• Title of article

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

  • Author/Authors

    Praveen M. Bahadduri، نويسنده , , Abhijit Ray، نويسنده , , Akash Khandelwal، نويسنده , , Peter W. Swaan، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    3
  • From page
    2555
  • To page
    2557
  • 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 [3H]-GlySar and three compounds displayed a significant cellular uptake specifically mediated by hPEPT1.
  • Keywords
    fluorescence , CoMFA , Transporter , Alexa Fluor 350™ , hPEPT1 , Peptide conjugation , High-throughput screening
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Serial Year
    2008
  • Journal title
    Bioorganic & Medicinal Chemistry Letters
  • Record number

    799399