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...

Disgrifiad llawn

Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:ACS Med Chem Lett
Prif Awduron: 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.
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: American Chemical Society 2015
Mynediad Ar-lein: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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