M871 -: A novel peptide antagonist selectively recognizing the galanin receptor type 2
M871 -: A novel peptide antagonist selectively recognizing the galanin receptor type 2
复制标题
DOI：
10.1007/s10989-005-9008-x
复制
发表时间：
2006-06-01
影响因子：
2.5
通讯作者：
Langell, U.
中科院分区：
文献类型：
--
作者：
Sollenberg, U. E.;Lundstrom, L.;Langell, U.
甘丙肽及其三种受体与多种生理过程有关，分布于中枢和外周神经系统。甘丙肽激活的信号传导系统的性质的进一步知识可以最好地获得的肽和非肽配体的可用性，是选择性的不同受体亚型。本研究描述了嵌合肽甘丙肽-（2-13）Glu-His-（Pro）（3）-（Ala-Leu）（2）-Ala-酰胺（M871）的结合和信号数据。该化合物与甘丙肽受体2型结合的亲和力比与甘丙肽受体I型结合的亲和力高30倍以上，并对甘丙肽受体2型表现出拮抗作用，阻断CHO细胞中甘丙肽产生的磷酸肌醇释放增加。这种肽为甘丙肽受体生理学的研究开辟了新的可能性。
Galanin and its three receptors have been linked to a wide variety of physiological processes and are distributed in both the central and peripheral nervous systems. Further knowledge of the properties of galanin-activated signaling systems can best be obtained by the availability of peptide and non-peptide ligands that are selective for the different receptor subtypes. The current study describes binding and signaling data for the chimeric peptide, galanin-(2-13)Glu-His-(Pro)(3)-(Ala-Leu)(2)-Ala-amide (M871). This compound binds to the galanin receptor type 2 with more than 30-fold higher affinity than to the galanin receptor type I and exhibits antagonist actions at galanin receptor type 2, blocking increased release of inositol phosphate produced by galanin in CHO cells. This peptide opens new possibilities for the study of galanin receptor physiology.