Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease

[Image: see text] A series of imidazo[1,2-b]pyridazin-8-amine kinase inhibitors were discovered to allosterically inhibit the endoribonuclease function of the dual kinase-endoribonuclease inositol-requiring enzyme 1α (IRE1α), a key component of the unfolded protein response in mammalian cells and a...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Colombano, Giampiero, Caldwell, John J., Matthews, Thomas P., Bhatia, Chitra, Joshi, Amar, McHardy, Tatiana, Mok, Ngai Yi, Newbatt, Yvette, Pickard, Lisa, Strover, Jade, Hedayat, Somaieh, Walton, Michael I., Myers, Stephanie M., Jones, Alan M., Saville, Harry, McAndrew, Craig, Burke, Rosemary, Eccles, Suzanne A., Davies, Faith E., Bayliss, Richard, Collins, Ian
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6437697/
https://ncbi.nlm.nih.gov/pubmed/30779566
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01721
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