SLC15A1

Summary

Gene Symbol: SLC15A1
Description: solute carrier family 15 member 1
Alias: HPECT1, HPEPT1, PEPT1, solute carrier family 15 member 1, Caco-2 oligopeptide transporter, intestinal H+/peptide cotransporter, macrophage oligopeptide transporter PEPT1, oligopeptide transporter, small intestine isoform, peptide transporter 1, solute carrier family 15 (oligopeptide transporter), member 1
Species: human

Top Publications

  1. pmc Accumulation and oriented transport of ampicillin in Caco-2 cells from its pivaloyloxymethylester prodrug, pivampicillin
    Hugues Chanteux
    Unité de Pharmacologie Cellulaire et Moléculaire, Université catholique de Louvain 73 70, avenue E Mounier, 73, B 1200 Brussels, Belgium
    Antimicrob Agents Chemother 49:1279-88. 2005
  2. ncbi The oligopeptide transporter (Pept-1) in human intestine: biology and function
    S A Adibi
    Department of Medicine, University of Pittsburgh School of Medicine, Pennsylvania 15213, USA
    Gastroenterology 113:332-40. 1997
  3. ncbi An oligopeptide transporter is expressed at high levels in the pancreatic carcinoma cell lines AsPc-1 and Capan-2
    D E Gonzalez
    Department of Pharmaceutical Research and Development, Genentech, Inc, South San Francisco, California 94080, USA
    Cancer Res 58:519-25. 1998
  4. ncbi Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2
    M E Ganapathy
    Department of Medicine, Medical College of Georgia, Augusta 30912, USA
    J Biol Chem 270:25672-7. 1995
  5. doi PepT1 oligopeptide transporter (SLC15A1) gene polymorphism in inflammatory bowel disease
    Marco Zucchelli
    Department of Biosciences and Nutrition, Karolinska Institutet, Stockholm, Sweden
    Inflamm Bowel Dis 15:1562-9. 2009
  6. pmc Pathogenic bacteria induce colonic PepT1 expression: an implication in host defense response
    Hang Thi Thu Nguyen
    Department of Medicine, Emory University, Atlanta, Georgia 30322, USA
    Gastroenterology 137:1435-47.e1-2. 2009
  7. pmc PepT1 mediates transport of the proinflammatory bacterial tripeptide L-Ala-{gamma}-D-Glu-meso-DAP in intestinal epithelial cells
    Guillaume Dalmasso
    Department of Medicine, Emory University, Atlanta, GA 30322, USA
    Am J Physiol Gastrointest Liver Physiol 299:G687-96. 2010
  8. pmc The PepT1-NOD2 signaling pathway aggravates induced colitis in mice
    Guillaume Dalmasso
    Department of Medicine, Division of Digestive Diseases, Emory University, Atlanta, Georgia 30322, USA
    Gastroenterology 141:1334-45. 2011
  9. ncbi Characteristics of dipeptide transport in pig jejunum in vitro
    C Winckler
    Research Centre for Animal Production and Technology, , Germany
    J Comp Physiol B 169:495-500. 1999
  10. pmc Future direction of renal positron emission tomography
    Zsolt Szabo
    Division of Nuclear Medicine, Johns Hopkins University School of Medicine, Baltimore, MD 21287, USA
    Semin Nucl Med 36:36-50. 2006

Detail Information

Publications214 found, 100 shown here

  1. pmc Accumulation and oriented transport of ampicillin in Caco-2 cells from its pivaloyloxymethylester prodrug, pivampicillin
    Hugues Chanteux
    Unité de Pharmacologie Cellulaire et Moléculaire, Université catholique de Louvain 73 70, avenue E Mounier, 73, B 1200 Brussels, Belgium
    Antimicrob Agents Chemother 49:1279-88. 2005
    ..Release of ampicillin from cells incubated with PIVA was unaffected by PEPT1 and OCTN2 inhibitors but was sharply decreased after ATP depletion or addition of bis(4-nitrophenyl)-phosphate (..
  2. ncbi The oligopeptide transporter (Pept-1) in human intestine: biology and function
    S A Adibi
    Department of Medicine, University of Pittsburgh School of Medicine, Pennsylvania 15213, USA
    Gastroenterology 113:332-40. 1997
    ....
  3. ncbi An oligopeptide transporter is expressed at high levels in the pancreatic carcinoma cell lines AsPc-1 and Capan-2
    D E Gonzalez
    Department of Pharmaceutical Research and Development, Genentech, Inc, South San Francisco, California 94080, USA
    Cancer Res 58:519-25. 1998
    ....
  4. ncbi Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2
    M E Ganapathy
    Department of Medicine, Medical College of Georgia, Augusta 30912, USA
    J Biol Chem 270:25672-7. 1995
    ..It is concluded that there are marked differences between the intestinal and renal peptide transporters in the recognition of beta -lactam antibiotics as substrates...
  5. doi PepT1 oligopeptide transporter (SLC15A1) gene polymorphism in inflammatory bowel disease
    Marco Zucchelli
    Department of Biosciences and Nutrition, Karolinska Institutet, Stockholm, Sweden
    Inflamm Bowel Dis 15:1562-9. 2009
    ..The intestinal transporter PepT1, encoded by the SLC15A1 gene, mediates intracellular uptake of bacterial products that can induce inflammation and NF-kappaB activation ..
  6. pmc Pathogenic bacteria induce colonic PepT1 expression: an implication in host defense response
    Hang Thi Thu Nguyen
    Department of Medicine, Emory University, Atlanta, Georgia 30322, USA
    Gastroenterology 137:1435-47.e1-2. 2009
    Expression of the di/tripeptide transporter PepT1 has been observed in the colon under inflammatory conditions; however, the inducing factors and underlying mechanisms remain unknown...
  7. pmc PepT1 mediates transport of the proinflammatory bacterial tripeptide L-Ala-{gamma}-D-Glu-meso-DAP in intestinal epithelial cells
    Guillaume Dalmasso
    Department of Medicine, Emory University, Atlanta, GA 30322, USA
    Am J Physiol Gastrointest Liver Physiol 299:G687-96. 2010
    b>PepT1 is a di/tripeptide transporter highly expressed in the small intestine, but poorly or not expressed in the colon. However, during chronic inflammation, such as inflammatory bowel disease, PepT1 expression is induced in the colon...
  8. pmc The PepT1-NOD2 signaling pathway aggravates induced colitis in mice
    Guillaume Dalmasso
    Department of Medicine, Division of Digestive Diseases, Emory University, Atlanta, Georgia 30322, USA
    Gastroenterology 141:1334-45. 2011
    The human di/tripeptide transporter human intestinal H-coupled oligonucleotide transporter (hPepT1) is abnormally expressed in colons of patients with inflammatory bowel disease, although its exact role in pathogenesis is unclear...
  9. ncbi Characteristics of dipeptide transport in pig jejunum in vitro
    C Winckler
    Research Centre for Animal Production and Technology, , Germany
    J Comp Physiol B 169:495-500. 1999
    ..Moreover, RT-PCR studies with primers derived from rabbit PepT1 identified two PCR fragments of identical size to rabbit PepT1 from pig intestinal mRNA preparations...
  10. pmc Future direction of renal positron emission tomography
    Zsolt Szabo
    Division of Nuclear Medicine, Johns Hopkins University School of Medicine, Baltimore, MD 21287, USA
    Semin Nucl Med 36:36-50. 2006
    ..on the investigation of metabolism (acetate), membrane transporters (organic cation and anion transporters, pepT1 and pepT2, GLUT, SGLT), enzymes (ACE), and receptors (AT1R)...
