AI Article Synopsis
- The kisspeptin receptor (GPR54 or KISS1R) plays a crucial role in reproduction, metabolism, and cancer, but there are few tools available to visualize it directly in cells and tissues.
- Researchers have developed a new acid-resistant fluorescent probe called Trp-BODIPY PLUS, which allows for the synthesis of fluorescent bioactive peptides that can easily bind to target receptors.
- Using Trp-BODIPY PLUS, scientists created innovative kisspeptin-based probes that enabled them to successfully image and track GPR54 receptor activity in human cells and mouse pancreatic islets.
Article 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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10952496 | PMC |
| http://dx.doi.org/10.1002/ange.202302688 | DOI Listing |
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