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三种降钙素受体刺激肽的结构与生物学特性,降钙素基因相关肽家族的新成员

Structure and biological properties of three calcitonin receptor-stimulating peptides, novel members of the calcitonin gene-related peptide family.

作者信息

Katafuchi Takeshi, Minamino Naoto

机构信息

Department of Pharmacology, National Cardiovascular Center Research Institute, 5-7-1 Fujishirodai, Suita, 565-8565 Osaka, Japan.

出版信息

Peptides. 2004 Nov;25(11):2039-45. doi: 10.1016/j.peptides.2004.08.013.

DOI:10.1016/j.peptides.2004.08.013
PMID:15501538
Abstract

In this review, we describe the structure and biological properties of calcitonin receptor-stimulating peptide-1 (CRSP-1), CRSP-2 and CRSP-3, the novel members of the CGRP family. CRSP-1, which has been identified in the pig, cow, dog, and horse, is a specific ligand for the calcitonin (CT) receptor, and porcine CRSP-1 elicits a 100-fold greater effect on a recombinant porcine CT receptor than porcine CT, although this peptide has high structural similarity with CGRP. CRSP-1 is expressed and synthesized mainly in the central nervous system (CNS), pituitary and thyroid gland. In an in vivo experiment, bolus administration of CRSP-1 into rats reduced the plasma calcium concentration, but did not alter blood pressure, indicating its action as a CT receptor agonist in the peripheral circulation. In the CNS, CRSP-1 is also deduced to be an endogenous agonist for the CT receptor. CRSP-2 has been identified in the pig and dog, and CRSP-3 has been identified only in the pig. They are expressed and synthesized mainly in the CNS and thyroid gland. However, their endogenous molecular forms, receptors, and biological activity remain unidentified.

摘要

在本综述中,我们描述了降钙素基因相关肽(CGRP)家族的新成员——降钙素受体刺激肽-1(CRSP-1)、CRSP-2和CRSP-3的结构和生物学特性。已在猪、牛、狗和马中鉴定出的CRSP-1是降钙素(CT)受体的特异性配体,尽管该肽与CGRP具有高度的结构相似性,但猪CRSP-1对重组猪CT受体的作用比猪CT强100倍。CRSP-1主要在中枢神经系统(CNS)、垂体和甲状腺中表达和合成。在一项体内实验中,向大鼠推注CRSP-1可降低血浆钙浓度,但不改变血压,表明其在外周循环中作为CT受体激动剂的作用。在中枢神经系统中,CRSP-1也被推断为CT受体的内源性激动剂。已在猪和狗中鉴定出CRSP-2,仅在猪中鉴定出CRSP-3。它们主要在中枢神经系统和甲状腺中表达和合成。然而,它们的内源性分子形式、受体和生物学活性仍未明确。

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引用本文的文献

1
Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25.降钙素/CGRP 肽家族药理学的最新进展:IUPHAR 评论 25。
Br J Pharmacol. 2018 Jan;175(1):3-17. doi: 10.1111/bph.14075. Epub 2017 Nov 28.