General Information of Drug Transporter (DT)
DT ID DTD0021 Transporter Info
Gene Name SLC15A1
Transporter Name Peptide transporter 1
Gene ID
6564
UniProt ID
P46059
Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)

Chemical Compound

  DT Modulation1

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of Ceftibuten [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of Cephradine [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Fosinopril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Fluvastatin results in decreased activity of SLC15A1 protein [18]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Fluorouracil results in decreased activity of SLC15A1 protein [19]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Quinapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Zinc inhibits the reaction JBP 485 binds to SLC15A1 protein [50]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Zinc inhibits the reaction JBP 485 binds to SLC15A1 protein which results in decreased uptake of JBP 485 [50]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Zinc results in decreased activity of SLC15A1 protein [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation4

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of Ceftibuten [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation5

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of Cephradine [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation6

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of glycylsarcosine [33]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Aspartame results in decreased activity of SLC15A1 protein [18]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

AICA ribonucleotide results in decreased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  DT Modulation1

Benzo(a)pyrene results in increased methylation of SLC15A1 exon [43]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Benzo(a)pyrene results in increased methylation of SLC15A1 promoter [43]

Regulation Mechanism

Transcription Factor Info

  2-amino-3,8-dimethylimidazo(4,5-f)quinoxaline

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

  DT Modulation1

2-amino-3,8-dimethylimidazo(4,5-f)quinoxaline results in decreased expression of SLC15A1 mRNA [35]

Regulation Mechanism

Transcription Factor Info

  benazepril

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

  DT Modulation1

benazepril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  benzo(e)pyrene

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

  DT Modulation1

benzo(e)pyrene results in increased methylation of SLC15A1 intron [44]

Regulation Mechanism

Transcription Factor Info

  Benzoic Acid

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

  DT Modulation1

Benzoic Acid analog binds to SLC15A1 protein [45]

Regulation Mechanism

Transcription Factor Info

  Cilazapril

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

  DT Modulation1

Cilazapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  Estradiol

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

  DT Modulation1

Estradiol co-treated with Progesterone results in decreased expression of SLC15A1 mRNA [46]

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 SLC15A1 promoter [47]

Regulation Mechanism

Transcription Factor Info

  glycylsarcosine

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

  DT Modulation1

benazepril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Cilazapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Fosinopril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation4

glycylsarcosine inhibits the reaction SLC15A1 protein results in increased transport of Lisdexamfetamine Dimesylate [48]

Regulation Mechanism

Transcription Factor Info

  DT Modulation5

glycylsarcosine results in decreased activity of SLC15A1 protein [48]

Regulation Mechanism

Transcription Factor Info

  DT Modulation6

moexipril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation7

Perindopril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation8

quinaprilat inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation9

Quinapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation10

Ramipril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation11

SLC15A1 protein results in increased transport of glycylsarcosine [49]

Regulation Mechanism

Transcription Factor Info

  DT Modulation12

SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation13

spirapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation14

trandolapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  DT Modulation15

Valganciclovir inhibits the reaction SLC15A1 protein results in increased transport of glycylsarcosine [49]

Regulation Mechanism

Transcription Factor Info

  DT Modulation16

Zinc results in decreased activity of SLC15A1 protein which results in decreased uptake of glycylsarcosine [33]

Regulation Mechanism

Transcription Factor Info

  JBP 485

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

  DT Modulation1

JBP 485 binds to and results in decreased activity of SLC15A1 protein [50]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Zinc inhibits the reaction JBP 485 binds to SLC15A1 protein [50]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Zinc inhibits the reaction JBP 485 binds to SLC15A1 protein which results in decreased uptake of JBP 485 [50]

Regulation Mechanism

Transcription Factor Info

  Lactic Acid

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

  DT Modulation1

Lactic Acid results in decreased expression of SLC15A1 mRNA [36]

Regulation Mechanism

Transcription Factor Info

  Lisdexamfetamine Dimesylate

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

  DT Modulation1

glycylsarcosine inhibits the reaction SLC15A1 protein results in increased transport of Lisdexamfetamine Dimesylate [48]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