  11. pmc An Arabidopsis peptide transporter is a member of a new class of membrane transport proteins
    H Y Steiner
    Department of Microbiology, University of Tennessee, Knoxville 37996 0845
    Plant Cell 6:1289-99. 1994
    ..the Arabidopsis nitrate-inducible nitrate transporter (CHL1), the rabbit small intestine oligopeptide transporter (PepT1), and the yeast peptide transporter (Ptr2p), respectively, but little identity to other proteins known to be ..
  12. doi The effect of glucagon-like peptide 2 injection on performance, small intestinal morphology, and nutrient transporter expression of stressed broiler chickens
    X F Hu
    The State Key Laboratory of Animal Nutrition, College of Animal Science and Technology, China Agricultural University, Beijing 100193, P R China
    Poult Sci 89:1967-74. 2010
    ..1 (SGLT-1), vitamin D-dependent calcium-binding protein-28,000 molecular weight (CaBP-D28k), and peptide transporter 1 (PepT-1) mRNA in the duodenum and of liver fatty acid-binding protein (L-FABP) mRNA in the jejunum...
  13. pmc The proton-coupled amino acid transporter, SLC36A1 (hPAT1), transports Gly-Gly, Gly-Sar and other Gly-Gly mimetics
    S Frølund
    Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, Denmark
    Br J Pharmacol 161:589-600. 2010
    ..and to investigate Gly-Sar transport via SLC36A1 and the proton-coupled dipeptide/tripeptide transporter, SLC15A1 in Caco-2 cells...
  14. ncbi Concentration-dependent atypical intestinal absorption of cyclic phenylalanylserine: small intestine acts as an interface between the body and ingested compounds
    Takashi Mizuma
    Department of Biopharmaceutics and Drug Rationale Research Center, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Horinouchi, Hachioji, Tokyo, Japan
    Biol Pharm Bull 26:1625-8. 2003
    ..in the presence of glycylsarcosine, cephalexin or cephradine, substrates for H+/oligopeptide cotransporter (PEPT1)...
  15. doi Gene ablation for PEPT1 in mice abolishes the effects of dipeptides on small intestinal fluid absorption, short-circuit current, and intracellular pH
    Mingmin Chen
    Department of Gastroenterology, Hepatology and Endocrinology, Hannover Medical School, Carl Neuberg Strasse 1, D 30625 Hannover, Germany
    Am J Physiol Gastrointest Liver Physiol 299:G265-74. 2010
    ..Immunohistochemistry for PEPT1 failed to detect any protein in enterocyte apical membranes in Slc15a1(-/-) animals. Saturable Gly-Sar uptake in Slc15a1(-/-) everted sac preparations was no longer detectable...
  16. ncbi Uptake of cyclic dipeptide by PEPT1 in Caco-2 cells: phenolic hydroxyl group of substrate enhances affinity for PEPT1
    Takashi Mizuma
    Department of Biopharmaceutics and Drug Rational Research Center, School of Pharmacy, Tokyo University of Pharmacy and Life Science TUPLS, Hachioji, Japan
    J Pharm Pharmacol 54:1293-6. 2002
    Uptake of cyclic dipeptides by H+/oligopeptide cotransporter (PEPT1) was studied in monolayers of the human intestinal cell line, Caco-2...
  17. ncbi Concentration-dependent preferences of absorptive and excretive transport cause atypical intestinal absorption of cyclic phenylalanylserine: small intestine acts as an interface between the body and ingested compounds
    Takashi Mizuma
    Department of Biopharmaceutics and Drug Rational Research Center School of Pharmacy, Tokyo University of Pharmacy and Life Science, 1432 1 Horinouchi, Hachioji, Tokyo 192 0392, Japan
    Res Commun Mol Pathol Pharmacol 111:199-209. 2002
    ..in the presence of glycylsarcosine, cephalexin or cephradine, substrates for H+/oligopeptide cotransporter (PEPT1). CLabs of cyclo(Phe-Ser) also decreased at 4 degrees C...
  18. ncbi Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells
    T Terada
    Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Japan
    Am J Physiol 273:F706-11. 1997
    b>PEPT1 and PEPT2 are H(+)-coupled peptide transporters expressed preferentially in the intestine and kidney, respectively, which mediate uphill transport of oligopeptides and peptide-like drugs such as beta-lactam antibiotics...
  19. ncbi The effect of wellsolve, a novel solubilizing agent, on the intestinal barrier function and intestinal absorption of griseofulvin in rats
    Khuriah Abdul Hamid
    Department of Biopharmaceutics, Kyoto Pharmaceutical University, Misasagi, Yamashina ku, Kyoto 607 8414, Japan
    Biol Pharm Bull 32:1898-905. 2009
    ..function of intestinal membrane barrier and transporters including P-glycoprotein (P-gp) and peptide transporter (PEPT1) was examined by an in vitro diffusion chamber and an in situ closed loop method...
  20. ncbi Decisive structural determinants for the interaction of proline derivatives with the intestinal H+/peptide symporter
    M Brandsch
    Biozentrum, Martin Luther University Halle Wittenberg, Germany
    Eur J Biochem 266:502-8. 1999
    ..interaction, the affinity of short amide and imide derivatives for the intestinal H+/peptide symporter (PEPT1) was investigated by measuring their ability to inhibit Gly-Sar transport in Caco-2 cells...
  21. ncbi PEPT1 as a paradigm for membrane carriers that mediate electrogenic bidirectional transport of anionic, cationic, and neutral substrates
    Gabor Kottra
    Molecular Nutrition Unit, Technical University of Munich, Hochfeldweg 2, D 85350 Freising Weihenstephan, Germany
    J Biol Chem 277:32683-91. 2002
    ..electrogenic transfer of selected anionic, cationic, and neutral dipeptides by the intestinal peptide transporter PEPT1. Anionic dipeptides such as Gly-Asp and Asp-Gly are transported in their neutral and negatively charged forms with ..
  22. ncbi [Active drug delivery by heterologous expression of membrane transporters]
    Yoshimichi Sai
    Graduate School of Natural Science and Technology, Kanazawa University, 13 1 Takara machi, Kanazawa 920 0934, Japan
    Yakugaku Zasshi 123:413-22. 2003
    The oligopeptide transporter PEPT1 is predominantly expressed in the brush-border membranes of small intestinal epithelial cells, where it plays pivotal roles in the efficient absorption of di-/tripeptides...
  23. doi Comparison of drug transporter gene expression and functionality in Caco-2 cells from 10 different laboratories
    Rose Hayeshi
    Discovery DMPK and Bioanalytical Chemistry, AstraZeneca R and D Molndal, S 431 83 Molndal, Sweden
    Eur J Pharm Sci 35:383-96. 2008
    ..MDR1 and PepT1 function was investigated using talinolol and Gly-Sar transport, respectively...
  24. ncbi [Intestinal absorption and secretion mechanism of carboxylate drugs]
    Shirou Itagaki
    Laboratory of Clinical Pharmaceutics and Therapeutics, Department of Biopharmaceutical Sciences and Pharmacy, Division of Biopharmaceutical Sciences and Pharmacy, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita ku, Sapporo, Japan
    Yakugaku Zasshi 129:1341-9. 2009
    ..reaches the maximal serum concentration after oral administration, nateglinide itself is not transported by PepT1 or MCT1...
  25. pmc H+-coupled nutrient, micronutrient and drug transporters in the mammalian small intestine
    David T Thwaites
    Epithelial Research Group, Institute for Cell and Molecular Biosciences, Faculty of Medical Sciences, Framlington Place, University of Newcastle upon Tyne, Newcastle upon Tyne NE2 4HH, UK
    Exp Physiol 92:603-19. 2007
    ..expressed at the mammalian small intestinal brush-border membrane include: the di/tripeptide transporter PepT1 (SLC15A1); the proton-coupled amino-acid transporter PAT1 (SLC36A1); the divalent metal transporter DMT1 (SLC11A2); the ..
