Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

[Image: see text] Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated...

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Publicado no:ACS Med Chem Lett
Main Authors: Evans, Catherine A., Liu, Tao, Lescarbeau, André, Nair, Somarajan J., Grenier, Louis, Pradeilles, Johan A., Glenadel, Quentin, Tibbitts, Thomas, Rowley, Ann M., DiNitto, Jonathan P., Brophy, Erin E., O’Hearn, Erin L., Ali, Janid A., Winkler, David G., Goldstein, Stanley I., O’Hearn, Patrick, Martin, Christian M., Hoyt, Jennifer G., Soglia, John R., Cheung, Culver, Pink, Melissa M., Proctor, Jennifer L., Palombella, Vito J., Tremblay, Martin R., Castro, Alfredo C.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5018865/
https://ncbi.nlm.nih.gov/pubmed/27660692
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00238
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