Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity

[Image: see text] Amino-quinazoline BRaf kinase inhibitor 2 was identified from a library screen as a modest inhibitor of the unfolded protein response (UPR) regulating potential anticancer target IRE1α. A combination of crystallographic and conformational considerations were used to guide structure...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: Beveridge, Ramsay E., Wallweber, Heidi Ackerly, Ashkenazi, Avi, Beresini, Maureen, Clark, Kevin R., Gibbons, Paul, Ghiro, Elise, Kaufman, Susan, Larivée, Alexandre, Leblanc, Melissa, Leclerc, Jean-Philippe, Lemire, Alexandre, Ly, Cuong, Rudolph, Joachim, Schwarz, Jacob B., Srivastava, Sanjay, Wang, Weiru, Zhao, Liang, Braun, Marie-Gabrielle
Format: Artigo
Language:Inglês
Published: American Chemical Society 2020
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC7734639/
https://ncbi.nlm.nih.gov/pubmed/33335661
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00344
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