Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides

Methyl groups can have profound effects in drug discovery but the underlying mechanisms are diverse and incompletely understood. Here we report the stereospecific effect of a single, solvent-exposed methyl group in bicyclic [4.3.1] aza-amides, robustly leading to a 2 to 10-fold increase in binding a...

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Detalles Bibliográficos
Autores principales: Kolos, Jürgen M., Pomplun, Sebastian, Jung, Sascha, Rieß, Benedikt, Purder, Patrick L., Voll, Andreas M., Merz, Stephanie, Gnatzy, Monika, Geiger, Thomas M., Quist-Løkken, Ingrid, Jatzlau, Jerome, Knaus, Petra, Holien, Toril, Bracher, Andreas, Meyners, Christian, Czodrowski, Paul, Krewald, Vera, Hausch, Felix
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8597852/
https://www.ncbi.nlm.nih.gov/pubmed/34820091
http://dx.doi.org/10.1039/d1sc04638a

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