  26. doi Investigation of the role of oligopeptide transporter PEPT1 and sodium/glucose cotransporter SGLT1 in intestinal absorption of their substrates using small GTP-binding protein Rab8-null mice
    Yukio Kato
    Division of Pharmaceutical Sciences, Graduate School of Natural Science and Technology, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Drug Metab Dispos 37:602-7. 2009
    A small GTP-binding protein, Rab8, is essential for apical localization of oligopeptide transporter PEPT1/SLC15A1 and sodium/glucose cotransporter SGLT1/SLC5A1 in small intestine; deficiency of rab8 gene results in mislocalization and ..
  27. doi Lactation stage-dependent expression of transporters in rat whole mammary gland and primary mammary epithelial organoids
    Samuel E Gilchrist
    University of British Columbia, Vancouver, Canada
    Fundam Clin Pharmacol 24:205-14. 2010
    ..in early lactation, which may remain elevated or decline with advancing lactation (Octn1, Cnt2, Cnt3, Ent1, Pept1, Pept2); (iii) constant but decreasing later in lactation (Octn3, Dmt1); (iv) increasing until mid-to-late ..
  28. pmc Delta-aminolevulinic acid is a substrate for the amino acid transporter SLC36A1 (hPAT1)
    S Frølund
    Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK 2100 Copenhagen, Denmark
    Br J Pharmacol 159:1339-53. 2010
    ..Oral administration of ALA has been used in patients with prostate and bladder cancer. The present aim was to investigate the mechanism of intestinal absorption of ALA and its transport via the amino acid transporter SLC36A1...
  29. doi The effect of plant protein-based diet supplemented with dipeptide or free amino acids on digestive tract morphology and PepT1 and PepT2 expressions in common carp (Cyprinus carpio L.)
    Teresa Ostaszewska
    Warsaw University of Life Sciences, Warszawa, Poland
    Comp Biochem Physiol A Mol Integr Physiol 157:158-69. 2010
    ..After 4 weeks of experimental feeding the highest relative expression of PepT1 gene was observed in fish fed PP diet, while the lowest expression occurred in fish fed CON...
  30. ncbi Constitutive expression of various xenobiotic and endobiotic transporter mRNAs in the choroid plexus of rats
    Supratim Choudhuri
    Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, 3901 Rainbow Blvd, Kansas City, KS 66160 7417, USA
    Drug Metab Dispos 31:1337-45. 2003
    ..Mrp3, Oct1, Oct2, Oatp1, Oatp4, Oatp5, Oatp12, Oat-K (1/2), Ntcp, Bsep, Ibat, Mdr1a, Mdr1b, Mdr2, Oat1, Ent2, Pept1, AbcG5, AbcG8] were expressed at very low levels in choroid plexus...
  31. ncbi Demonstration of functional dipeptide transport with expression of PEPT2 in guinea pig cardiomyocytes
    Hua Lin
    Bristol Heart Institute, University of Bristol, Bristol Royal Infirmary, Bristol BS2 8HW, UK
    Pflugers Arch 453:915-22. 2007
    The transporters PEPT1 and PEPT2 accept a broad spectrum of substrates including small, naturally occurring peptides and peptidomimetic drugs...
  32. ncbi Role of PEPT2 in peptide/mimetic trafficking at the blood-cerebrospinal fluid barrier: studies in rat choroid plexus epithelial cells in primary culture
    Cathaleen Shu
    College of Pharmacy, Department of Pharmaceutical Sciences, Upjohn Center for Clinical Pharmacology, University of Michigan, 1310 E Catherine Street, Ann Arbor, MI 48109, USA
    J Pharmacol Exp Ther 301:820-9. 2002
    ..Immunoblot analyses and immunofluorescent confocal microscopy demonstrated the presence of PEPT2, but not PEPT1, in rat choroid plexus epithelial cells...
  33. doi Synthesis, transport and pharmacokinetics of 5'-amino acid ester prodrugs of 1-beta-D-arabinofuranosylcytosine
    Yongbing Sun
    Department of Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China
    Mol Pharm 6:315-25. 2009
    ..To develop an oral alternative for 1 and utilize the intestinal oligopeptide transporter 1 (PepT1), a series of 5'-amino acid ester derivatives of 1 was synthesized to clarify which modification was the most ..
  34. pmc The apical (hPepT1) and basolateral peptide transport systems of Caco-2 cells are regulated by AMP-activated protein kinase
    Myrtani Pieri
    School of Life Sciences, Oxford Brookes University, Headington, Oxford OX3 0BP, UK
    Am J Physiol Gastrointest Liver Physiol 299:G136-43. 2010
    ..and transepithelial fluxes of [(3)H]-D-Phe-L-Gln were carried out in differentiated Caco-2 cell monolayers, and hPepT1 and glucose transporter 2 (GLUT2) protein levels were quantified by immunogold electron microscopy...
  35. pmc ABC and SLC transporter expression and proton oligopeptide transporter (POT) mediated permeation across the human blood--brain barrier cell line, hCMEC/D3 [corrected]
    Stephen M Carl
    Department of Industrial and Physical Pharmacy, School of Pharmacy, Purdue University, West Lafayette, Indiana, USA
    Mol Pharm 7:1057-68. 2010
    ..hCMEC/D3 cells express both hPHT1 and hPHT2, while little to no expression of either hPepT1 or hPepT2 was observed. The relative expression of other ABC and SLC transporters is discussed...
  36. ncbi Pharmacokinetics and mechanism of intestinal absorption of JBP485 in rats
    Jian Cang
    Department of Clinical Pharmacology, College of Pharmacy, Dalian Medical University, Dalian, China
    Drug Metab Pharmacokinet 25:500-7. 2010
    ..transport of JBP485 were examined in everted intestinal sacs, in situ jejunal perfusion, Caco-2 cells and PEPT1 transfected Hela cells. The gastrointestinal absorption of JBP485 was rapid. T(1/2β) was 2.25 ± 0...
  37. ncbi Transcellular transport of a highly polar 3+ net charge opioid tetrapeptide
    Kesheng Zhao
    Department of Pharmacology, Weill Medical College of Cornell University, New York, New York 10021, USA
    J Pharmacol Exp Ther 304:425-32. 2003
    ..Peptide transporters (PEPT1 and PEPT2) play a major role in the uptake of di- and tripeptides across cell membranes, but their ability to ..
  38. ncbi Monocarboxylate transporter 1 mediates DL-2-Hydroxy-(4-methylthio)butanoic acid transport across the apical membrane of Caco-2 cell monolayers
    Raquel Martín-Venegas
    Departament de Fisiologia, Facultat de Farmacia, Universitat de Barcelona, 08028 Barcelona, Spain
    J Nutr 137:49-54. 2007
    ..betaine, or glycyl-sarcosine excluded the participation of systems proton amino acid transporter 1 and peptide transporter 1. In contrast, alpha-cyano-4-hydroxycinnamate, phloretin, L-lactate, beta-hydroxybutyrate, butyrate, and ..
  39. ncbi Identification of the histidine residues involved in substrate recognition by a rat H+/peptide cotransporter, PEPT1
    T Terada
    Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Japan
    FEBS Lett 394:196-200. 1996
    The LLC-PK1 cells stably transfected with a rat PEPT1 cDNA transported ceftibuten (anion) and cephradine (zwitterion), both oral beta-lactam antibiotics, in a H+-gradient-dependent manner...
