Illuminating the Path to Enhanced Bioimaging by Phosphole-based Fluorophores

Mareike Schenk, Nils Koenig, Evamarie Hey-Hawkins,Annette G. Beck-Sickinger

CHEMBIOCHEM(2024)

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摘要
As the research of biological systems becomes increasingly complex, there is a growing demand for fluorophores with a diverse range of wavelengths. In this study, we introduce phosphole-based fluorophores that surpass existing options like dansyl chloride. The reactive S-Cl bond in chlorosulfonylimino-5-phenylphosphole derivatives allows rapid and direct coupling to peptides making the fluorophores easily introducible to peptides. This coupling process occurs under mild conditions, demonstrated for [F7,P34]-NPY and its shorter analogues. Peptides linked with our fluorophores exhibit similar receptor activation to the control peptide, while maintaining high stability and low toxicity, making them ideal biolabeling reagents. In fluorescence microscopy experiments, they can be easily visualized even at low concentrations, without suffering from the typical issue of bleaching. These phosphole-based fluorophores represent a significant leap forward in the field. Their versatility, ease of modification, superior performance, and applicability in biological labeling make them a promising choice for researchers seeking advanced tools to unravel the details of complex biological systems. This study introduces a new class of phosphole-based fluorophores for advanced biological research. These fluorophores outperform existing options, are easily synthesized, and can be coupled to peptides with high selectivity. Labeled peptides maintain stability and low toxicity while exhibiting receptor activation, making them ideal for biolabeling. In fluorescence microscopy, these fluorophores remain visible at low concentrations without bleaching. image
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关键词
Biolabeling,Fluorescence,Peptides,Phospholes
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