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/ange.202302688
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发表时间：
2023
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蛋白偶联的Kisspeptin受体(GPR54或KISS1R)是生殖、代谢和癌症生物学中的重要介体，然而，目前在细胞和完整组织中直接成像这些受体的荧光探针或抗体有限，这有助于了解它们的多重生物学作用。在这里，我们描述了一种新的耐酸BODIPY氨基酸(Trp-BODIPY plus)的合理设计和表征，以及它在固相合成荧光生物活性多肽中的实现。Trp-BODIPY plus保留了短线状肽和环状肽的结合能力，并在目标结合时显示出显着的开启荧光发射，用于免洗成像。最后，我们利用Trp-BODIPY plus制备了第一批基于Kispeptin的荧光探针，并通过荧光成像技术可视化了Gpr54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.