Synthesis of Small-Molecule Fluorescent Probes for the In Vitro Imaging of Calcium-Activated Potassium Channel K_Ca 3.1.

ABSTRACT: Small-molecule probes for the in vitro imaging of K_Ca 3.1 channel-expressing cells were developed. Senicapoc, showing high affinity and selectivity for the K_Ca 3.1 channels, was chosen as the targeting component. BODIPY dyes 15-20 were synthesized and connected by a Cu^I -catalyzed azide-alkyne [3+2]cycloaddition with propargyl ether senicapoc derivative 8, yielding fluorescently labeled ligands 21-26. The dimethylpyrrole-based imaging probes 25 and 26 allow staining of K_Ca 3.1 channels in NSCLC cells. The specificity was shown by removing the punctate staining pattern by pre-incubation with senicapoc. The density of K_Ca 3.1 channels detected with 25 and by immunostaining was identical. The punctate structure of the labeled channels cou

SUBMITTER: Brommel K 

PROVIDER: S-EPMC7318252 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature