4YZ9

Crystal Structure of human phosphorylated IRE1alpha in complex with a type III kinase inhibitor (GSK2850163A)

Summary for 4YZ9

Entry DOI	10.2210/pdb4yz9/pdb
Related	4YZC 4YZD
Descriptor	Serine/threonine-protein kinase/endoribonuclease IRE1, (5R)-2-(3,4-dichlorobenzyl)-N-(4-methylbenzyl)-2,7-diazaspiro[4.5]decane-7-carboxamide (3 entities in total)
Functional Keywords	active, inhibitor, complex, ire1, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (Human)
Cellular location	Endoplasmic reticulum membrane ; Single-pass type I membrane protein : O75460
Total number of polymer chains	3
Total formula weight	141170.95
Authors	Concha, N.O. (deposition date: 2015-03-24, release date: 2015-11-11, Last modification date: 2023-09-27)
Primary citation	Concha, N.O.,Smallwood, A.,Bonnette, W.,Totoritis, R.,Zhang, G.,Federowicz, K.,Yang, J.,Qi, H.,Chen, S.,Campobasso, N.,Choudhry, A.E.,Shuster, L.E.,Evans, K.A.,Ralph, J.,Sweitzer, S.,Heerding, D.A.,Buser, C.A.,Su, D.S.,DeYoung, M.P. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1 alpha Endoribonuclease Activity. Mol.Pharmacol., 88:1011-1023, 2015 Cited by PubMed: 26438213 DOI: 10.1124/mol.115.100917 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.463 Å)

Structure validation