Thyrotropin releasing hormone analogs: A building block approach to the construction of tetracyclic peptidomimetics

被引：17

作者：

Chu, WH

Perlman, JH

Gershengorn, MC

Moeller, KD ^{[1
]}

机构：

[1] Washington Univ, Dept Chem, St Louis, MO 63130 USA

[2] Cornell Univ, Coll Med, Dept Med, Div Mol Med, New York, NY 10021 USA

[3] New York Hosp, New York, NY 10021 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(98)00567-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A building block based approach was used to synthesize a pair of tetracyclic peptidomimetics that constrain all but one of the rotational degrees of freedom of the hypothalamic tripeptide hormone thyroliberin. One of the analogs bound to the thyroliberin endocrine receptor (TRH-R) with an affinity greater than that of an analog without constraints. The tetracyclic peptidomimetics were found to be partial agonists for the TRH-R receptor. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3093 / 3096

页数：4

共 27 条

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