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Page 1
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. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870
Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).
Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MHA, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CAGN, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z. Trani G, et al. Among authors: brookfield fa. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5818-5823. doi: 10.1016/j.bmcl.2014.10.020. Epub 2014 Oct 12. Bioorg Med Chem Lett. 2014. PMID: 25455497
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: brookfield fa. J Med Chem. 2012 Feb 9;55(3):1021-46. doi: 10.1021/jm201310y. Epub 2012 Jan 27. J Med Chem. 2012. PMID: 22224594
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: brookfield fa. J Med Chem. 2015 Feb 12;58(3):1159-83. doi: 10.1021/jm501350y. Epub 2015 Jan 23. J Med Chem. 2015. PMID: 25590515
Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease.
Prime ME, Brookfield FA, Courtney SM, Gaines S, Marston RW, Ichihara O, Li M, Vaidya D, Williams H, Pedret-Dunn A, Reed L, Schaertl S, Toledo-Sherman L, Beconi M, Macdonald D, Muñoz-Sanjuan I, Dominguez C, Wityak J. Prime ME, et al. Among authors: brookfield fa. ACS Med Chem Lett. 2012 Aug 9;3(9):731-5. doi: 10.1021/ml3001352. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900540 Free PMC article.
Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Armer RE, Ashton MR, Boyd EA, Brennan CJ, Brookfield FA, Gazi L, Gyles SL, Hay PA, Hunter MG, Middlemiss D, Whittaker M, Xue L, Pettipher R. Armer RE, et al. Among authors: brookfield fa. J Med Chem. 2005 Oct 6;48(20):6174-7. doi: 10.1021/jm050519b. J Med Chem. 2005. PMID: 16190744
SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.
Wityak J, Prime ME, Brookfield FA, Courtney SM, Erfan S, Johnsen S, Johnson PD, Li M, Marston RW, Reed L, Vaidya D, Schaertl S, Pedret-Dunn A, Beconi M, Macdonald D, Muñoz-Sanjuan I, Dominguez C. Wityak J, et al. Among authors: brookfield fa. ACS Med Chem Lett. 2012 Oct 4;3(12):1024-8. doi: 10.1021/ml300241m. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900424 Free PMC article.
Exploiting differences in caspase-2 and -3 S₂ subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors.
Maillard MC, Brookfield FA, Courtney SM, Eustache FM, Gemkow MJ, Handel RK, Johnson LC, Johnson PD, Kerry MA, Krieger F, Meniconi M, Muñoz-Sanjuán I, Palfrey JJ, Park H, Schaertl S, Taylor MG, Weddell D, Dominguez C. Maillard MC, et al. Among authors: brookfield fa. Bioorg Med Chem. 2011 Oct 1;19(19):5833-51. doi: 10.1016/j.bmc.2011.08.020. Epub 2011 Aug 16. Bioorg Med Chem. 2011. PMID: 21903398
14 results