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Structure based design of a Grp94-selective inhibitor: Exploiting a key residue in Grp94 to optimize paralog-selective binding

Grp94 and Hsp90, the ER and cytoplasmic hsp90 paralogs, share a conserved ATP-binding pocket that has been targeted for therapeutics. Paralog-selective inhibitors may lead to drugs with fewer side effects. Here, we analyzed 1 (BnIm), a benzyl imidazole resorcinylic inhibitor, for its mode of binding...

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Pubblicato in:J Med Chem
Autori principali: Que, Nanette L. S., Crowley, Vincent M., Duerfeldt, Adam S., Zhao, Jinbo, Kent, Caitlin N., Blagg, Brian S. J., Gewirth, Daniel T.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5897183/
https://ncbi.nlm.nih.gov/pubmed/29528635
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b01608
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