Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1).
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.
Bahadduri
Praveen M
PM
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA.
Ray
Abhijit
A
Khandelwal
Akash
A
Swaan
Peter W
PW
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D000074011:Peptide Transporter 1; D010455:Peptides / Q000737:chemistry*; D027981:Symporters / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*
D005456:Fluorescent Dyes; D000074011:Peptide Transporter 1; D010455:Peptides; C082186:SLC15A1 protein, human; D027981:Symporters