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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

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Published on: September 13, 2013

Probing PAC1 receptor activation across species with an engineered sensor.

Reto B Cola¹, Salome N Niethammer², Preethi Rajamannar³

¹Institute of Pharmacology and Toxicology, University of Zürich, Zurich, Switzerland.

|August 15, 2024

Summary

Scientists developed PAClight1P78A, a new sensor for Class-B1 G-protein-coupled receptors (GPCRs). This tool enhances drug discovery and basic research by enabling easier investigation of these important drug targets in various models.

Keywords:

PAC1 receptor PACAP VIP adenylate cyclase-activating polypeptide biochemistry chemical biology genetically-encoded fluorescent sensors human mouse neuropeptides vasoactive intestinal peptide zebrafish

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Area of Science:

Biochemistry
Molecular Biology
Pharmacology

Background:

Class-B1 G-protein-coupled receptors (GPCRs) are crucial drug targets but challenging for high-throughput screening and animal studies.
Investigating GPCRs requires advanced tools for in vitro and in vivo applications.

Purpose of the Study:

To engineer a novel, genetically encoded sensor based on the human PAC1 receptor (hmPAC1R) for Class-B1 GPCRs.
To characterize the sensor's performance for in vitro and in vivo applications, aiding drug development and basic research.

Main Methods:

Engineered PAClight1P78A, a genetically encoded sensor derived from hmPAC1R.
Characterized sensor expression, brightness, and performance in transfected and stably expressing cells.
Demonstrated sensor utility in ex vivo and in vivo mouse models and in living zebrafish larvae.

Main Results:

PAClight1P78A exhibits a high dynamic range (1100%), excellent ligand selectivity, and rapid activation kinetics (1.15 s).
Robust sensor expression and fluorescence responses were observed in various animal models (mice and zebrafish).
The sensor proved effective for both in vitro and in vivo applications.

Conclusions:

PAClight1P78A is a versatile, high-performance sensor for Class-B1 GPCRs.
This novel tool facilitates research and drug development targeting GPCRs.
The sensor empowers a broad range of life science applications.