Specific pharmacological and Gi/o protein responses of some native GPCRs in neurons

Chanjuan Xu, Yiwei Zhou, Yuxuan Liu, Li Lin, Peng Liu, Xiaomei Wang, Zhengyuan Xu, Jean-Philippe Pin (), Philippe Rondard () and Jianfeng Liu ()
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Chanjuan Xu: Huazhong University of Science and Technology
Yiwei Zhou: Huazhong University of Science and Technology
Yuxuan Liu: Huazhong University of Science and Technology
Li Lin: Huazhong University of Science and Technology
Peng Liu: Huazhong University of Science and Technology
Xiaomei Wang: Huazhong University of Science and Technology
Zhengyuan Xu: Huazhong University of Science and Technology
Jean-Philippe Pin: Université de Montpellier, CNRS, INSERM
Philippe Rondard: Université de Montpellier, CNRS, INSERM
Jianfeng Liu: Huazhong University of Science and Technology

Nature Communications, 2024, vol. 15, issue 1, 1-14

Abstract: Abstract G protein-coupled receptors (GPCRs) constitute the largest family of membrane proteins and are important drug targets. The discovery of drugs targeting these receptors and their G protein signaling properties are based on assays mainly performed with modified receptors expressed in heterologous cells. However, GPCR responses may differ in their native environment. Here, by using highly sensitive Gi/o sensors, we reveal specific properties of Gi/o protein-mediated responses triggered by GABAB, α2 adrenergic and cannabinoid CB1 receptors in primary neurons, different from those in heterologous cells. These include different profiles in the Gi/o protein subtypes-mediated responses, and differences in the potencies of some ligands even at similar receptor expression levels. Altogether, our results show the importance of using biosensors compatible with primary cells for evaluating the activities of endogenous GPCRs in their native environment.

Date: 2024
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DOI: 10.1038/s41467-024-46177-z

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