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Page 1
Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease.
Toledo-Sherman LM, Prime ME, Mrzljak L, Beconi MG, Beresford A, Brookfield FA, Brown CJ, Cardaun I, Courtney SM, Dijkman U, Hamelin-Flegg E, Johnson PD, Kempf V, Lyons K, Matthews K, Mitchell WL, O'Connell C, Pena P, Powell K, Rassoulpour A, Reed L, Reindl W, Selvaratnam S, Friley WW, Weddell DA, Went NE, Wheelan P, Winkler C, Winkler D, Wityak J, Yarnold CJ, Yates D, Munoz-Sanjuan I, Dominguez C. Toledo-Sherman LM, et al. Among authors: winkler c, winkler d. J Med Chem. 2015 Feb 12;58(3):1159-83. doi: 10.1021/jm501350y. Epub 2015 Jan 23. J Med Chem. 2015. PMID: 25590515
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.
Prime ME, Andersen OA, Barker JJ, Brooks MA, Cheng RK, Toogood-Johnson I, Courtney SM, Brookfield FA, Yarnold CJ, Marston RW, Johnson PD, Johnsen SF, Palfrey JJ, Vaidya D, Erfan S, Ichihara O, Felicetti B, Palan S, Pedret-Dunn A, Schaertl S, Sternberger I, Ebneth A, Scheel A, Winkler D, Toledo-Sherman L, Beconi M, Macdonald D, Muñoz-Sanjuan I, Dominguez C, Wityak J. Prime ME, et al. Among authors: winkler d. J Med Chem. 2012 Feb 9;55(3):1021-46. doi: 10.1021/jm201310y. Epub 2012 Jan 27. J Med Chem. 2012. PMID: 22224594
The novel KMO inhibitor CHDI-340246 leads to a restoration of electrophysiological alterations in mouse models of Huntington's disease.
Beaumont V, Mrzljak L, Dijkman U, Freije R, Heins M, Rassoulpour A, Tombaugh G, Gelman S, Bradaia A, Steidl E, Gleyzes M, Heikkinen T, Lehtimäki K, Puoliväli J, Kontkanen O, Javier RM, Neagoe I, Deisemann H, Winkler D, Ebneth A, Khetarpal V, Toledo-Sherman L, Dominguez C, Park LC, Munoz-Sanjuan I. Beaumont V, et al. Among authors: winkler d. Exp Neurol. 2016 Aug;282:99-118. doi: 10.1016/j.expneurol.2016.05.005. Epub 2016 May 6. Exp Neurol. 2016. PMID: 27163548
Fragment-based identification of Hsp90 inhibitors.
Barker JJ, Barker O, Boggio R, Chauhan V, Cheng RK, Corden V, Courtney SM, Edwards N, Falque VM, Fusar F, Gardiner M, Hamelin EM, Hesterkamp T, Ichihara O, Jones RS, Mather O, Mercurio C, Minucci S, Montalbetti CA, Müller A, Patel D, Phillips BG, Varasi M, Whittaker M, Winkler D, Yarnold CJ. Barker JJ, et al. Among authors: winkler d. ChemMedChem. 2009 Jun;4(6):963-6. doi: 10.1002/cmdc.200900011. ChemMedChem. 2009. PMID: 19301319
Metabolism and pharmacokinetics of JM6 in mice: JM6 is not a prodrug for Ro-61-8048.
Beconi MG, Yates D, Lyons K, Matthews K, Clifton S, Mead T, Prime M, Winkler D, O'Connell C, Walter D, Toledo-Sherman L, Munoz-Sanjuan I, Dominguez C. Beconi MG, et al. Among authors: winkler d. Drug Metab Dispos. 2012 Dec;40(12):2297-306. doi: 10.1124/dmd.112.046532. Epub 2012 Aug 31. Drug Metab Dispos. 2012. PMID: 22942319
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z. Burch JD, et al. Among authors: winkler d. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870
Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism.
Marcotte D, Zeng W, Hus JC, McKenzie A, Hession C, Jin P, Bergeron C, Lugovskoy A, Enyedy I, Cuervo H, Wang D, Atmanene C, Roecklin D, Vecchi M, Vivat V, Kraemer J, Winkler D, Hong V, Chao J, Lukashev M, Silvian L. Marcotte D, et al. Among authors: winkler d. Bioorg Med Chem. 2013 Jul 15;21(14):4011-9. doi: 10.1016/j.bmc.2013.04.019. Epub 2013 Apr 19. Bioorg Med Chem. 2013. PMID: 23647822
Novel MK2 inhibitors by fragment screening.
Keminer O, Kraemer J, Kahmann J, Sternberger I, Scheich C, Jungmann J, Schaert S, Winkler D, Ichihara O, Whittaker M, Ullmann D, Hesterkamp T. Keminer O, et al. Among authors: winkler d. Comb Chem High Throughput Screen. 2009 Aug;12(7):697-703. doi: 10.2174/138620709788923700. Epub 2009 Aug 1. Comb Chem High Throughput Screen. 2009. PMID: 19531016
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