期刊
JOURNAL OF PHARMACOLOGICAL SCIENCES
卷 126, 期 4, 页码 302-309出版社
JAPANESE PHARMACOLOGICAL SOC
DOI: 10.1254/jphs.14R13CP
关键词
G protein-coupled receptor; cellular dielectric spectroscopy; electrical impedance-based biosensor; CellKey (TM) system; GPCR assay method
资金
- Ministry of Education, Culture, Sports, Science and Technology of Japan [25860199, 25860200, 24590740, 25462442]
- Yokoyama Foundation for Clinical Pharmacology
- Foundation for Promotion of Cancer Research in Japan
- Tsumura Co.
- Daiichi Sankyo Co., Ltd.
- Showa Yakuhin Kako Co., Ltd.
- Grants-in-Aid for Scientific Research [24590740, 25860200, 25870461, 25860199, 25462442] Funding Source: KAKEN
The G protein-coupled receptors (GPCRs) form the largest and the most versatile superfamily that share a seven-transmembrane-spanning architecture. GPCR-signaling is involved in vision, taste, olfaction, sympathetic/parasympathetic nervous functions, metabolism, and immune regulation, indicating that GPCRs are extremely important therapeutic targets for various diseases. Cellular dielectric spectroscopy (CDS) is a novel technology that employs a label-free, real-time and cell-based assay approach for the comprehensive pharmacological evaluation of cells that exogenously or endogenously express GPCRs. Among the biosensors that use CDS technology, the CellKey (TM) system not only detects the activation of GPCRs but also distinguishes between signals through different subtypes of the Go protein (Gs, Gi/o, and Gq). In this review, we discuss the traditional assays and then introduce the principles by which the CellKey (TM) system evaluates GPCR activation, followed by a perspective on the advantages and future prospects of this system.
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