新型配体 MRGPRX1-孤啡肽 LVV-H7 和 VV-H7 的分离。

Isolation of new ligands for orphan receptor MRGPRX1-hemorphins LVV-H7 and VV-H7.

机构信息

Research Unit of Biomedicine, University of Oulu, Oulu, Finland; Biocenter Oulu, University of Oulu, Oulu, Finland.

Okinawa Institute of Science and Technology Graduate University, Tancha, Onna-son, Okinawa, Japan.

出版信息

Peptides. 2017 Oct;96:61-66. doi: 10.1016/j.peptides.2017.08.011. Epub 2017 Sep 1.

DOI:10.1016/j.peptides.2017.08.011

PMID:28867075

Abstract

The human MAS-related G protein-coupled receptor X1 (MRGPRX1) is a member of the GPCR family. The receptor is primate specific and expressed in the sensory neurons of dorsal root ganglion and trigeminal ganglion, where it is considered to be involved in the pain perception. The MRGPRX1 has unusual binding mechanism, as it is activated by several different ligands as well as several different fragments of precursor proteins. Thus, we hypothesize that it is activated by several unknown compounds as well since the receptor is still classified as orphan. Here, we describe the isolation of two novel endogenous ligands for the MRGPRX1 from human platelet preparation. The isolated ligands are hemoglobin β-chain fragments, known members of the hemorphin family.

摘要

人类 MAS 相关 G 蛋白偶联受体 X1（MRGPRX1）是 GPCR 家族的一员。该受体是灵长类动物特有的，表达于背根神经节和三叉神经节的感觉神经元中，被认为参与疼痛感知。MRGPRX1 具有不寻常的结合机制，因为它被多种不同的配体以及几种不同的前体蛋白片段激活。因此，我们假设它也被几种未知的化合物激活，因为该受体仍被归类为孤儿受体。在这里，我们描述了从人血小板制剂中分离出的两种新型 MRGPRX1 内源性配体。分离出的配体是血红蛋白β链片段，已知属于血红蛋白家族。