利用哺乳动物细胞和酵母细胞研究低聚物形态G蛋白偶联受体的技术现状

Title:Current Techniques for Studying Oligomer Formations of G-Protein-Coupled Receptors Using Mammalian and Yeast Cells

Volume: 23 Issue: 16

Author(s): Yasuyuki Nakamura, Jun Ishii, Akihiko Kondo

Affiliation:

关键词: G蛋白偶联受体，齐聚，共振能量转移，酿酒酵母，双杂交系统，报告基因检测，药物发现。

摘要: G-protein-coupled receptors (GPCRs) are physiologically important transmembrane proteins that sense signaling molecules such as hormones, neurotransmitters, and various sensory stimuli; GPCRs represent major molecular targets for drug discovery. Although GPCRs traditionally have been thought to function as monomers or homomers, in the recent years these proteins have also been shown to function as heteromers. Heteromerization among GPCRs is expected to generate potentially large functional and physiological diversity and to provide new opportunities for drug discovery. However, due to the existence of numerous combinations, the larger universe of possible GPCR heteromers is unknown, and thus its functional significance is still poorly understood. The oligomerization of GPCRs in living cells now has been demonstrated in mammalian cells and in native tissues by using genetic, biochemical, and physiological approaches, as well as various resonance energy transfer (RET) technologies. In addition, the yeast Saccharomyces cerevisiae, which can serve as a biosensor for monitoring eukaryotic biological processes, can also be used for the identification of functionally significant heteromer pairs of GPCRs. In this review, we focus on studies of GPCR oligomers, and summarize the technologies used to evaluate GPCR oligomerization. We additionally consider the potential limitations of these methods at present, and envision the possible future applications of these techniques.

Cite this article as:

Yasuyuki Nakamura, Jun Ishii, Akihiko Kondo , Current Techniques for Studying Oligomer Formations of G-Protein-Coupled Receptors Using Mammalian and Yeast Cells, Current Medicinal Chemistry 2016; 23 (16) . https://dx.doi.org/10.2174/0929867323666160407113353