vanMontfort RLM - Search Results

1

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.

Faisal A, Mak GWY, Gurden MD, Xavier CPR, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, Burke R, vanMontfort RLM, Blagg J, Raynaud FI, Eccles SA, Hoelder S, Linardopoulos S. Faisal A, et al. Among authors: vanmontfort rlm. Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23. Br J Cancer. 2017. PMID: 28334731 Free PMC article.

2

Insights into the conformational variability and regulation of human Nek2 kinase.

Westwood I, Cheary DM, Baxter JE, Richards MW, van Montfort RL, Fry AM, Bayliss R. Westwood I, et al. J Mol Biol. 2009 Feb 20;386(2):476-85. doi: 10.1016/j.jmb.2008.12.033. Epub 2008 Dec 24. J Mol Biol. 2009. PMID: 19124027 Free PMC article.

3

Identification of inhibitors of checkpoint kinase 1 through template screening.

Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, Collins I. Matthews TP, et al. J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j. J Med Chem. 2009. PMID: 19572549

4

Drugging the PI3 kinome: from chemical tools to drugs in the clinic.

Workman P, Clarke PA, Raynaud FI, van Montfort RL. Workman P, et al. Cancer Res. 2010 Mar 15;70(6):2146-57. doi: 10.1158/0008-5472.CAN-09-4355. Epub 2010 Feb 23. Cancer Res. 2010. PMID: 20179189 Free PMC article. Review.

5

Targeting HSP70: the second potentially druggable heat shock protein and molecular chaperone?

Powers MV, Jones K, Barillari C, Westwood I, van Montfort RL, Workman P. Powers MV, et al. Cell Cycle. 2010 Apr 15;9(8):1542-50. doi: 10.4161/cc.9.8.11204. Epub 2010 Apr 15. Cell Cycle. 2010. PMID: 20372081

6

Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.

Matthews TP, McHardy T, Klair S, Boxall K, Fisher M, Cherry M, Allen CE, Addison GJ, Ellard J, Aherne GW, Westwood IM, van Montfort R, Garrett MD, Reader JC, Collins I. Matthews TP, et al. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4045-9. doi: 10.1016/j.bmcl.2010.05.096. Epub 2010 May 27. Bioorg Med Chem Lett. 2010. PMID: 20561787

7

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. J Med Chem. 2010 Nov 11;53(21):7682-98. doi: 10.1021/jm1008727. J Med Chem. 2010. PMID: 20936789 Free PMC article.

8

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. J Med Chem. 2011 Mar 24;54(6):1626-39. doi: 10.1021/jm1011726. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366329

9

Analysis of water patterns in protein kinase binding sites.

Barillari C, Duncan AL, Westwood IM, Blagg J, van Montfort RL. Barillari C, et al. Proteins. 2011 Jul;79(7):2109-21. doi: 10.1002/prot.23032. Epub 2011 May 9. Proteins. 2011. PMID: 21557316

10

Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.

Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Reader JC, et al. J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22111927 Free PMC article.

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