  40. doi Quantitative evaluation of PEPT1 contribution to oral absorption of cephalexin in rats
    Takanori Hironaka
    Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University, 1 1 1 Tsushima naka, Okayama, 700 8530, Japan
    Pharm Res 26:40-50. 2009
    b>PEPT1 mediates the intestinal absorption of many drugs, but its contribution to oral absorption of drugs is still controversial...
  41. ncbi Direct evidence for efficient transport and minimal metabolism of L-cephalexin by oligopeptide transporter 1 in budded baculovirus fraction
    Keisuke Mitsuoka
    Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan
    Biol Pharm Bull 32:1459-61. 2009
    The oligopeptide transporter PEPT1 (SLC15A1) is responsible for absorption of peptidic nutrients in the small intestine...
  42. pmc Enhanced cancer cell growth inhibition by dipeptide prodrugs of floxuridine: increased transporter affinity and metabolic stability
    Yasuhiro Tsume
    Department of Pharmaceutical Science, University of Michigan, Ann Arbor, Michigan 48109, USA
    Mol Pharm 5:717-27. 2008
    ..were synthesized, and their chemical stability in buffers, resistance to glycosidic bond metabolism, affinity for PEPT1, enzymatic activation and permeability in cancer cells were determined and compared to those of mono amino acid ..
  43. doi Gene expression of nutrient transporters in the small intestine of chickens from lines divergently selected for high or low juvenile body weight
    C R Mott
    Department of Animal and Poultry Sciences, Virginia Polytechnic Institute and State University, Blacksburg 24061 0306, USA
    Poult Sci 87:2215-24. 2008
    ..This study examined correlated responses to selection in the developmental gene expression of PepT1, EAAT3, SGLT1, and GLUT5 in the small intestine of chickens from lines divergently selected for 48 generations for ..
  44. ncbi beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter
    M E Ganapathy
    Department of Medicine, Medical College of Georgia, Augusta, Georgia 30912, USA
    J Biol Chem 275:1699-707. 2000
    ..antibiotics that were not recognized by OCTN2 were good substrates for the H(+)-coupled peptide transporters PEPT1 and PEPT2...
  45. pmc Function and immunolocalization of overexpressed human intestinal H+/peptide cotransporter in adenovirus-transduced Caco-2 cells
    C P Hsu
    Johnson and Johnson, Drug Metabolism, Route 202, P O Box 300, Raritan, NJ 08869, USA
    AAPS PharmSci 1:E12. 1999
    To determine the localization of the human intestinal H+/peptide cotransporter (hPepT1) and its function in intestinal epithelial cells after adenoviral transduction.
  46. ncbi Severe villus atrophy and chronic malabsorption induced by azathioprine
    Thomas R Ziegler
    Department of Medicine, Center for Clinical and Molecular Nutrition, Emory University School of Medicine, 1364 Clifton Road, Atlanta, GA 30322, USA
    Gastroenterology 124:1950-7. 2003
    ..Duodenal mucosal histology and expression of brush border enzyme dipeptidyl peptidase IV and peptide transporter PepT1 messenger RNA levels were determined before and after azathioprine discontinuation...
  47. ncbi Transport of levovirin prodrugs in the human intestinal Caco-2 cell line
    Fujun Li
    Pharmaceutics, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
    J Pharm Sci 95:1318-25. 2006
    ..to improve the permeability of LVV across the intestinal epithelium by targeting the di/tri-peptide carrier, PepT1. Caco-2 cell monolayers were employed to study the transport and hydrolysis properties of the prodrugs...
  48. ncbi Peptide transporter substrate identification during permeability screening in drug discovery: comparison of transfected MDCK-hPepT1 cells to Caco-2 cells
    Praveen V Balimane
    Metabolism and Pharmacokinetics, Bristol Myers Squibb, Princeton, NJ 08543, USA
    Arch Pharm Res 30:507-18. 2007
    The purpose of this study was to investigate the utility of stably transfected MDCK-hPepT1 cells for identifying peptide transporter substrates in early drug discovery and compare the characteristics of this cell line with Caco-2 cells...
  49. ncbi Dietary protein quality and feed restriction influence abundance of nutrient transporter mRNA in the small intestine of broiler chicks
    Elizabeth R Gilbert
    Department of Animal and Poultry Sciences, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA
    J Nutr 138:262-71. 2008
    ..The objective of this study was to evaluate the effect of dietary protein quality on intestinal peptide transporter (PepT1), amino acid transporter [Na+-independent cationic and zwitterionic amino acid transporter (b(o,+)AT), excitatory ..
  50. doi Expression of the oligopeptide transporter, PepT1, in larval Atlantic cod (Gadus morhua)
    J J Amberg
    University of Idaho, Hagerman Fish Culture Experiment Station, 3059 F National Fish Hatchery Road, Hagerman, ID 83332, USA
    Comp Biochem Physiol B Biochem Mol Biol 150:177-82. 2008
    The intestinal absorption of di- and tri-peptides generally occurs via the oligopeptide transporter, PepT1. This study evaluates the expression of PepT1 in larval Atlantic cod (Gadus morhua) during the three weeks following the onset of ..
  51. pmc Transport of the photodynamic therapy agent 5-aminolevulinic acid by distinct H+-coupled nutrient carriers coexpressed in the small intestine
    Catriona M H Anderson
    Epithelial Research Group, Institute for Cell and Molecular Biosciences, Faculty of Medical Sciences, Framlington Place, Newcastle University, Newcastle upon Tyne, UK
    J Pharmacol Exp Ther 332:220-8. 2010
    ..and 4-aminomethylbenzoic acid for, respectively, PAT1 and the H(+)-coupled di/tripeptide transporter PepT1 (SLC15A1) were examined...
  52. doi Lactobacillus plantarum consumption increases PepT1-mediated amino acid absorption by enhancing protein kinase C activity in spontaneously colitic mice
    Hong qi Chen
    Department of General Surgery, Affiliated Sixth People s Hospital, Shanghai, People s Republic of China
    J Nutr 140:2201-6. 2010
    ..of Lactobacillus plantarum (LP) on intestinal nutrient absorption, particularly oligopeptide transporter 1 (PepT1)-mediated absorption of dietary protein under inflammatory conditions, has not yet been characterized...
  53. ncbi Effects of progesterone and norethisterone on cephalexin uptake in the human intestinal cell line Caco-2
    Kazuhiro Watanabe
    Hokkaido College of Pharmacy, 7 1 Katsuraoka cho, Otaru, Hokkaido 047 0264, Japan
    Biol Pharm Bull 27:559-63. 2004
    Little is known about the regulatory effects of steroid hormones on the intestinal H(+)/oligopeptide transporter PEPT1. In the present study, we investigated the effects of progesterone and its related compounds on the uptake of ..
  54. ncbi Enhanced absorption and growth inhibition with amino acid monoester prodrugs of floxuridine by targeting hPEPT1 transporters
    Yasuhiro Tsume
    Department of Pharmaceutical Science, College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI 48109 1065, USA
    Molecules 13:1441-54. 2008
    ..038 x 10(-6) cm/sec). MDCK cells stably transfected with the human oligopeptide transporter PEPT1 (MDCK/hPEPT1) exhibited enhanced cell growth inhibition in the presence of the prodrugs...
  55. doi Dietary protein hydrolysates and free amino acids affect the spatial expression of peptide transporter PepT1 in the digestive tract of Atlantic cod (Gadus morhua)
    Snorre Bakke
    Department of Biology, University of Bergen, Norway
    Comp Biochem Physiol B Biochem Mol Biol 156:48-55. 2010
    The effects of dietary inclusions of size-fractionated peptides and free amino acids (FAAs) on Peptide Transporter 1 (PepT1) mRNA levels were assessed along the length of the intestine of juvenile Atlantic cod (Gadus morhua)...
  56. ncbi Metoclopramide modifies oral cephalexin pharmacokinetics in dogs
    A P Prados
    Farmacologia, Facultad de Ciencias Veterinarias, Universidad de Buenos Aires, Buenos Aires, Argentina
    J Vet Pharmacol Ther 30:127-31. 2007
    ..cephalexin absorption by affecting its delivery to the intestine, and/or enhancing intestinal transporter PEPT1 function...
  57. ncbi Cloning and characterization of a rat H+/peptide cotransporter mediating absorption of beta-lactam antibiotics in the intestine and kidney
    H Saito
    Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Japan
    J Pharmacol Exp Ther 275:1631-7. 1995
    A complementary DNA (cDNA) encoding the rat H+/peptide cotransporter (PepT1) was isolated, and the transport characteristics of orally active beta-lactam antibiotics were assessed by measuring uptake into Xenopus oocytes expressing the ..
  58. pmc Stoichiometry and pH dependence of the rabbit proton-dependent oligopeptide transporter PepT1
    A Steel
    Department of Medicine, Brigham and Women s Hospital, Boston, MA 02115, USA
    J Physiol 498:563-9. 1997
    1. The intestinal H(+)-coupled peptide transporter PepT1, displays a broad substrate specificity and accepts most charged and neutral di- and tripeptides...
  59. ncbi A novel inhibitor of the mammalian peptide transporter PEPT1
    I Knutter
    Institute of Biochemistry, Department of Biochemistry Biotechnology, and Biozentrum, Martin Luther University Halle Wittenberg, Halle, Germany
    Biochemistry 40:4454-8. 2001
    ..evidence that the dipeptide derivative Lys[Z(NO(2))]-Pro is an effective competitive inhibitor of mammalian PEPT1 with an apparent binding affinity of 5-10 microM...
  60. pmc Genomic structure of proton-coupled oligopeptide transporter hPEPT1 and pH-sensing regulatory splice variant
    A Urtti
    Department of Biopharmaceutical Sciences, University of California San Francisco, CA 94143 0446, USA
    AAPS PharmSci 3:E6. 2001
    ..symport is driven by pH gradients, while the profile of pH sensitivity is regulated by a closely related protein, hPEPT1-RF. We investigated the genomic structure of hPEPT1 and hPEPT1-RF...
  61. ncbi Intestinal absorption of cephalexin in diabetes mellitus model rats
    Kazuhiro Watanabe
    Hokkaido College of Pharmacy, 7 1 Katsuraoka cho, Otaru, Hokkaido 047 0264, Japan
    Eur J Pharm Sci 19:91-8. 2003
    ..intestinal absorption and pharmacokinetics of cephalexin, as well as the intestinal H+/oligopeptide transporter PEPT1 mRNA and protein levels in type 1 and type 2 diabetic rats...
  62. ncbi Molecular and functional characterisation of the zebrafish (Danio rerio) PEPT1-type peptide transporter
    Tiziano Verri
    Department of Biological and Environmental Sciences and Technologies, University of Lecce, Via provinciale Lecce Monteroni, I 73100 Lecce, Italy
    FEBS Lett 549:115-22. 2003
    ..and functional characterisation of a novel peptide transporter from zebrafish, orthologue to mammalian and avian PEPT1. Zebrafish PEPT1 is a low-affinity/high-capacity system...
  63. ncbi Enhanced intestinal absorption of drugs by activation of peptide transporter PEPT1 using proton-releasing polymer
    Takashi Nozawa
    Faculty of Pharmaceutical Sciences, Department of Molecular Biopharmaceutics, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278 8510, Japan
    J Pharm Sci 92:2208-16. 2003
    ..In the present study, an increased supply of the driving force for peptide transporter PEPT1 by utilizing a proton-releasing polymer, Eudragit L100-55, was employed to increase the intestinal transport ..
  64. ncbi Genetic polymorphisms in human proton-dependent dipeptide transporter PEPT1: implications for the functional role of Pro586
    Eric Y Zhang
    Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Pharmacol Exp Ther 310:437-45. 2004
    The human proton-dependent dipeptide transporter (PEPT1, gene SLC15A1) is important for intestinal absorption of di- and tripeptides and a variety of peptidomimetic compounds...
  65. ncbi A novel pineal-specific product of the oligopeptide transporter PepT1 gene: circadian expression mediated by cAMP activation of an intronic promoter
    Pascaline Gaildrat
    Section on Neuroendocrinology, Laboratory of Developmental Neurobiology, NICHD, National Institutes of Health, Bethesda, Maryland 20892 4480, USA
    J Biol Chem 280:16851-60. 2005
    The oligopeptide transporter 1, PepT1, is a member of the Slc15 family of 12 membrane-spanning domain transporters; PepT1 has proton/peptide cotransport activity and is selectively expressed in intestinal epithelial cells, where it is ..
  66. ncbi Conformational restrictions in ligand binding to the human intestinal di-/tripeptide transporter: implications for design of hPEPT1 targeted prodrugs
    Jon Våbenø
    Department of Medicinal Chemistry, Institute of Pharmacy, University of Tromsø, N 9037 Tromsø, Norway
    Bioorg Med Chem 13:1977-88. 2005
    ..aiding the design of dipeptidomimetic pro-moieties targeting the human intestinal di-/tripeptide transporter hPEPT1. First, the conformation in which substrates bind to hPEPT1 (the bioactive conformation) was identified by ..
  67. ncbi The extracellular pH dependency of transport activity by human oligopeptide transporter 1 (hPEPT1) expressed stably in Chinese hamster ovary (CHO) cells: a reason for the bell-shaped activity versus pH
    Yuki Fujisawa
    Laboratory of Biophysical Chemistry, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan
    Biol Pharm Bull 29:997-1005. 2006
    Human oligopeptide transporter (hPEPT1) translocates di/tri-peptide by coupling to movement of proton down the electrochemical gradient...
  68. ncbi Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines
    Constanze Hilgendorf
    Discovery Drug Metabolism and Pharmacokinetics and Bioanalytical Chemistry, AstraZeneca Research and Development, Molndal, Sweden
    Drug Metab Dispos 35:1333-40. 2007
    ..Transporters that were highly expressed in the intestine included HPT1, PEPT1, BCRP, MRP2, and MDR1, whereas, in the liver, OCT1, MRP2, OATP-C, NTCP and BSEP were the main transporters...
  69. ncbi Long-term effect of leptin on H+-coupled peptide cotransporter 1 activity and expression in vivo: evidence in leptin-deficient mice
    Patrick Hindlet
    Department of Clinical Pharmacy Unité Propre de Recherche et de l Enseignement Supérieur, Equipe d Accueil 2706, Faculty of Pharmaceutical Sciences Paris XI, 5, rue Jean Baptiste Clement, 92296 Chatenay Malabry, France
    J Pharmacol Exp Ther 323:192-201. 2007
    The H+-coupled peptide cotransporter 1 (PepT1) mediates absorption of peptides and peptidomimetic drugs...
  70. doi Quantitative prediction of oral absorption of PEPT1 substrates based on in vitro uptake into Caco-2 cells
    Rikako Shimizu
    School of Pharmacy, Kitasato University, 5 9 1 Shirokane, Minato ku, Tokyo 108 8641, Japan
    Int J Pharm 354:104-10. 2008
    The method for predicting the fraction absorbed (Fa) of the PEPT1 substrates was established based on the in vitro uptake into Caco-2 cells...
  71. doi Oral absorption of ampicillin: role of paracellular route vs. PepT1 transporter
    Guylène Lafforgue
    Laboratoire Cinétique des Xénobiotiques, Faculte des sciences pharmaceutiques, 35 chemin des Maraichers, 31062 Toulouse Cedex 4, France
    Fundam Clin Pharmacol 22:189-201. 2008
    ..The improved rat everted gut sac system was used, with an emphasis on the role of the PepT1 transporter...
  72. doi Molecular mechanism of dipeptide and drug transport by the human renal H+/oligopeptide cotransporter hPEPT2
    Monica Sala-Rabanal
    Dept of Physiology, David Geffen School of Medicine at UCLA, 10833 Le Conte Ave, 53 330 CHS, Los Angeles, CA 90095 1751, USA
    Am J Physiol Renal Physiol 294:F1422-32. 2008
    The human proton/oligopeptide cotransporters hPEPT1 and hPEPT2 have been targeted to enhance the bioavailability of drugs and prodrugs. Previously, we established the mechanisms of drug transport by hPEPT1...
  73. pmc Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1)
    Praveen M Bahadduri
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA
    Bioorg Med Chem Lett 18:2555-7. 2008
    We employed a computational approach to design and synthesize a series of fluorescently labeled hPEPT1 substrates. Five Alexa Fluor-350-labeled peptides were assessed for their in vitro inhibitory activity in hPEPT1-transfected CHO cells...
  74. doi Expression profiling of the solute carrier gene family in chicken intestine from the late embryonic to early post-hatch stages
    H Li
    Department of Animal and Poultry Sciences, Virginia Tech, Blacksburg, VA 24061 0306, USA
    Anim Genet 39:407-24. 2008
    ..between E18 and D14 including the amino acid transporters rBAT, y(+)LAT-2 and EAAT3, the peptide transporter PepT1 and the sugar transporters SGLT1, GLUT2 and GLUT5. The amino acid transporters CAT-1 and CAT-2 were downregulated...
  75. doi Peptide derivation of poorly absorbable drug allows intestinal absorption via peptide transporter
    Akihiro Kikuchi
    Faculty of Pharmaceutical Sciences, Tokyo University of Science, Chiba, Japan
    J Pharm Sci 98:1775-87. 2009
    ..absorption of low-permeability drugs could be improved by utilization of the intestinal influx transporter PEPT1. We investigated whether peptide derivatives of poorly absorbable nonamino acid-like drugs might be substrates of ..
  76. doi Modeling of the intestinal peptide transporter hPepT1 and analysis of its transport capacities by docking and pharmacophore mapping
    Alessandro Pedretti
    Istituto di Chimica Farmaceutica e Tossicologica Pietro Pratesi, Facolta di Farmacia, Universita degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy
    ChemMedChem 3:1913-21. 2008
    ..Hence, the first objective of this study was to generate a reliable model for the structure of the hPepT1 protein, which is the main intestinal transporter involved in the absorption of both dietary peptides and ..
  77. ncbi Inhibitory effect of zinc on the absorption of beta-lactam antibiotic ceftibuten via the peptide transporters in rats
    Miyako Okamura
    Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Kyoto, Japan
    Drug Metab Pharmacokinet 23:464-8. 2008
    ..Previously, we showed that zinc inhibits the transport of glycylsarcosine via the intestinal peptide transporter PEPT1 in the human intestinal cell line Caco-2...
  78. doi Stimulation of electrogenic intestinal dipeptide transport by the glucocorticoid dexamethasone
    Rexhep Rexhepaj
    Department of Physiology, University of Tubingen, Gmelinstr 5, 72076, Tubingen, Germany
    Pflugers Arch 459:191-202. 2009
    ..Intestinal PepT1 was expressed in Xenopus oocytes, and peptide transport was determined by dual electrode voltage clamping...
  79. doi Lactobacillus plantarum ameliorates colonic epithelial barrier dysfunction by modulating the apical junctional complex and PepT1 in IL-10 knockout mice
    Hong qi Chen
    Dept of General Surgery, Affiliated Sixth People s Hospital, Shanghai Jiao Tong Univ, People s Republic of China
    Am J Physiol Gastrointest Liver Physiol 299:G1287-97. 2010
    ..Oligopeptide transporter 1 (PepT1)-mediated transepithelial transport was evaluated by measuring the plasma cephalexin concentration...
  80. doi Hijacking solute carriers for proton-coupled drug transport
    Catriona M H Anderson
    Epithelial Research Group, Institute for Cell and Molecular Biosciences, Faculty of Medical Sciences, Newcastle University, Newcastle upon Tyne, United Kingdom
    Physiology (Bethesda) 25:364-77. 2010
    ..These transporters include PepT1 and PepT2 (SLC15A1/2), PCFT (SLC46A1), PAT1 (SLC36A1), OAT10 (SLC22A13), OATP2B1 (SLCO2B1), MCT1 (SLC16A1), and MATE1 and MATE2-K (..
  81. doi The chick embryo yolk sac membrane expresses nutrient transporter and digestive enzyme genes
    L Yadgary
    Department of Animal Science, Hebrew University, Rehovot, Israel
    Poult Sci 90:410-6. 2011
    ..enzymes aminopeptidase N (APN) and sucrase-isomaltase (SI); the nutrient transporters oligopeptide transporter Pept1, cationic amino acid transporter CAT1, and sodium glucose transporter SGLT1; and the micronutrient transporters ..
  82. pmc Protein hydrolysate-induced cholecystokinin secretion from enteroendocrine cells is indirectly mediated by the intestinal oligopeptide transporter PepT1
    Alice P Liou
    Department of Anatomy, Physiology, and Cell Biology, School of Veterinary Medicine, University of California Davis, USA
    Am J Physiol Gastrointest Liver Physiol 300:G895-902. 2011
    ..Indirect functional evidence suggests that PepT1 may play a role in CCK-mediated changes in gastric motor function...
  83. doi Fragmental modeling of hPepT2 and analysis of its binding features by docking studies and pharmacophore mapping
    Alessandro Pedretti
    Dipartimento di Scienze Farmaceutiche Pietro Pratesi, Facolta di Farmacia, Universita degli Studi di Milano, Via Mangiagalli, 25, I 20133 Milano, Italy
    Bioorg Med Chem 19:4544-51. 2011
    ..the key features required for an optimal hPepT2 affinity and confirmed the main factors governing the hPepT2/hPepT1 selectivity...
  84. ncbi The mechanisms responsible for garlic - drug interactions and their in vivo relevance
    Katja Berginc
    Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia
    Curr Drug Metab 14:90-101. 2013
    ..BCRP) and uptake (MonoCarboxylate Transporter 1 - MCT1, Organic Anion Transporting Polypeptide - OATP, Peptide transporter 1 - PepT1) transporters were caused by changes in electrophysiological membrane properties and by allosteric ..
  85. pmc Alternating access mechanism in the POT family of oligopeptide transporters
    Nicolae Solcan
    Department of Biochemistry, University of Oxford, Oxford, UK
    EMBO J 31:3411-21. 2012
    ..In mammals, peptide transport occurs via PepT1 and PepT2, which belong to the proton-dependent oligopeptide transporter, or POT family...
  86. doi The ontogeny of nutrient transporter and digestive enzyme gene expression in domestic pigeon (Columba livia) intestine and yolk sac membrane during pre- and posthatch development
    X Y Dong
    Feed Science Institute, Zhejiang University, Zijingang Campus, Hangzhou, 310058, China
    Poult Sci 91:1974-82. 2012
    ..We investigated the oligopeptide transporter Pept1, sodium glucose transporter SGLT1, glucose transporter GLUT2, aminopeptidase-N (APN), and sucrase-isomaltase (SI)...
