Official websites use. Share sensitive information only on official, secure websites. Michael acceptors MACs were considered as possible CAXs because their irreversible bioconjugation to thiols is well known from covalent drugs. Uptake inhibition is reported as decreasing cellular fluorescence with increasing concentration of, e. The finestructure visible within the cytosol was characteristic of the endoplasmic reticulum ER. Delivery to ER and nucleus but neither plasma membrane nor endolysosomes supported that MACs enter the cytosol by direct penetration and not by endocytosis.
These trends should, however, not be overinterpreted because signal intensity within cells depends strongly on CAXs quenching , concentration, incubation time, cell culture, pH, and so on. This was particularly remarkable for ETP 31 because this is otherwise an excellent inhibitor.
The distinct pattern generated by inhibitors was important, first of all, to support that MAC 16 indeed enters cells by TMU and not by passive diffusion. It thus strengthened the emerging view of TMU as a dynamic covalent network with diverse exchange partners and pathways to enter into cells. Dimer 33 was an outstanding inhibitor. As a service to our authors and readers, this journal provides supporting information supplied by the authors.
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Shybeka, J. Maynard, S. Saidjalolov, D. Moreau, N. Sakai, S. Matile, Angew. This section collects any data citations, data availability statements, or supplementary materials included in this article. As a library, NLM provides access to scientific literature. Angew Chem Int Ed Engl. Find articles by Inga Shybeka. Find articles by John R J Maynard. Find articles by Saidbakhrom Saidjalolov. Find articles by Dimitri Moreau.
