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Updated: Jul 28, 2026
Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
Acid-Resistant BODIPY Amino Acids for Peptide-Based Fluorescence Imaging of GPR54 Receptors in Pancreatic Islets
Lorena Mendive-Tapia1, Laia Miret-Casals2, Nicole D Barth1
1Centre for Inflammation Research The University of Edinburgh EH16 4TJ Edinburgh UK.
Abstract:
The G protein-coupled kisspeptin receptor (GPR54 or KISS1R) is an important mediator in reproduction, metabolism and cancer biology; however, there are limited fluorescent probes or antibodies for direct imaging of these receptors in cells and intact tissues, which can help to interrogate their multiple biological roles. Herein, we describe the rational design and characterization of a new acid-resistant BODIPY-based amino acid (Trp-BODIPY PLUS), and its implementation for solid-phase synthesis of fluorescent bioactive peptides. Trp-BODIPY PLUS retains the binding capabilities of both short linear and cyclic peptides and displays notable turn-on fluorescence emission upon target binding for wash-free imaging. Finally, we employed Trp-BODIPY PLUS to prepare some of the first fluorogenic kisspeptin-based probes and visualized the expression and localization of GPR54 receptors in human cells and in whole mouse pancreatic islets by fluorescence imaging.
Insights
Researchers developed a new fluorescent probe for imaging the kisspeptin receptor (GPR54). This tool enables visualization of GPR54 in cells and tissues, aiding research in reproduction, metabolism, and cancer.
Area of Science:
- Biochemistry and Molecular Biology
- Chemical Biology
- Cell Biology
Background:
- The G protein-coupled kisspeptin receptor (GPR54/KISS1R) is crucial for reproduction, metabolism, and cancer.
- Limited availability of fluorescent probes and antibodies hinders direct imaging of GPR54 in biological systems.
- Understanding GPR54's roles requires advanced imaging tools for cellular and tissue-level analysis.
Purpose of the Study:
- To design and characterize a novel acid-resistant fluorescent amino acid probe.
- To synthesize fluorogenic bioactive peptides using the new probe for GPR54 imaging.
- To visualize GPR54 receptor expression and localization in human cells and mouse pancreatic islets.
Main Methods:
- Rational design and synthesis of an acid-resistant BODIPY-based amino acid (Trp-BODIPY PLUS).
- Solid-phase synthesis of fluorescent bioactive peptides incorporating Trp-BODIPY PLUS.
- Fluorescence imaging of GPR54 receptors in human cells and mouse pancreatic islets using novel kisspeptin-based probes.
Main Results:
- Trp-BODIPY PLUS retains peptide binding capabilities and exhibits turn-on fluorescence upon target binding.
- Wash-free imaging of target receptors is achievable with the developed fluorescent probes.
- The first fluorogenic kisspeptin-based probes were successfully prepared and used for GPR54 visualization.
Conclusions:
- A novel Trp-BODIPY PLUS probe enables the creation of effective fluorescent bioactive peptides.
- This technology provides a valuable tool for wash-free, high-sensitivity imaging of GPR54.
- The developed probes facilitate direct visualization of GPR54 in cellular and tissue contexts, advancing reproductive and metabolic research.