SLC15A1 protein results in increased transport of Lisdexamfetamine Dimesylate [48]

Regulation Mechanism

Transcription Factor Info

  Methapyrilene

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

  DT Modulation1

Methapyrilene results in increased methylation of SLC15A1 intron [44]

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 SLC15A1 mRNA [37]

Regulation Mechanism

Transcription Factor Info

  mifobate

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

  DT Modulation1

mifobate inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  moexipril

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

  DT Modulation1

moexipril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

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 SLC15A1 mRNA [37]

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 SLC15A1 mRNA [51]

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 SLC15A1 promoter [47]

Regulation Mechanism

Transcription Factor Info

  Perindopril

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

  DT Modulation1

Perindopril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  phenylalanylserine

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

  DT Modulation1

phenylalanylserine analog binds to SLC15A1 protein [45]

Regulation Mechanism

Transcription Factor Info

  pirinixic acid

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

  DT Modulation1

pirinixic acid binds to and results in increased activity of PPARA protein which results in decreased expression of SLC15A1 mRNA [52]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

pirinixic acid results in increased expression of SLC15A1 mRNA [34]

Regulation Mechanism

Transcription Factor Info

  Progesterone

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

  DT Modulation1

Estradiol co-treated with Progesterone results in decreased expression of SLC15A1 mRNA [46]

Regulation Mechanism

Transcription Factor Info

  quinaprilat

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

  DT Modulation1

quinaprilat inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  Ramipril

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

  DT Modulation1

Ramipril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  repaglinide

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

  DT Modulation1

repaglinide results in decreased activity of SLC15A1 protein [18]

Regulation Mechanism

Transcription Factor Info

  Rosiglitazone

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

  DT Modulation1

Metformin inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

mifobate inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  DT Modulation4

Sirolimus inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  Sirolimus

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

  DT Modulation1

Sirolimus inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  spirapril

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

  DT Modulation1

spirapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

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 SLC15A1 promoter [47]

Regulation Mechanism

Transcription Factor Info

  trandolapril

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

  DT Modulation1

trandolapril inhibits the reaction SLC15A1 protein results in increased uptake of glycylsarcosine [42]

Regulation Mechanism

Transcription Factor Info

  Triiodothyronine

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

  DT Modulation1

Resveratrol inhibits the reaction Triiodothyronine results in decreased expression of SLC15A1 mRNA [25]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Resveratrol inhibits the reaction Triiodothyronine results in decreased expression of SLC15A1 protein [25]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Triiodothyronine results in decreased expression of SLC15A1 mRNA [25]

Regulation Mechanism

Transcription Factor Info

  DT Modulation4

Triiodothyronine results in decreased expression of SLC15A1 protein [25]

Regulation Mechanism

Transcription Factor Info

  Valganciclovir

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

  DT Modulation1

SLC15A1 protein results in increased transport of Valganciclovir [49]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Valganciclovir inhibits the reaction SLC15A1 protein results in increased transport of glycylsarcosine [49]

Regulation Mechanism

Transcription Factor Info

  Vanadium

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

  DT Modulation1

Vanadium results in decreased expression of SLC15A1 mRNA [53]

Regulation Mechanism

Transcription Factor Info

Approved Drug

  Valacyclovir

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

  DT Modulation1

Valacyclovir inhibits the transportation of Cefadroxil by SLC15A1 (Ki = 910 microM) [1]

Affected Drug/Substrate

Cefadroxil Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  DT Modulation2

Valacyclovir inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 1280 microM) [1]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  DT Modulation3

Valacyclovir inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 4080 microM) [3]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Oocytes-PEPT1

  DT Modulation4

Valacyclovir inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 400 microM) [6]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  Cefixime

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

  DT Modulation1

Cefixime inhibits the transportation of Cefadroxil by SLC15A1 (Ki = 1310 microM) [2]

Affected Drug/Substrate

Cefadroxil Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cefixime inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 10000 microM) [5]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation3

