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Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay.
J Biomol Screen. 2013 Mar;18(3):298-308. doi: 10.1177/1087057112465647. Epub 2012 Nov 8.
J Biomol Screen. 2013.
PMID: 23139381
Multiple autophosphorylations significantly enhance the endoribonuclease activity of human inositol requiring enzyme 1α.
Itzhak D, Bright M, McAndrew P, Mirza A, Newbatt Y, Strover J, Widya M, Thompson A, Morgan G, Collins I, Davies F.
Itzhak D, et al.
BMC Biochem. 2014 Feb 13;15:3. doi: 10.1186/1471-2091-15-3.
BMC Biochem. 2014.
PMID: 24524643
Free PMC article.
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Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease.
Colombano G, Caldwell JJ, Matthews TP, Bhatia C, Joshi A, McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R, Collins I.
Colombano G, et al.
J Med Chem. 2019 Mar 14;62(5):2447-2465. doi: 10.1021/acs.jmedchem.8b01721. Epub 2019 Mar 5.
J Med Chem. 2019.
PMID: 30779566
Free PMC article.
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Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel.
Ryckmans T, Aubdool AA, Bodkin JV, Cox P, Brain SD, Dupont T, Fairman E, Hashizume Y, Ishii N, Kato T, Kitching L, Newman J, Omoto K, Rawson D, Strover J.
Ryckmans T, et al.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4857-9. doi: 10.1016/j.bmcl.2011.06.035. Epub 2011 Jun 21.
Bioorg Med Chem Lett. 2011.
PMID: 21741838
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