摘要
随着荧光成像技术的迅速发展,用于研究配体-受体相互作用的荧光技术的稳健性导致了一系列新型荧光配体的问世。既要考虑到受体配体的高亲和性,同时兼顾观察二者甚至在单个细胞水准上相互作用的荧光性能,这大大激发了研究人员在GPCR配体领域的研究兴趣。另外,由于这类配体在非药理性方面的优势及其使用的技术,荧光配体作为一种药理学工具日益用于GRCRs研究。本文,基于2007年以来文献在荧光GPCR领域的小分子、非肽类配体描述的结果,我们从受体亲和力、标记小分子的荧光基团及其在GPCR研究方面的荧光特性和应用对进行了报导。
关键词: 二聚物 ,荧光性,荧光配体,荧光素,蛋白偶联受体,低聚体
Current Medicinal Chemistry
Title:Fluorescent GPCR Ligands as New Tools in Pharmacology-Update, Years 2008- Early 2014
Volume: 21 Issue: 34
Author(s): Kamil J. Kuder and Katarzyna Kiec-Kononowicz
Affiliation:
关键词: 二聚物 ,荧光性,荧光配体,荧光素,蛋白偶联受体,低聚体
摘要: The robust of fluorescent techniques to study the ligand-receptor interaction followed by rapidly developing fluorescence imaging techniques resulted in a burst of the novel fluorescent ligands development. Taking into consideration not only ligand’s high affinity to the receptor, but also their fluorescent properties to visualize the interaction even in the single cell level, gives the researchers a strong impulse to investigate that field of GPCR ligands. Moreover, paying attention to the “non pharmacological” advantages of these ligands, as well as the techniques to be used, fluorescent ligands become commonly used pharmacological tools to study GPCRs. Herein we report on the results described in the literature since late 2007 in the field of the fluorescent GPCR small, non-peptide ligands according the receptor affinity, fluorophores that has been used to tag the molecules and their fluorescent properties as well as their application in GPCR research.
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Cite this article as:
Kuder J. Kamil and Kiec-Kononowicz Katarzyna, Fluorescent GPCR Ligands as New Tools in Pharmacology-Update, Years 2008- Early 2014, Current Medicinal Chemistry 2014; 21 (34) . https://dx.doi.org/10.2174/0929867321666140826120058
DOI https://dx.doi.org/10.2174/0929867321666140826120058 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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