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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
