Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway

[Image: see text] A high-throughput screen to discover inhibitors of p97 ATPase activity identified an indole amide that bound to an allosteric site of the protein. Medicinal chemistry optimization led to improvements in potency and solubility. Indole amide 3 represents a novel uncompetitive inhibit...

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Publicado no:ACS Med Chem Lett
Main Authors: Alverez, Celeste, Bulfer, Stacie L., Chakrasali, Ramappa, Chimenti, Michael. S., Deshaies, Raymond J., Green, Neal, Kelly, Mark, LaPorte, Matthew G., Lewis, Taber S., Liang, Mary, Moore, William J., Neitz, R. Jeffrey, Peshkov, Vsevolod A., Walters, Michael A., Zhang, Feng, Arkin, Michelle R., Wipf, Peter, Huryn, Donna M.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4753542/
https://ncbi.nlm.nih.gov/pubmed/26985295
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00396
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