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

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2555-7. doi: 10.1016/j.bmcl.2008.03.044. Epub 2008 Mar 20.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Drug Design*
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / chemistry
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Peptide Transporter 1
  • Peptides / chemistry*
  • Symporters / chemistry
  • Symporters / genetics
  • Symporters / metabolism*

Substances

  • Fluorescent Dyes
  • Peptide Transporter 1
  • Peptides
  • SLC15A1 protein, human
  • Symporters