Impact of Dendrimer Terminal Group Chemistry on Blockage of the Anthrax Toxin Channel: A Single Molecule Study.

ABSTRACT: Nearly all the cationic molecules tested so far have been shown to reversibly block K⁺ current through the cation-selective PA63 channels of anthrax toxin in a wide nM-mM range of effective concentrations. A significant increase in channel-blocking activity of the cationic compounds was achieved when multiple copies of positively charged ligands were covalently linked to multivalent scaffolds, such as cyclodextrins and dendrimers. Even though multivalent binding can be strong when the individual bonds are relatively weak, for drug discovery purposes we often strive to design multivalent compounds with high individual functional group affinity toward the respective binding site on a multivalent target. Keeping this requirement in mind, here we perform a single-channel/single-molecule study

SUBMITTER: Yamini G 

PROVIDER: S-EPMC5127133 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature