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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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Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:J Med Chem
Prif Awduron: 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
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: American Chemical Society 2019
Mynediad Ar-lein: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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