Cefixime inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 12000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation4

Cefixime inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cyclacillin

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

  DT Modulation1

Cyclacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 600 microM) [4]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cyclacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 350 microM) [4]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  DT Modulation3

Cyclacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 500 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation4

Cyclacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Ceftibuten

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

  DT Modulation1

Ceftibuten inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 870 microM) [5]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Ceftibuten inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 710 microM) [5]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  DT Modulation3

Ceftibuten inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 340 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation4

Ceftibuten inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Ampicillin

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

  DT Modulation1

Ampicillin inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 10000 microM) [9]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  DT Modulation2

Ampicillin inhibits the transportation of Valacyclovir by SLC15A1 [1]

Affected Drug/Substrate

Valacyclovir Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  DT Modulation3

Ampicillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefuroxime

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

  DT Modulation1

Cefuroxime inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 26000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cefuroxime inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki > 5000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation3

Cefuroxime inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Losartan

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

  DT Modulation1

Losartan inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 52 microM) [10]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  DT Modulation2

Losartan inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 24 microM) [10]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Valsartan

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

  DT Modulation1

Valsartan inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 560 microM) [10]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  DT Modulation2

Valsartan inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 390 microM) [10]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefamandole

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

  DT Modulation1

Cefamandole inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 8100 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cefamandole inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefmetazole

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

  DT Modulation1

Cefmetazole inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 28000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cefmetazole inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cephapirin

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

  DT Modulation1

Cephapirin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki > 10000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cephapirin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cephradine

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

  DT Modulation1

Cephradine inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 9.8 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cephradine inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cloxacillin

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

  DT Modulation1

Cloxacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 3000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Cloxacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Dicloxacillin

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

  DT Modulation1

Dicloxacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 7200 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Dicloxacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Moxalactam

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

  DT Modulation1

Moxalactam inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 12300 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Moxalactam inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Oxacillin

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

  DT Modulation1

Oxacillin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 12000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Oxacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefadroxil

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

  DT Modulation1

Cefadroxil inhibits the transportation of Glycylsarcosine by SLC15A1 [11]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  DT Modulation2

Cefadroxil inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Irbesartan

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

  DT Modulation1

Irbesartan inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 230 microM) [10]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Levodopa

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

  DT Modulation1

Levodopa inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 141200 microM) [12]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  Methyldopa

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

  DT Modulation1

Methyldopa inhibits the transportation of Glycylsarcosine by SLC15A1 (IC50 = 151600 microM) [12]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Chinese hamster ovary (CHO) cells-PEPT1

  Fosinopril

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

  DT Modulation1

Fosinopril inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 35.5 microM) [13]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefsulodin

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

  DT Modulation1

Cefsulodin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki > 30000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Ceftazidime

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

  DT Modulation1

Ceftazidime inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki > 10000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Bestatin

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

  DT Modulation1

Bestatin inhibits the transporation of melatonin by SLC15A1 (IC50 = 1000 microM) [14]

Affected Drug/Substrate

Melatonin Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)

  Loracarbef

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

  DT Modulation1

Loracarbef inhibits the transportation of Cefadroxil by SLC15A1 [2]

Affected Drug/Substrate

Cefadroxil Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefdinir

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

  DT Modulation1

Cefdinir inhibits the transportation of Glycylsarcosine by SLC15A1 [5]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human cervical cancer cell line (Hela)-PEPT1

  Captopril

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

  DT Modulation1

Captopril inhibits the transportation of Sulpiride by SLC15A1 [15]

Affected Drug/Substrate

Sulpiride Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefaclor

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

  DT Modulation1

Cefaclor inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefazolin

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

  DT Modulation1

Cefazolin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefepime

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

  DT Modulation1

Cefepime inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefotaxime

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

  DT Modulation1

Cefotaxime inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefoxitin

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

  DT Modulation1

Cefoxitin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cefpodoxime

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

  DT Modulation1

Cefpodoxime inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Ceftriaxone

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

  DT Modulation1

Ceftriaxone inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cephalexin

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

  DT Modulation1

Cephalexin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Cephalothin

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

  DT Modulation1

Cephalothin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Floxacillin

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

  DT Modulation1

Flucloxacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Penicillin V

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

  DT Modulation1

Penicillin V inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Piperacillin

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

  DT Modulation1

Piperacillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Azathioprine

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

  DT Modulation1

Azathioprine inhibits the expression of SLC15A1 [16]

