期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 62, 期 20, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202302688
关键词
Diabetes; Fluorescence; GPCRs; Probes; Solid-Phase Peptide Synthesis
This study describes the rational design and characterization of a new acid-resistant BODIPY-based amino acid (Trp-BODIPY PLUS) and its application in solid-phase synthesis of fluorescent bioactive peptides. The amino acid retains the binding capabilities of both short linear and cyclic peptides and shows notable turn-on fluorescence emission upon target binding for wash-free imaging. Trp-BODIPY PLUS was used to prepare fluorogenic kisspeptin-based probes and visualize the expression and localization of GPR54 receptors in human cells and whole mouse pancreatic islets by fluorescence imaging.
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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据