Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase Cθ (PKCθ) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis

[Image: see text] PKCθ plays an important role in T cell biology and is a validated target for a number of disease states. A series of potent and selective PKCθ inhibitors were designed and synthesized starting from a HTS hit compound. Cell activity, while initially a challenge to achieve, was built...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Collier, Philip N., Twin, Heather C., Knegtel, Ronald M. A., Boyall, Dean, Brenchley, Guy, Davis, Christopher J., Keily, Shazia, Mak, Chau, Miller, Andrew, Pierard, Françoise, Settimo, Luca, Bolton, Clare M., Chiu, Peter, Curnock, Adam, Doyle, Elisabeth, Tanner, Adam J., Jimenez, Juan-Miguel
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6693473/
https://ncbi.nlm.nih.gov/pubmed/31417666
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00134
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