Cellular fluorescent high-throughput screening assays of the ATP-gated P2X7 receptorReport as inadecuate




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Chinese Science Bulletin

, Volume 58, Issue 23, pp 2812–2819

First Online: 07 June 2013Received: 05 June 2012Accepted: 17 September 2012DOI: 10.1007-s11434-013-5870-7

Cite this article as: Jiang, Y., Yin, Q. & Li, S. Chin. Sci. Bull. 2013 58: 2812. doi:10.1007-s11434-013-5870-7

Abstract

The P2X7 receptor P2X7R is an important member of the P2X family of ligand-gated ion channels that respond to ATP as the endogenous agonist. Studies suggest that P2X7R plays a potentially pivotal role in a variety of physiological functions, including peripheral and central neuronal transmission, smooth muscle contraction, and inflammation. Thus, P2X7R may be a potential target for drug development. Here, we used a FlexStation to examine the function of recombinant P2X7R stably expressed in human embryonic kidney 293 cells and to compare three high-throughput screening assays: a membrane potential assay, an ethidium bromide uptake assay, and a calcium influx assay. We found that all three assays were suitable for the analysis of P2X7R, but the calcium influx assay was the most robust and is the best choice as a first high-throughput screening assay when embarking on a P2X7R drug discovery project.

KeywordsP2X7R high-throughput screening FlexStation calcium influx assay membrane potential assay ethidium bromide EtBr uptake assay This article is published with open access at Springerlink.com

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Author: YaQin Jiang - Qi Yin - ShiYou Li

Source: https://link.springer.com/







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