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

被引：5

作者：

Bahadduri, Praveen M. ^{[1
]}

Ray, Abhijit ^{[1
]}

Khandelwal, Akash ^{[1
]}

Swaan, Peter W.

机构：

[1] Univ Maryland, Sch Pharm, Dept Pharmaceut Sci, Baltimore, MD 21201 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 08期

关键词：

Alexa fluor 350 (TM); hPEPT1; peptide conjugation; fluorescence; high-throughput screening; CoMFA; transporter;

D O I：

10.1016/j.bmcl.2008.03.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We employed a computational approach to design and synthesize a series of. fluorescently labeled hPEPT1 substrates. Five Alexa Fluor-350 (TM)-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 [H-3]-GlySar and three compounds displayed a significant cellular uptake specifically mediated by hPEPT1. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2555 / 2557

页数：3

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