Predicting the Antinociceptive Efficacy of σ1 Receptor Ligands by a Novel Receptor Fluorescence Resonance Energy Transfer (FRET) Based Biosensor

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• 作者：Maricel Gómez-Soler ; Víctor Fernández-Due?as ; Enrique Portillo-Salido ; Pilar Pérez ; Daniel Zamanillo ; José Miguel Vela ; Javier Burgue?o ; Francisco Ciruela
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：January 9, 2014
• 年：2014
• 卷：57
• 期：1
• 页码：238-242
• 全文大小：251K
• ISSN：1520-4804

文摘

We have developed a novel methodology for monitoring the 蟽₁ receptor activation switch in living cells. Our assay uncovered the intrinsic nature of 蟽₁ receptor ligands by recording the ligand-mediated conformational changes of this chaperone protein. The change triggered by each ligand correlated well with its ability to attenuate formalin induced nociception in an animal model of pain. This tool may assist in predicting the antinociceptive efficacy of 蟽₁ receptor ligands.