 N-Nitrosopyrrolidine results in decreased expression of SLC5A2 mRNA [18]

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 SLC5A2 mRNA [25]

Regulation Mechanism

 Transcription Factor Info

  Phlorhizin

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

  DT Modulation1

 Phlorhizin results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  remogliflozin etabonate

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

  DT Modulation1

 remogliflozin etabonate results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  sergliflozin

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

  DT Modulation1

 sergliflozin results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  sodium arsenite

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

  DT Modulation1

 sodium arsenite results in increased expression of SLC5A2 mRNA [27]

Regulation Mechanism

 Transcription Factor Info

  T 1095

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

  DT Modulation1

 T 1095 results in decreased activity of SLC5A2 protein [9]

Regulation Mechanism

 Transcription Factor Info

  Tetrachlorodibenzodioxin

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

  DT Modulation1

 Tetrachlorodibenzodioxin affects the expression of SLC5A2 mRNA [17]

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 SLC5A2 gene [28]

Regulation Mechanism

 Transcription Factor Info

Approved Drug

  Dapagliflozin

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

  DT Modulation1

 Dapagliflozin inhibits the transportation of Methyl-alpha-D-glucopyranoside by SLC5A2 [5]

Affected Drug/Substrate

 Methyl-alpha-D-glucopyranoside Modulation Type Inhibition

  DT Modulation2

 Dapagliflozin inhibits the activity of SLC5A2 [6]

Cell System

 Chinese hamster ovary (CHO) cells-SGLT2

  Canagliflozin

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

  DT Modulation1

 Canagliflozin inhibits the activity of SLC5A2 [9]

  Cisplatin

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

  DT Modulation1

 Cisplatin inhibits the expression of SLC5A2 [10]

  Urethane

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

  DT Modulation1

 Urethane inhibits the expression of SLC5A2 [11]

  Cannabidiol

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

  DT Modulation1

 Cannabidiol increases the expression of SLC5A2 [12]

  Pioglitazone

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

  DT Modulation1

 Pioglitazone inhibits the activity of SLC5A2 [13]

  Ertugliflozin

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

  DT Modulation1

 Ertugliflozin inhibits the activity of SLC5A2 [14]

  Troglitazone

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

  DT Modulation1

 Troglitazone induces the activity of SLC5A2 [15]

Drug in Phase 3 Trial

  Bexagliflozin

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

  DT Modulation1

 Bexagliflozin inhibits the activity of SLC5A2 [19]

Drug in Phase 1 Trial

  Remogliflozin etabonate

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

  DT Modulation1

 Remogliflozin etabonate inhibits the activity of SLC5A2 [9]

Investigative Drug

  Phlorizin

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

  DT Modulation1

 Phlorizin inhibits the transportation of 2-Deoxyglucose by SLC5A2 [1]

Affected Drug/Substrate

 2-Deoxyglucose Modulation Type Inhibition

Cell System

 Human embryonic kidney 293 cells (HEK293)-SGLT2

  DT Modulation2

 Phlorizin inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [2]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  DT Modulation3

 Phlorizin inhibits the transportation of D-glucose by SLC5A2 [3]

Affected Drug/Substrate

 D-glucose Modulation Type Inhibition

  Formononetin

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

  DT Modulation1

 Formononetin inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  DT Modulation2

 Formononetin inhibits the activity of SLC5A2 [4]

  Sophoraflavanone G

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

  DT Modulation1

 Sophoraflavanone G inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  DT Modulation2

 Sophoraflavanone G inhibits the activity of SLC5A2 [4]

  Sergliflozin A

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

  DT Modulation1

 Sergliflozin A inhibits the transportation of D-glucose by SLC5A2 [3]

Affected Drug/Substrate

 D-glucose Modulation Type Inhibition

  DT Modulation2

 Sergliflozin A inhibits the activity of SLC5A2 [7]

  Alstiphyllanine D

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

  DT Modulation1

 Alstiphyllanine D inhibits the transportation of Alpha-D-glucopyranoside by SLC5A2 [8]

Affected Drug/Substrate

 Alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Alstiphyllanine E

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

  DT Modulation1

 Alstiphyllanine E inhibits the transportation of Alpha-D-glucopyranoside by SLC5A2 [8]

Affected Drug/Substrate

 Alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Alstiphyllanine F

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

  DT Modulation1

 Alstiphyllanine F inhibits the transportation of Alpha-D-glucopyranoside by SLC5A2 [8]

Affected Drug/Substrate

 Alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Kuraidin

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

  DT Modulation1

 Kuraidin inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Kurarinone

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

  DT Modulation1

 Kurarinone inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Kushenol N

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

  DT Modulation1

 Kushenol N inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Maackiain

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

  DT Modulation1

 Maackiain inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [4]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Acerogenin A

