Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization

[Image: see text] We report herein the first systematic exploration of inhibitors of the mitotic kinase Nek2. Starting from HTS hit aminopyrazine 2, compounds with improved activity were identified using structure-based design. Our structural biology investigations reveal two notable observations. F...

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Huvudupphovsmän: Whelligan, Daniel K., Solanki, Savade, Taylor, Dawn, Thomson, Douglas W., Cheung, Kwai-Ming J., Boxall, Kathy, Mas-Droux, Corine, Barillari, Caterina, Burns, Samantha, Grummitt, Charles G., Collins, Ian, van Montfort, Rob L. M., Aherne, G. Wynne, Bayliss, Richard, Hoelder, Swen
Materialtyp: Artigo
Språk:Inglês
Publicerad: American Chemical Society 2010
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC2972649/
https://ncbi.nlm.nih.gov/pubmed/20936789
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm1008727
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