Yoshida Morikatsu, Miyazato Mikiya, Kangawa Kenji
Department of Biochemistry, National Cerebral and Cardiovascular Center Research Institute, Suita, Osaka, Japan.
Methods Enzymol. 2012;514:33-44. doi: 10.1016/B978-0-12-381272-8.00002-7.
G protein-coupled receptors (GPCRs) constitute the largest family of cell-surface receptors. These proteins play a crucial role in physiology by facilitating cell communication through recognition of diverse ligands, including bioactive peptides, amines, nucleosides, and lipids. The human genome sequencing project identified more than 100 orphan GPCRs, whose ligands had not yet been discovered. We subsequently identified ghrelin, neuromedin U, and neuromedin S as endogenous ligands of various orphan GPCRs and have proposed various mechanisms through which these peptides regulate physiological functions through their cognate GPCRs. In this chapter, we review methods for identifying novel peptide ligands of orphan GPCRs.
G蛋白偶联受体（GPCRs）构成了细胞表面受体的最大家族。这些蛋白质通过识别多种配体（包括生物活性肽、胺、核苷和脂质）来促进细胞通讯，从而在生理学中发挥关键作用。人类基因组测序计划鉴定出了100多种孤儿GPCR，其配体尚未被发现。随后，我们鉴定出胃饥饿素、神经介素U和神经介素S为各种孤儿GPCR的内源性配体，并提出了这些肽通过其同源GPCR调节生理功能的各种机制。在本章中，我们综述了鉴定孤儿GPCR新型肽配体的方法。
