Proceedings of the Symposium on Progress in Organic Reactions and Syntheses
31th Synposium on Progress in Organic Reactions and Syntheses
Session ID : 1P-36
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Host: Division of Organic Chemistry, The Pharmaceutical Society of Japan

Investigation of Structural Requirements of Peptide Transporter (PEPT1) Substrates Utilizing Various Alkene Type Dipeptide Isosteres
*Ayumu Niida, Kenji Tomita, Hiroaki Tanigaki, Nobutaka Fujii, Hirokazu Tamamura, Akira Otaka, Tomohiro Terada, Ken-ichi Inui
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Keywords: peptide mimetics, alkene dipeptide isosteres, organocopper, PEPT1
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Abstract

We described new synthetic routes for (Z)-alkene or (E)-fluoroalkene dipeptide isosteres as cis-amide equivalents and application of the synthetic dipeptide isosteres to probe structural requirement of peptide transporter (PEPT1). We evaluated affinities of synthetic Phe-Gly derivatives for human di/tripeptide transporter, PEPT1. In this experiment, trans-amide isosteres exhibited superior affinities for PEPT1 compared to cis-amide equivalents. This result suggested that PEPT1 predominantly recognizes trans-amide conformations of dipeptides.

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© 2005 The Pharmaceutical Society of Japan
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