Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

[Image: see text] We recently reported the discovery of GSK2606414 (1), a selective first in class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which inhibited PERK activation in cells and demonstrated tumor growth inhibition in a human tumor xenograft in mice. In co...

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Main Authors: Axten, Jeffrey M., Romeril, Stuart P., Shu, Arthur, Ralph, Jeffrey, Medina, Jesús R., Feng, Yanhong, Li, William Hoi Hong, Grant, Seth W., Heerding, Dirk A., Minthorn, Elisabeth, Mencken, Thomas, Gaul, Nathan, Goetz, Aaron, Stanley, Thomas, Hassell, Annie M., Gampe, Robert T., Atkins, Charity, Kumar, Rakesh
格式: Artigo
語言:Inglês
出版: American Chemical Society 2013
在線閱讀:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027568/
https://ncbi.nlm.nih.gov/pubmed/24900593
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml400228e
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