Inhibition of Thiol?Mediated Uptake with Irreversible Covalent Inhibitors

Thiol-mediated uptake is emerging as method of choice to penetrate cells. This study focuses on irreversible covalent inhibitors thiol-mediated uptake. High-content high-throughput screening the so far largest collection hypervalent iodine reagents affords that are more than 250 times active Ellman’s reagent and rival best dynamic inhibitors. Comparison with other reveals inhibition within one series follows reactivity, whereas across deviates from reactivity. These trends support molecular recognition, besides exchange, contributes significantly The most powerful were Fukuyama’s nosyl protecting group super-cinnamaldehydes have been introduced activators pain receptor TRPA1. Considering several viruses use different forms enter cells, identification new general interest for discovery antivirals.