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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6437697/
https://www.ncbi.nlm.nih.gov/pubmed/30779566
http://dx.doi.org/10.1021/acs.jmedchem.8b01721

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