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The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery.
Bradley AR, Echalier A, Fairhead M, Strain-Damerell C, Brennan P, Bullock AN, Burgess-Brown NA, Carpenter EP, Gileadi O, Marsden BD, Lee WH, Yue W, Bountra C, von Delft F. Bradley AR, et al. Among authors: echalier a. Essays Biochem. 2017 Nov 8;61(5):495-503. doi: 10.1042/EBC20170051. Print 2017 Nov 8. Essays Biochem. 2017. PMID: 29118096 Free PMC article. Review.
8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.
Carbain B, Paterson DJ, Anscombe E, Campbell AJ, Cano C, Echalier A, Endicott JA, Golding BT, Haggerty K, Hardcastle IR, Jewsbury PJ, Newell DR, Noble ME, Roche C, Wang LZ, Griffin RJ. Carbain B, et al. Among authors: echalier a. J Med Chem. 2014 Jan 9;57(1):56-70. doi: 10.1021/jm401555v. Epub 2013 Dec 23. J Med Chem. 2014. PMID: 24304238
Meriolins (3-(pyrimidin-4-yl)-7-azaindoles): synthesis, kinase inhibitory activity, cellular effects, and structure of a CDK2/cyclin A/meriolin complex.
Echalier A, Bettayeb K, Ferandin Y, Lozach O, Clément M, Valette A, Liger F, Marquet B, Morris JC, Endicott JA, Joseph B, Meijer L. Echalier A, et al. J Med Chem. 2008 Feb 28;51(4):737-51. doi: 10.1021/jm700940h. Epub 2008 Jan 31. J Med Chem. 2008. PMID: 18232649
M.; Marionneau-Lambert, S.; Ferandin, Y.; Lozach, O.; Morris, J.; Mateo-Lozano, S.; Druckes, P.; Schachtele, C.; Kubbutat, M.; Liger, F.; Marquet, B.; Joseph, B.; Echalier, A.; Endicott, J.; Notario, V.; Meijer, L. Cancer Res. 2007, 67, 8325-8334) in complex with CD …
M.; Marionneau-Lambert, S.; Ferandin, Y.; Lozach, O.; Morris, J.; Mateo-Lozano, S.; Druckes, P.; Schachtele, C.; Kubbutat, M.; Liger, F.; Ma …
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RETV804M Kinase.
Newton R, Waszkowycz B, Seewooruthun C, Burschowsky D, Richards M, Hitchin S, Begum H, Watson A, French E, Hamilton N, Jones S, Lin LY, Waddell I, Echalier A, Bayliss R, Jordan AM, Ogilvie D. Newton R, et al. Among authors: echalier a. ACS Med Chem Lett. 2020 Feb 28;11(4):497-505. doi: 10.1021/acsmedchemlett.9b00615. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292556 Free PMC article.
Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases.
Bettayeb K, Tirado OM, Marionneau-Lambot S, Ferandin Y, Lozach O, Morris JC, Mateo-Lozano S, Drueckes P, Schächtele C, Kubbutat MH, Liger F, Marquet B, Joseph B, Echalier A, Endicott JA, Notario V, Meijer L. Bettayeb K, et al. Among authors: echalier a. Cancer Res. 2007 Sep 1;67(17):8325-34. doi: 10.1158/0008-5472.CAN-07-1826. Cancer Res. 2007. PMID: 17804748
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