Detection of human GPCR activity in drosophila S2 cells using the Tango system

Salim, Emil and Hori, Aki and Matsubara, Kohei and Takano-Shimizu, Toshiyuki and Pratomo, Andre Rizky and Marianne, Marianne and Syahputra, Armia and Husori, Dadang Irfan and Inoue, Asuka and Abdullah, Maryam Aisyah and Shamsudin, Nur Farisya and Rullah, Kamal and Kuraishi, Takayuki (2025) Detection of human GPCR activity in drosophila S2 cells using the Tango system. International Journal of Molecular Sciences, 26 (1). ISSN 1661-6596 E-ISSN 1422-0067

Preview	PDF - Published Version Available under License Creative Commons Attribution. Download (2MB) | Preview
	PDF (SCOPUS) - Supplemental Material Restricted to Registered users only Download (113kB) | Request a copy
Preview	PDF (WOS) - Supplemental Material Download (661kB) | Preview

Abstract

G protein-coupled receptors (GPCRs) are essential cell surface proteins involved in transducing extracellular signals into intracellular responses, regulating various physiological processes. This study validated the use of the Tango assay, a sensitive method for detecting GPCR activation, in Drosophila Schneider 2 (S2) cells, focusing on the human Dopamine Receptor D4 (DRD4). Plasmids encoding the LexA-tagged human DRD4 receptor and a luciferase reporter were co-transfected into Drosophila S2 cells and stimulated with dopamine. Receptor activation was measured by quantifying the luciferase activity. The system showed high specificity for dopamine, with no activation in response to octopamine, a non-ligand for DRD4. Furthermore, the system effectively detects activation by a novel compound. These results demonstrate that Drosophila S2 cells, coupled with the Tango assay, provide a viable model for studying human GPCR function and ligand specificity. This system enables the rapid screening of potential GPCR ligands in a cost-effective cellular model.

Item Type:	Article (Journal)
Uncontrolled Keywords:	human GPCRs; Drosophila S2 cells; Tango system; human DRD4; dopamine
Subjects:	R Medicine > RS Pharmacy and materia medica > RS403 Materia Medica-Pharmaceutical Chemistry
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Pharmacy Kulliyyah of Pharmacy > Department of Pharmaceutical Chemistry
Depositing User:	Dr Kamal Rullah
Date Deposited:	04 Feb 2025 12:10
Last Modified:	04 Feb 2025 12:10
URI:	http://irep.iium.edu.my/id/eprint/119122

Actions (login required)

View Item