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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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Τόπος έκδοσης:ACS Med Chem Lett
Κύριοι συγγραφείς: 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.
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: American Chemical Society 2015
Διαθέσιμο Online: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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