Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists

被引：5
|
作者：
Misu, Ryosuke [1 ]
Noguchi, Taro [1 ]
Ohno, Hiroaki [1 ]
Oishi, Shinya [1 ]
Fujii, Nobutaka [1 ]
机构：
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 08期
关键词：
Neurokinin B; MePhe(7)]-neurokinin B; NK3R; Tachykinin; GnRH; METASTASIS-SUPPRESSOR GENE; PROTEIN-COUPLED RECEPTOR; PULSE-GENERATOR ACTIVITY; KISSPEPTIN NEURONS; ARCUATE NUCLEUS; SUBSTANCE-P; HORMONE SECRETION; DYNORPHIN-A; FEMALE RAT; KISS-1;
D O I：
10.1016/j.bmc.2013.01.036
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). NKB with the consensus sequence of the tachykinin peptide family also binds to other tachykinin receptors [neurokinin-1 receptor (NK1R) and neurokinin-2 receptor (NK2R)] with low selectivity. In order to identify the structural requirements for the development of novel potent and selective NK3R agonists, a structure-activity relationship (SAR) study of [MePhe(7)]-NKB and other naturally occurring tachykinin peptides was performed. The substitutions to naturally occurring tachykinins with Asp and MePhe improved the receptor binding and agonistic activity for NK3R. The corresponding substitutions to NKB provided an NK3R selective analog. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2413 / 2417
页数：5
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