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2016 Fiscal Year Final Research Report

Screening for peptide ligands that activate beta-arrestin biasd cell signaling of orphan GPCRs

Research Project

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Project/Area Number 26460333
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field General pharmacology
Research InstitutionThe University of Tokyo

Principal Investigator

Kumagai Hidetoshi  東京大学, 医学部附属病院, 特任助教 (20281008)

Co-Investigator(Renkei-kenkyūsha) YANAGISAWA Masashi  国際統合睡眠医科学研究機構, 教授 (20202369)
Project Period (FY) 2014-04-01 – 2017-03-31
KeywordsGPCR / Gタンパク質 / β-アレスチン / 生理活性ペプチド
Outline of Final Research Achievements

Our purpose of this study is to identify endogenouse ligands for orphan GPCRs by newly developed screening systems. We utilized two intracellular signaling pathways, G-proteins and β-arrestin for detection of GPCR activation. To detect β-arrestin signaling, we monitored the ligand activated GPCR-mediated β-arrestin recruitment by using enzymatic complementation of E. coli β-galactosidase, alpha and omega fragments. In terms of detection of G-protein signaling, we generated a new technology that simply monitoring activities of any G-protein alpha subunits leading to minimization of experimental steps. We have optimized these assay systems suitable for high through put screening and being conducting the screening.

Free Research Field

分子薬理学

URL: 

Published: 2018-03-22  

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