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- W3104991008 abstract "Ellman's reagent has caused substantial confusion and concern as a probe for thiol-mediated uptake because it is the only established inhibitor available but works neither efficiently nor reliably. Here we use fluorescent cyclic oligochalcogenides that enter cells by thiol-mediated uptake to systematically screen for more potent inhibitors, including epidithiodiketopiperazines, benzopolysulfanes, disulfide-bridged γ-turned peptides, heteroaromatic sulfones and cyclic thiosulfonates, thiosulfinates and disulfides. With nanomolar activity, the best inhibitors identified are more than 5000 times better than Ellman's reagent. Different activities found with different reporters reveal thiol-mediated uptake as a complex multitarget process. Preliminary results on the inhibition of the cellular uptake of pseudo-lentivectors expressing SARS-CoV-2 spike protein do not exclude potential of efficient inhibitors of thiol-mediated uptake for the development of new antivirals." @default.
- W3104991008 created "2020-11-23" @default.
- W3104991008 creator A5021760829 @default.
- W3104991008 creator A5021801739 @default.
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- W3104991008 creator A5081942045 @default.
- W3104991008 date "2021-01-01" @default.
- W3104991008 modified "2023-10-17" @default.
- W3104991008 title "Inhibitors of thiol-mediated uptake" @default.
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- W3104991008 doi "https://doi.org/10.1039/d0sc05447j" @default.