  Arsenic Trioxide

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

  DT Modulation1

Arsenic Trioxide inhibits the expression of SLC15A1 [17]

  Fluvastatin

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

  DT Modulation1

Fluvastatin inhibits the activity of SLC15A1 [18]

  Repaglinide

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

  DT Modulation1

Repaglinide inhibits the activity of SLC15A1 [18]

  Fluorouracil

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

  DT Modulation1

Fluorouracil inhibits the expression of SLC15A1 [19]

  Cyclosporine

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

  DT Modulation1

Cyclosporine inhibits the expression of SLC15A1 [20]

  Isotretinoin

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

  DT Modulation1

Isotretinoin inhibits the expression of SLC15A1 [21]

  Metformin

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

  DT Modulation1

Metformin increases the expression of SLC15A1 [22]

  DT Modulation2

Metformin inhibits the reaction Rosiglitazone results in increased expression of and results in increased activity of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  DT Modulation3

Metformin results in decreased activity of and results in decreased expression of SLC15A1 protein [22]

Regulation Mechanism

Transcription Factor Info

  Zoledronic Acid

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

  DT Modulation1

Zoledronic Acid increases the expression of SLC15A1 [23]

  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 SLC15A1 [24]

  Liothyronine

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

  DT Modulation1

Liothyronine inhibits the expression of SLC15A1 [25]

  Rifampin

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

  DT Modulation1

Rifampin inhibits the expression of SLC15A1 [26]

  Urethane

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

  DT Modulation1

Urethane inhibits the expression of SLC15A1 [27]

  Acetaminophen

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

  DT Modulation1

Acetaminophen inhibits the expression of SLC15A1 [28]

  Cisplatin

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

  DT Modulation1

Cisplatin induces the activity of SLC15A1 [19]

  Quinapril

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

  DT Modulation1

Quinapril inhibits the activity of SLC15A1 [29]

  Insulin

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

  DT Modulation1

Insulin induces the activity of SLC15A1 [30]

  Enalapril

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

  DT Modulation1

Enalapril inhibits the activity of SLC15A1 [31]

  Ibuprofen

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

  DT Modulation1

Ibuprofen analog binds to SLC15A1 protein [45]

Regulation Mechanism

Transcription Factor Info

Drug in Phase 3 Trial

  Benzylpenicillin

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

  DT Modulation1

Benzylpenicillin inhibits the transportation of Glycylsarcosine by SLC15A1 (Ki = 30000 microM) [7]

Affected Drug/Substrate

Glycylsarcosine Modulation Type Inhibition

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  DT Modulation2

Benzylpenicillin inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

  Resveratrol

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

  DT Modulation1

Resveratrol increases the expression of SLC15A1 [32]

Regulation Mechanism

via enhancement of Nuclear factor erythroid 2-related factor 2 (NFE2L2) Transcription Factor Info

Cell System

Human colon adenocarcinoma cells (Caco-2)

Drug in Phase 2 Trial

  MeIQx

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

  DT Modulation1

MeIQx inhibits the expression of SLC15A1 [35]

Drug in Phase 1 Trial

  Aspartame

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

  DT Modulation1

Aspartame inhibits the activity of SLC15A1 [18]

  AICA ribonucleotide

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

  DT Modulation1

AICA ribonucleotide inhibits the activity of SLC15A1 [22]

Discontinued Drug

  MDL-28170

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

  DT Modulation1

MDL-28170 inhibits the activity of SLC15A1 [8]

Cell System

Human enterocyte-like 2 cell (Caco-2)-PEPT1

Investigative Drug

  Milchsaure

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

  DT Modulation1

Milchsaure inhibits the expression of SLC15A1 [36]

  4-AMBA

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

  DT Modulation1

4-AMBA inhibits the activity of SLC15A1 [39], [40]

  [11C]GlySar

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

  DT Modulation1

[11C]GlySar modulates the activity of SLC15A1 [41]

  [14C]GlySar

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

  DT Modulation1

[14C]GlySar modulates the activity of SLC15A1 [41]

  [3H]GlySar

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

  DT Modulation1

[3H]GlySar modulates the activity of SLC15A1 [41]

Natural Product

  DT Modulation1

Resveratrol inhibits the reaction Triiodothyronine results in decreased expression of SLC15A1 mRNA [25]

Regulation Mechanism

Transcription Factor Info

  DT Modulation2

Resveratrol inhibits the reaction Triiodothyronine results in decreased expression of SLC15A1 protein [25]

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 inhibits the expression of SLC15A1 [37]

  Tobacco Smoke Pollution

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

  DT Modulation1

Tobacco Smoke Pollution affects the expression of SLC15A1 [38]

Environmental toxicant

  Zinc

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

  DT Modulation1

Zinc inhibits the activity of SLC15A1 [33]

Mycotoxins

  Aflatoxin B1

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

  DT Modulation1

Aflatoxin B1 affects the expression of SLC15A1 [20]

Carcinogen

  Benzo(a)pyrene

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

  DT Modulation1

Benzo(a)pyrene inhibits the expression of SLC15A1 [37]

