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ID: ALA1144795

Journal: Bioorg Med Chem Lett

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

Authors: Bahadduri PM, Ray A, Khandelwal A, Swaan PW.

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.

CiteXplore: 18374571

DOI: 10.1016/j.bmcl.2008.03.044