  87. doi Pivotal roles of peptide transporter PEPT1 and ATP-binding cassette (ABC) transporter ABCG2 in 5-aminolevulinic acid (ALA)-based photocytotoxicity of gastric cancer cells in vitro
    Yuichiro Hagiya
    Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, 4259 Nagatsuta cho, Midori ku, Yokohama 226 8501, Japan
    Photodiagnosis Photodyn Ther 9:204-14. 2012
    ..In the present study, by focusing on genes involved in the porphyrin biosynthesis pathway, we aimed to explore biomarkers that are predictive for the efficacy of ALA-PDT...
  88. pmc Influence of overexpression of efflux proteins on the function and gene expression of endogenous peptide transporters in MDR-transfected MDCKII cell lines
    Zhiying Wang
    Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri Kansas City, Health Sciences Building, 2464 Charlotte Street, Kansas City, MO 64108 2718, USA
    Int J Pharm 441:40-9. 2013
    ..Levels of mRNA for both canine PepT1 and PepT2 were substantially reduced when efflux transporters overexpressed but enhanced when mRNA-levels of ..
  89. doi Propylene glycol-linked amino acid/dipeptide diester prodrugs of oleanolic acid for PepT1-mediated transport: synthesis, intestinal permeability, and pharmacokinetics
    Feng Cao
    State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, P R China
    Mol Pharm 10:1378-87. 2013
    ..of oleanolic acid (OA), a Biopharmaceutics Classification System (BCS) class IV drug, designed to target peptide transporter 1 (PepT1) have been synthesized and evaluated...
  90. pmc Proton-coupled oligopeptide transporter family SLC15: physiological, pharmacological and pathological implications
    David E Smith
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA
    Mol Aspects Med 34:323-36. 2013
    ..In this review, we provide updated information on the structure-function of PepT1 (SLC15A1), PepT2 (SLC15A2), PhT1 (SLC15A4) and PhT2 (SLC15A3), and their expression and localization in key tissues...
  91. doi Maternal protein restriction during pregnancy affects gene expression and immunolocalization of intestinal nutrient transporters in rats
    Daniela F Pinheiro
    Department of Physiology, Universidade Estadual Paulista, Botucatu, Brazil
    Clin Sci (Lond) 125:281-9. 2013
    ..The presence of SGLT1 (sodium-glucose co-transporter 1), GLUT2 (glucose transporter 2), PEPT1 (peptide transporter 1) and the intestinal proliferation were evaluated by immunohistochemical techniques and the abundance of ..
  92. pmc Impact of peptide transporter 1 on the intestinal absorption and pharmacokinetics of valacyclovir after oral dose escalation in wild-type and PepT1 knockout mice
    Bei Yang
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan
    Drug Metab Dispos 41:1867-74. 2013
    ..properties of valacyclovir, including the potential for saturable proton-coupled oligopeptide transporter 1 (PepT1)-mediated intestinal uptake, after escalating oral doses of prodrug within the clinical dose range...
  93. pmc Transcriptional and functional regulation of the intestinal peptide transporter PEPT1
    Britta Spanier
    Biochemistry, Technische Universitat Munchen, ZIEL Research Center of Nutrition and Food Sciences, Gregor Mendel Straße 2, D 85350 Freising, Germany
    J Physiol 592:871-9. 2014
    ..different di- and tripeptides is performed by the high-capacity/low-affinity peptide transporter isoform PEPT1 (SLC15A1)...
  94. doi Enhanced visualization of small peptides absorbed in rat small intestine by phytic-acid-aided matrix-assisted laser desorption/ionization-imaging mass spectrometry
    Seong Min Hong
    Division of Bioresources and Bioenvironmental Sciences, Faculty of Agriculture, Graduate School, Kyushu University, 6 10 1 Hakozaki, Fukuoka 812 8581, Japan
    Anal Chem 85:10033-9. 2013
    ..Penetrants through intestinal peptide transporter 1, i.e., glycyl-sarcosine (Gly-Sar, 147.1 m/z) and antihypertensive dipeptide, Val-Tyr (281...
  95. doi Disturbed intestinal nitrogen homeostasis in a mouse model of high-fat diet-induced obesity and glucose intolerance
    Thi Thu Huong Do
    Universite Pierre et Marie Curie, Paris, Unité mixte de recherche S938, Paris, France
    Am J Physiol Endocrinol Metab 306:E668-80. 2014
    The oligopeptide transporter peptide cotransporter-1 Slc15a1 (PEPT1) plays a major role in the regulation of nitrogen supply, since it is responsible for 70% of the dietary nitrogen absorption...
  96. pmc Intestinal deletion of leptin signaling alters activity of nutrient transporters and delayed the onset of obesity in mice
    Annabelle Tavernier
    Institut National de la Santé et de la Recherche Médicale INSERM Unité Mixte de Recherche en Santé UMRS 1149, Unité de Formation et de Recherche UFR de Médecine Paris Diderot, Sorbonne Paris Cité, Paris, France
    FASEB J 28:4100-10. 2014
    ..cotransporter SGLT-1 and GLUT2 were unaffected in LEPR-B-KO jejunum, while GLUT5-mediated fructose transport and PepT1-mediated peptide transport were substantially reduced (P<0.01)...
  97. doi Downregulation of duodenal SLC transporters and activation of proinflammatory signaling constitute the early response to high altitude in humans
    Kacper A Wojtal
    Division of Gastroenterology and Hepatology, Department of Internal Medicine, University Hospital Zurich, Zurich, Switzerland
    Am J Physiol Gastrointest Liver Physiol 307:G673-88. 2014
    ..1/2 (CNT1/2), organic anion transporting polypeptide 2B1 (OATP2B1), organic cation transporter 2 (OCTN2), peptide transporter 1 (PEPT1), serotonin transporter (SERT), and higher levels of IFN-γ, IL-6, and IL-17A...
  98. pmc Duodenum has the greatest potential to absorb soluble non-ammonia nitrogen in the nonmesenteric gastrointestinal tissues of dairy cows
    Ying ming Xie
    Institute of Dairy Science, MOE Key Laboratory of Molecular Animal Nutrition, College of Animal Sciences, Zhejiang University, Hangzhou 310058, China
    J Zhejiang Univ Sci B 16:503-10. 2015
    ..This work was designed to investigate the expression of the peptide transporter PepT1 and the AA transporters ASCT2, y(+)LAT1, and ATB(0,+), and the concentrations of PBAA, FAA, and soluble protein in ..
  99. doi Taste and move: glucose and peptide transporters in the gastrointestinal tract
    Hannelore Daniel
    Nutritional Physiology, Technische Universitat Munchen, 85350, Freising, Germany
    Exp Physiol 100:1441-50. 2015
    ..is mediated by the Na(+)-dependent SGLT1 protein, uptake of short-chain peptides is mediated by the H(+)-coupled PEPT1 protein...
  100. pmc Generation of enterocyte-like cells from human induced pluripotent stem cells for drug absorption and metabolism studies in human small intestine
    Tatsuya Ozawa
    Laboratory of Biochemistry and Molecular Biology, Graduate School of Pharmaceutical Sciences, Osaka University, Osaka 565 0871, Japan
    Sci Rep 5:16479. 2015
    ..The gene expression levels of cytochrome P450 3A4 (CYP3A4) and peptide transporter 1 in the hiPS-ELCs were higher than those in Caco-2 cells...
  101. pmc Species differences in the pharmacokinetics of cefadroxil as determined in wildtype and humanized PepT1 mice
    Yongjun Hu
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, MI, USA Electronic address
    Biochem Pharmacol 107:81-90. 2016
    PepT1 (SLC15A1) is a high-capacity low-affinity transporter that is important in the absorption of digested di/tripeptides from dietary protein in the small intestine...

Research Grants29

  1. Cranberry: Interactions with Anti-infectious Agents
    Gail Anderson; Fiscal Year: 2005
    ..The intestinal absorption of many beta-lactam antibiotics is mediated by peptide transporters (e.g. PepT1) and possibly OATP...
