A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP

Abstract Extensive functional studies of the exchange protein directly activated by cAMP (EPAC) family of signaling molecules have demonstrated that EPAC proteins play a fundamental role in several physiological and pathophysiological responses, therefore are attractive drug targets. In this report,...

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Autores principales:	Yingmin Zhu, Fang Mei, Pei Luo, Xiaodong Cheng
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/8e4267e28d4147aeaf640b336e562918
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spelling	oai:doaj.org-article:8e4267e28d4147aeaf640b336e5629182021-12-02T16:08:00ZA cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP10.1038/s41598-017-06432-42045-2322https://doaj.org/article/8e4267e28d4147aeaf640b336e5629182017-07-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-06432-4https://doaj.org/toc/2045-2322Abstract Extensive functional studies of the exchange protein directly activated by cAMP (EPAC) family of signaling molecules have demonstrated that EPAC proteins play a fundamental role in several physiological and pathophysiological responses, therefore are attractive drug targets. In this report, the development of a cell-based, medium to high throughput screening assay that is capable of monitoring EPAC-mediated activation of cellular Rap1 in an isoform-specific manner is described. This assay adapts a conventional ELISA format with immobilized RalGDS-RBD as a bait to selectively capture GTP-bound active Rap1. As a result, it fills an urgent need for a cell-based EPAC assay that can be conveniently performed using microtiter plates for the discovery and/or validation of isoform-specific EPAC agonists and antagonists.Yingmin ZhuFang MeiPei LuoXiaodong ChengNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-9 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Yingmin Zhu Fang Mei Pei Luo Xiaodong Cheng A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
description	Abstract Extensive functional studies of the exchange protein directly activated by cAMP (EPAC) family of signaling molecules have demonstrated that EPAC proteins play a fundamental role in several physiological and pathophysiological responses, therefore are attractive drug targets. In this report, the development of a cell-based, medium to high throughput screening assay that is capable of monitoring EPAC-mediated activation of cellular Rap1 in an isoform-specific manner is described. This assay adapts a conventional ELISA format with immobilized RalGDS-RBD as a bait to selectively capture GTP-bound active Rap1. As a result, it fills an urgent need for a cell-based EPAC assay that can be conveniently performed using microtiter plates for the discovery and/or validation of isoform-specific EPAC agonists and antagonists.
format	article
author	Yingmin Zhu Fang Mei Pei Luo Xiaodong Cheng
author_facet	Yingmin Zhu Fang Mei Pei Luo Xiaodong Cheng
author_sort	Yingmin Zhu
title	A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
title_short	A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
title_full	A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
title_fullStr	A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
title_full_unstemmed	A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP
title_sort	cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by camp
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/8e4267e28d4147aeaf640b336e562918
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_version_	1718384670876368896

A cell-based, quantitative and isoform-specific assay for exchange proteins directly activated by cAMP

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