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

  DT Modulation1

 Acerogenin A inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [2]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Acerogenin B

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

  DT Modulation1

 Acerogenin B inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [2]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

  Acerogenin C

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

  DT Modulation1

 Acerogenin C inhibits the transportation of methyl-alpha-D-glucopyranoside by SLC5A2 [2]

Affected Drug/Substrate

 methyl-alpha-D-glucopyranoside Modulation Type Inhibition

Cell System

 Monkey kidney tissue Fibroblast-like cell lines (COS)1-SGLT2

Natural Product

  Methyleugenol

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

  DT Modulation1

 Methyleugenol inhibits the expression of SLC5A2 [18]

  Resveratrol

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

  DT Modulation1

 Plant Extracts co-treated with Resveratrol results in decreased expression of SLC5A2 mRNA [26]

Regulation Mechanism

 Transcription Factor Info

Traditional Medicine

  Jinfukang

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

  DT Modulation1

 Jinfukang inhibits the expression of SLC5A2 [10]

Environmental toxicant

  Polychlorinated dibenzodioxin

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

  DT Modulation1

 Polychlorinated dibenzodioxin affects the expression of SLC5A2 [17]

Herbicide

  Atrazine

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

  DT Modulation1

 Atrazine increases the expression of SLC5A2 [16]
References
1 Targeting Type 2 Diabetes with C-Glucosyl Dihydrochalcones as Selective Sodium Glucose Co-Transporter 2 (SGLT2) Inhibitors: Synthesis and Biological Evaluation. J Med Chem. 2017 Jan 26;60(2):568-579.
2 Cyclic diarylheptanoids as Na+-glucose cotransporter (SGLT) inhibitors from Acer nikoense. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1070-4.
3 Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2. J Med Chem. 2009 Apr 9;52(7):1785-94.
4 Na+-glucose cotransporter (SGLT) inhibitory flavonoids from the roots of Sophora flavescens. Bioorg Med Chem. 2007 May 15;15(10):3445-9.
5 O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5632-5.
6 Synthesis and biological evaluation of novel tetrahydroisoquinoline-C-aryl glucosides as SGLT2 inhibitors for the treatment of type 2 diabetes. Eur J Med Chem. 2016 May 23;114:89-100.
7 Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners. Bioorg Med Chem. 2010 Mar 15;18(6):2178-94.
8 Alstiphyllanines E-H, picraline and ajmaline-type alkaloids from Alstonia macrophylla inhibiting sodium glucose cotransporter. Bioorg Med Chem. 2010 Mar 15;18(6):2152-2158.
9 Discovery of novel N-beta-D-xylosylindole derivatives as sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the management of hyperglycemia in diabetes. J Med Chem. 2011 Jan 13;54(1):166-78.
10 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
11 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
12 Cannabidiol induces antioxidant pathways in keratinocytes by targeting BACH1. Redox Biol. 2020 Jan;28:101321.
13 Insulin and glucose-lowering agents for treating people with diabetes and chronic kidney disease. Cochrane Database Syst Rev. 2018 Sep 24;9:CD011798.
14 Spotlight on ertugliflozin and its potential in the treatment of type 2 diabetes: evidence to date. Drug Des Devel Ther. 2017 Oct 3;11:2905-2919.
15 The effect of PPAR agonist on SGLT2 and glucagon expressions in alpha cells under hyperglycemia. J Endocrinol Invest. 2017 Oct;40(10):1069-1076.
16 Endoplasmic reticulum stress impairs insulin signaling through mitochondrial damage in SH-SY5Y cells. Neurosignals. 2012;20(4):265-80.
17 Identification of novel low-dose bisphenol a targets in human foreskin fibroblast cells derived from hypospadias patients. PLoS One. 2012;7(5):e36711.
18 Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297.
19 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
20 Integration of transcriptomic, proteomic and metabolomic data to reveal the biological mechanisms of AAI injury in renal epithelial cells. Toxicol In Vitro. 2021;70:105054.
21 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
22 EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011;63(4):284-93.
23 Identification of potential target genes of ROR-alpha in THP1 and HUVEC cell lines. Exp Cell Res. 2017;353(1):6-15.
24 Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011;54(8):2952-60.
25 A multi-omics approach to elucidate okadaic acid-induced changes in human HepaRG hepatocarcinoma cells. Arch Toxicol. 2024;98(9):2919-2935.
26 One-year supplementation with a grape extract containing resveratrol modulates inflammatory-related microRNAs and cytokines expression in peripheral blood mononuclear cells of type 2 diabetes and hypertensive patients with coronary artery disease. Pharmacol Res. 2013;72:69-82.
27 High-Throughput Transcriptomics of Nontumorigenic Breast Cells Exposed to Environmentally Relevant Chemicals. Environ Health Perspect. 2024;132(4):47002.
28 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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