Literature DB >> 18374571

Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1).

Praveen M Bahadduri1, Abhijit Ray, Akash Khandelwal, Peter W Swaan.   

Abstract

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. At least four labeled peptides show potent inhibitory activity toward hPEPT1-mediated uptake of [(3)H]-GlySar and three compounds displayed a significant cellular uptake specifically mediated by hPEPT1.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18374571      PMCID： PMC2396585          DOI： 10.1016/j.bmcl.2008.03.044

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Conjugation of dipeptide to fluorescent dyes enhances its affinity for a dipeptide transporter (PEPT1) in human intestinal Caco-2 cells.

Authors:  H Abe; M Satoh; S Miyauchi; S Shuto; A Matsuda; N Kamo
Journal:  Bioconjug Chem       Date:  1999 Jan-Feb       Impact factor: 4.774

2.  Molecular determinants of recognition for the intestinal peptide carrier.

Authors:  P W Swaan; J J Tukker
Journal:  J Pharm Sci       Date:  1997-05       Impact factor: 3.534

3.  Single-dose pharmacokinetics of valganciclovir in HIV- and CMV-seropositive subjects.

Authors:  D Jung; A Dorr
Journal:  J Clin Pharmacol       Date:  1999-08       Impact factor: 3.126

4.  In vitro and pharmacophore-based discovery of novel hPEPT1 inhibitors.

Authors:  Sean Ekins; Jeffrey S Johnston; Praveen Bahadduri; Vanessa M D'Souza; Abhijit Ray; Cheng Chang; Peter W Swaan
Journal:  Pharm Res       Date:  2005-04-07       Impact factor: 4.200

5.  Intestinal peptide transport: ex vivo uptake studies and localization of peptide carrier PEPT1.

Authors:  D A Groneberg; F Döring; P R Eynott; A Fischer; H Daniel
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2001-09       Impact factor: 4.052

6.  7-Amino-4-methyl-6-sulfocoumarin-3-acetic acid: a novel blue fluorescent dye for protein labeling.

Authors:  W Y Leung; P A Trobridge; R P Haugland; R P Haugland; F Mao
Journal:  Bioorg Med Chem Lett       Date:  1999-08-02       Impact factor: 2.823

7.  Three-dimensional quantitative structure-activity relationship analyses of peptide substrates of the mammalian H+/peptide cotransporter PEPT1.

Authors:  Sabine Gebauer; Ilka Knütter; Bianka Hartrodt; Matthias Brandsch; Klaus Neubert; Iris Thondorf
Journal:  J Med Chem       Date:  2003-12-18       Impact factor: 7.446

8.  A fluorescent hPept1 transporter substrate for uptake screening.

Authors:  Christopher P Landowski; Hyo-kyung Han; Kyung-Dall Lee; Gordon L Amidon
Journal:  Pharm Res       Date:  2003-11       Impact factor: 4.200

9.  Pharmacokinetics of the acyclovir pro-drug valaciclovir after escalating single- and multiple-dose administration to normal volunteers.

Authors:  S Weller; M R Blum; M Doucette; T Burnette; D M Cederberg; P de Miranda; M L Smiley
Journal:  Clin Pharmacol Ther       Date:  1993-12       Impact factor: 6.875
  9 in total
  1 in total

Review 1.  Bioavailability through PepT1: the role of computer modelling in intelligent drug design.

Authors:  David W Foley; Jeyaganesh Rajamanickam; Patrick D Bailey; David Meredith
Journal:  Curr Comput Aided Drug Des       Date:  2010-03       Impact factor: 1.606
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.