Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities

被引：7

作者：

Lundquist, JT

Büllesbach, EE

Dix, TA

机构：

[1] Med Univ S Carolina, Dept Pharmaceut Sci, Charleston, SC 29425 USA

[2] Med Univ S Carolina, Dept Biochem & Mol Biol, Charleston, SC 29425 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)00018-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recent evidence is consistent with neurotensin (NT)(8-13) adopting a Type I beta-turn conformation while binding the NT receptor, which would place the cationic side-chains of Arg(8) and Arg(9) in close proximity. This was the basis for the design, synthesis and analysis of truncated NT(9-13) analogues 1-5 with dicationic position 9 side-chains to emulate the functions of the 8 and 9 side-chains of NT(8-13). (C) 2000 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：453 / 455

页数：3

共 18 条

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[2] PHARMACOLOGICAL AND BIOCHEMICAL PROFILES OF UNIQUE NEUROTENSIN-8-13 ANALOGS EXHIBITING SPECIES SELECTIVITY, STEREOSELECTIVITY, AND SUPERAGONISM [J].