X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein

Squaramides constitute a novel class of RNA polymerase inhibitors of which genetic evidence and computational modeling previously have suggested an inhibitory mechanism mediated by binding to the RNA polymerase switch region. An iterative chemistry program increased the fraction unbound to human pla...

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Vydáno v:J Med Chem
Hlavní autoři: Molodtsov, Vadim, Fleming, Paul R., Eyermann, Charles J., Ferguson, Andrew D., Foulk, Melinda A., McKinney, David C., Masse, Craig E., Buurman, Ed T., Murakami, Katsuhiko S.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2015
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4658208/
https://ncbi.nlm.nih.gov/pubmed/25798859
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.5b00050
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