Health and Environmental Toxicant

  Pirinixic acid

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

  DT Modulation1

Pirinixic acid increases the expression of SLC15A1 [34]
References
1 Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line. J Pharmacol Exp Ther. 1999 Apr;289(1):448-54.
2 Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells. J Pharmacol Exp Ther. 1996 May;277(2):831-9.
3 Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir. Biochem Biophys Res Commun. 1998 Sep 18;250(2):246-51.
4 Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2. J Biol Chem. 1995 Oct 27;270(43):25672-7.
5 Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2. Biochim Biophys Acta. 1997 Mar 13;1324(2):296-308.
6 5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter. Pharm Res. 1998 Aug;15(8):1154-9.
7 Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. Eur J Pharm Biopharm. 2005 Jan;59(1):17-24.
8 Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1. J Med Chem. 2005 Jun 30;48(13):4410-9.
9 Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells. Pharm Res. 1996 Nov;13(11):1631-4.
10 High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
11 Human intestinal H+/peptide cotransporter. Cloning, functional expression, and chromosomal localization. J Biol Chem. 1995 Mar 24;270(12):6456-63.
12 CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs. J Pharm Sci. 1999 Mar;88(3):347-50.
13 Mechanism of intestinal absorption and renal reabsorption of an orally active ace inhibitor: uptake and transport of fosinopril in cell cultures. Drug Metab Dispos. 2001 Oct;29(10):1307-15.
14 Human transporters, PEPT1/2, facilitate melatonin transportation into mitochondria of cancer cells: An implication of the therapeutic potential. J Pineal Res. 2017 May;62(4).
15 Studies on intestinal absorption of sulpiride (1): carrier-mediated uptake of sulpiride in the human intestinal cell line Caco-2. Biol Pharm Bull. 2002 Jul;25(7):885-90.
16 Severe villus atrophy and chronic malabsorption induced by azathioprine. Gastroenterology. 2003 Jun;124(7):1950-7.
17 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
18 In vitro and pharmacophore-based discovery of novel hPEPT1 inhibitors. Pharm Res. 2005 Apr;22(4):512-7.
19 Regulation of human peptide transporter 1 (PEPT1) in gastric cancer cells by anticancer drugs. Cancer Lett. 2005 Dec 8;230(1):72-80.
20 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
21 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
22 Rosiglitazone and metformin have opposite effects on intestinal absorption of oligopeptides via the proton-dependent PepT1 transporter. Mol Pharmacol. 2012 Mar;81(3):319-27.
23 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
24 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.
25 Enhancement effect of resveratrol on the intestinal absorption of bestatin by regulating PEPT1, MDR1 and MRP2 in vivo and in vitro. Int J Pharm. 2015 Nov 10;495(1):588-598.
26 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
27 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
28 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
29 Differential recognition of ACE inhibitors in Xenopus laevis oocytes expressing rat PEPT1 and PEPT2. Pharm Res. 2000 May;17(5):526-32.
30 Role of insulin on jejunal PepT1 expression and function regulation in diabetic male and female rats. Can J Physiol Pharmacol. 2010 Jul;88(7):753-9.
31 The apical uptake transporter of levofloxacin is distinct from the peptide transporter in human intestinal epithelial Caco-2 cells. Drug Metab Pharmacokinet. 2008;23(5):373-8.
32 Nrf2 regulates the expression of the peptide transporter PEPT1 in the human colon carcinoma cell line Caco-2. Biochim Biophys Acta. 2014 Jun;1840(6):1747-54.
33 Inhibitory effect of zinc on PEPT1-mediated transport of glycylsarcosine and beta-lactam antibiotics in human intestinal cell line Caco-2. Pharm Res. 2003 Sep;20(9):1389-93.
34 Induction of intestinal peptide transporter 1 expression during fasting is mediated via peroxisome proliferator-activated receptor alpha. Am J Physiol Gastrointest Liver Physiol. 2006 Nov;291(5):G851-6.
35 Preferential induction of the AhR gene battery in HepaRG cells after a single or repeated exposure to heterocyclic aromatic amines. Toxicol Appl Pharmacol. 2010 Nov 15;249(1):91-100.
36 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
37 Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297.
38 Integration of transcriptome analysis with pathophysiological endpoints to evaluate cigarette smoke toxicity in an in vitro human airway tissue model. Arch Toxicol. 2021 May;95(5):1739-1761.
39 Transport of the photodynamic therapy agent 5-aminolevulinic acid by distinct H+-coupled nutrient carriers coexpressed in the small intestine. J Pharmacol Exp Ther. 2010 Jan;332(1):220-8.
40 Activation of vagal afferents in the rat duodenum by protein digests requires PepT1. J Nutr. 2005 Jun;135(6):1491-5.
41 Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 984).
42 Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited. J Pharmacol Exp Ther. 2008 Nov;327(2):432-41.
43 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017;8(1):1369-1391.
44 Effect of aflatoxin B(1), benzo[a]pyrene, and methapyrilene on transcriptomic and epigenetic alterations in human liver HepaRG cells. Food Chem Toxicol. 2018;121:214-223.
45 Affinity and translocation relationships via hPEPT1 of H-X aa-Ser-OH dipeptides: evaluation of H-Phe-Ser-OH as a pro-moiety for ibuprofen and benzoic acid prodrugs. Eur J Pharm Biopharm. 2011;77(2):327-31.
46 Ovarian steroids, mitogen-activated protein kinases, and/or aspartic proteinases cooperate to control endometrial remodeling by regulating gene expression in the stroma and glands. Endocrinology. 2010;151(9):4515-26.
47 DNA methylation alterations in response to pesticide exposure in vitro. Environ Mol Mutagen. 2012;53(7):542-9.
48 Absorption of lisdexamfetamine dimesylate and its enzymatic conversion to d-amphetamine. Neuropsychiatr Dis Treat. 2010 Jun 24;6:317-27.
49 Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000 Jun;89(6):781-9.
50 Inhibitory effect of zinc on the absorption of JBP485 via the gastrointestinal oligopeptide transporter (PEPT1) in rats. Drug Metab Pharmacokinet. 2011;26(5):494-502.
51 A multi-omics approach to elucidate okadaic acid-induced changes in human HepaRG hepatocarcinoma cells. Arch Toxicol. 2024;98(9):2919-2935.
52 Comparative analysis of gene regulation by the transcription factor PPARalpha between mouse and human. PLoS One. 2009;4(8):e6796.
53 Endothelial effects of emission source particles: acute toxic response gene expression profiles. Toxicol In Vitro. 2009 Feb;23(1):67-77.

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