  2. Role and Relevance of Pept1 in Drug Absorption, Disposition, and Dynamics
    David E Smith; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): PEPT1, a proton-coupled oligopeptide transporter (POT) of the SLC15 family, has nutritional importance because of its intestinal absorption of small peptides from the diet and because of its ..
  3. AMINOKETONE INHIBITORS OF THE DOPAMINE TRANSPORTER
    JOHN REINHARD; Fiscal Year: 2005
    ..if the ester conjugates can be taken up into caco-2 cells (by hPEPT1 and 2)...
  4. PEPT1: STRUCTURE-FUNCTION, SORTING AND MODULATION
    IAN HAWORTH; Fiscal Year: 2003
    ..We will test the hypothesis that specific amino acid residues in hPepT1 determine substrate and H+ translocation, trafficking of the transporter protein, and its modulation...
  5. High-Throughput Assay for the Intestinal Peptide Transporter
    Peter Swaan; Fiscal Year: 2005
    ..our proposed research on a pharmacologically relevant transport system, the small intestinal peptide transporter (PepT1)...
  6. Meropenem Prodrugs for XDR-TB
    Rory P Remmel; Fiscal Year: 2013
    ..esters (proxetil, suberolyl prodrugs) 2) Synthesize valeryl or dipeptidyl esters that are taken up by PepT1, an intestinal dipeptide transporter and 3) Prepare a bivalent prodrug that releases meropenem and clavulanate ..
  7. HPEPT1 IN INTESTINAL INFLAMMATION
    Didier Merlin; Fiscal Year: 2009
    ..products, such as fMLP and MDP, could be transported by the intestinal epithelial oligopeptide transporter, PepT1. Once taken up into the cytosol, these small bacterial peptides initiate an inflammatory response...
  8. Role and Regulation of Intestinal Na/H Exchanger
    Eugene Chang; Fiscal Year: 2007
    ..with other transporters such as the anion exchanger, DRA (Down-Regulated in Adenoma), the dipeptidy1 transporter hPepT1, adaptor proteins (E3KARP and NHERF), and other key molecules such as v- and t-SNARES required for membrane endo- ..
  9. PEPTIDOMIMETIC DRUGS--SUBSTRATES FOR PEPTIDE TRANSPORTER
    Malliga Ganapathy; Fiscal Year: 2000
    ..The intestinal peptide transporter, PEPT1, is of the low-affinity/high-capacity type whereas the primary transporter in the kidney, PEPT2, is of the high- ..
  10. Models for Screening Intestinal Transporter Prodrugs
    PHILLIP KISH; Fiscal Year: 2002
    ..g., the human dipeptide transporter or hpepT1) in order to cross the cell membrane and be absorbed into the body...
  11. MOLECULAR BIOLOGY OF BRUSH BORDER TRANSPORT PROTEINS
    Matthias Hediger; Fiscal Year: 1999
    ..and epithelial high affinity glutamate transporter EAAC1, the intestinal H+-coupled oligopeptide transporter PepT1 and its renal isoform hPepT2, and the renal facilitated urea transporter UT2...
  12. PROTEIN NUTRITION PEPTIDE TRANSPORT IN GUT AND KIDNEY
    FREDERICK LEIBACH; Fiscal Year: 2001
    ..A major portion of the studies proposed will be carried out using two recently cloned human peptide transporters, hPEPT1 and 2...
  13. DRUG ABSORPTION VIA THE PEPTIDE TRANSPORTER IN THE EYE
    Vincent Lee; Fiscal Year: 2002
    ..could be improved through derivatization into prodrugs that are substrates for the H+-dipeptide transporters (PepT1/PepT2)...
  14. DIET/GROWTH FACTOR MECHANISMS OF GUT ADAPTATION
    Thomas Ziegler; Fiscal Year: 2004
    ..important in gut adaption after massive small bowel resection, include the brush border di-/tripeptide transporter PepT1, glucagon-like peptide-2 (GLP-2), insulin-like growth factor-1 (IGF-1), intestinal trefoil factor, and ..
  15. Intestinal PepT1 in Health and Disease
    Didier Merlin; Fiscal Year: 2010
    ..Consistent with these findings, hPepT1 is expressed in the small intestine-like cell line Caco2-BBE but not in the colonic-like cell line HT29-Cl.19A...
  16. HPEPT1 IN INTESTINAL INFLAMMATION
    Didier Merlin; Fiscal Year: 2003
    ..The general aim of this proposal is to better understand expression of the intestinal epithelial transporter hPepT1 and its consequences for neutrophil-epithelial interactions. Specifically this proposal has five major aims...
  17. HPEPT1 IN INTESTINAL INFLAMMATION
    Didier Merlin; Fiscal Year: 2008
    ..hl?epT1; ii) hPepTl-r/iediated epithelial transport of fMLP enhances neutrophil-epithelial interactions; iii) hPepT1 can be aberrantly expressed in the colon under inflammatory states sueb as chronic ulcerative colitis and Crohn&..
  18. Mechanisms of Adaptation in Human Short Bowel Syndrome
    Thomas Ziegler; Fiscal Year: 2005
    ..The patients also demonstrate up-regulated expression of the di/tripeptide transporter PepT1 in colonic mucosa versus controls, suggesting a functional mechanism for endogenous gut adaptation...
  19. SHARED INSTRUMENTATION GRANT
    Zsolt Szabo; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  20. REGULATION OF NA-NUTRIENT CO-TRANSPORT
    UMA SUNDARAM SUNDARAM; Fiscal Year: 2010
    ..This knowledge will provide the basis for new and more efficacious treatment modalities for the most common morbidities of IBD specifically, malabsorption, diarrhea and malnutrition. ..
  21. PHARMACOKINETICS AND FETAL EXPOSURE TO NARCOTICS
    Hazel Szeto; Fiscal Year: 2002
    ..The proposed studies will provide new information on the functional roles of opiate receptor subtypes in the fetus, and should be helpful in the design of better analgesics for perinatal use. ..
  22. Endothelin Receptor Imaging of Cancer with PET
    Zsolt Szabo; Fiscal Year: 2007
    ..They have the potential to improve selection of cancer patients for treatment with endothelin antagonists. [unreadable] [unreadable] [unreadable]..
  23. Molecular Analysis of a Novel Opioid Peptide Transporter
    Vadivel Ganapathy; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  24. PET IMAGING OF THE 5HT TRANSPORTER IN ALCOHOLISM
    Zsolt Szabo; Fiscal Year: 2003
    ..The results of this project will lead to better understanding of the role of serotonin in the biological vulnerability for alcoholism and may lead to improved approaches to prevent and treat alcoholism. ..
  25. Mitoprotective and antioxidant peptides for DM treatment
    Hazel Szeto; Fiscal Year: 2006
    ..abstract_text> ..
  26. AMINO ACID TRANSPORTER B: PHARMACOLOGY & THERAPEUTIC USE
    Malliga Ganapathy; Fiscal Year: 2006
    ....
  27. Cell-Permeable Peptides for Mitochondrial Protection
    Hazel Szeto; Fiscal Year: 2005
    ..Potential collaborators for the animal studies have already been identified. ..
  28. CARNITINE TRANSPORTERS: STRUCTURE, FUNCTION & REGULATION
    Vadivel Ganapathy; Fiscal Year: 2003
    ..laevis oocytes. The regulation studies will be carried out in intact animals using the rat as a model and also in cultured cells of human origin. ..
  29. Immune Tolerance; Sigma Receptor as a Therapeutic Target
    Vadivel Ganapathy; Fiscal Year: 2003
    ....