Comparison of N-terminal modifications on neurotensin (8− 13) analogues correlates peptide stability but not binding affinity with in vivo efficacy

KS Orwig, MKR Lassetter, MK Hadden…

Index: Orwig, Kevin S.; Lassetter, McKensie R.; Hadden, M. Kyle; Dix, Thomas A. Journal of Medicinal Chemistry, 2009 , vol. 52, # 7 p. 1803 - 1813

Full Text: HTML

Citation Number: 24

Abstract

Neurotensin (8− 13) and two related analogues were used as model systems to directly compare various N-terminal peptide modifications representing both commonly used and novel capping groups. Each N-terminal modification prevented aminopeptidase cleavage but surprisingly differed in its ability to inhibit cleavage at other sites, a phenomenon attributed to long-range conformational effects. None of the capping groups were ...