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Page 1
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.
Whelligan DK, Solanki S, Taylor D, Thomson DW, Cheung KM, Boxall K, Mas-Droux C, Barillari C, Burns S, Grummitt CG, Collins I, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Whelligan DK, et al. Among authors: mas droux c. J Med Chem. 2010 Nov 11;53(21):7682-98. doi: 10.1021/jm1008727. J Med Chem. 2010. PMID: 20936789 Free PMC article.
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.
Solanki S, Innocenti P, Mas-Droux C, Boxall K, Barillari C, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Solanki S, et al. Among authors: mas droux c. J Med Chem. 2011 Mar 24;54(6):1626-39. doi: 10.1021/jm1011726. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366329
Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.
Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S. Innocenti P, et al. Among authors: mas droux c. J Med Chem. 2012 Apr 12;55(7):3228-41. doi: 10.1021/jm201683b. Epub 2012 Mar 23. J Med Chem. 2012. PMID: 22404346 Free PMC article.
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.
Matheson CJ, Coxon CR, Bayliss R, Boxall K, Carbain B, Fry AM, Hardcastle IR, Harnor SJ, Mas-Droux C, Newell DR, Richards MW, Sivaprakasam M, Turner D, Griffin RJ, Golding BT, Cano C. Matheson CJ, et al. Among authors: mas droux c. RSC Med Chem. 2020 May 22;11(6):707-731. doi: 10.1039/d0md00074d. eCollection 2020 Jun 1. RSC Med Chem. 2020. PMID: 33479670 Free PMC article.
11 results