Acid-Resistant BODIPY Amino Acids for Peptide-Based Fluorescence Imaging of GPR54 Receptors in Pancreatic Islets.
Acid-Resistant BODIPY Amino Acids for Peptide-Based Fluorescence Imaging of GPR54 Receptors in Pancreatic Islets.
复制标题
用于胰岛 GPR54 受体肽基荧光成像的耐酸 BODIPY 氨基酸。
DOI：
10.1002/anie.202302688
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发表时间：
2023
期刊：
影响因子：
--
通讯作者：
Mendive-Tapia L
中科院分区：
文献类型：
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作者：
Mendive-Tapia L
G蛋白偶联kisspeptin受体（GPR 54或KISS 1 R）是生殖、代谢和癌症生物学中的重要介质;然而，用于直接成像细胞和完整组织中这些受体的荧光探针或抗体有限，这有助于询问它们的多种生物学作用。在本文中，我们描述了一种新的耐酸BODIPY基氨基酸（Trp‐BODIPY PLUS）的合理设计和表征，以及其用于荧光生物活性肽的固相合成的实施。Trp‐BODIPY PLUS保留了短直链和环状肽的结合能力，并在靶点结合时显示出显著的开启荧光发射，用于免清洗成像。最后，我们使用Trp‐BODIPY PLUS制备了一些第一批基于kisspeptin的荧光探针，并通过荧光成像观察了GPR 54受体在人细胞和整个小鼠胰岛中的表达和定位。
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.