Upregulation of L-type calcium channels (LTCCs) is implicated in a range of cardiovascular and neurological disorders. Therefore, the development of toolboxes that unlock fast imaging protocols in live cells is coveted. Herein, we report a library of first-in-class far-red small-molecule-based fluorescent ligands (FluoDiPines), able to target LTCCs. All fluorescent ligands were evaluated in whole-cell patch-clamp and live-cell Ca2+ imaging whereby FluoDiPine 6 was found to be the best candidate for live-cell fluorescence imaging. Low concentration of FluoDiPine 6 (50 nM) and a quick labeling protocol (5 min) are successfully applied to fixed and live cells to image LTCCs with good specificity.
Novel Far-Red Fluorescent 1,4-Dihydropyridines for L-Type Calcium Channel Imaging / Borgarelli, Carlotta; Klingl, Yvonne E; Escamilla-Ayala, Abril; Scarponi, Carlotta; La Rovere, Rita M L; Stoklund Dittlau, Katarina; Bultynck, Geert; Sampaolesi, Maurilio; Schoenberger, Matthias; Munck, Sebastian; Van Den Bosch, Ludo; De Borggraeve, Wim M; Ismalaj, Ermal. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 1520-4804. - 67:20(2024), pp. 18038-18052. [10.1021/acs.jmedchem.4c00565]
Novel Far-Red Fluorescent 1,4-Dihydropyridines for L-Type Calcium Channel Imaging
Sampaolesi, Maurilio;
2024
Abstract
Upregulation of L-type calcium channels (LTCCs) is implicated in a range of cardiovascular and neurological disorders. Therefore, the development of toolboxes that unlock fast imaging protocols in live cells is coveted. Herein, we report a library of first-in-class far-red small-molecule-based fluorescent ligands (FluoDiPines), able to target LTCCs. All fluorescent ligands were evaluated in whole-cell patch-clamp and live-cell Ca2+ imaging whereby FluoDiPine 6 was found to be the best candidate for live-cell fluorescence imaging. Low concentration of FluoDiPine 6 (50 nM) and a quick labeling protocol (5 min) are successfully applied to fixed and live cells to image LTCCs with good specificity.| File | Dimensione | Formato | |
|---|---|---|---|
|
Borgarelli_Novel-Far-Red_2024.pdf
solo gestori archivio
Tipologia:
Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza:
Tutti i diritti riservati (All rights reserved)
Dimensione
4.76 MB
Formato
Adobe PDF
|
4.76 MB | Adobe PDF | Contatta l'autore |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
