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Page 1
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.
Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D. Clarke PA, et al. Among authors: box g. Elife. 2016 Dec 9;5:e20722. doi: 10.7554/eLife.20722. Elife. 2016. PMID: 27935476 Free PMC article.
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J. Dale T, et al. Among authors: box g. Nat Chem Biol. 2015 Dec;11(12):973-980. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26. Nat Chem Biol. 2015. PMID: 26502155 Free PMC article.
The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106.
Walton MI, Eve PD, Hayes A, Valenti M, De Haven Brandon A, Box G, Boxall KJ, Aherne GW, Eccles SA, Raynaud FI, Williams DH, Reader JC, Collins I, Garrett MD. Walton MI, et al. Among authors: box g. Mol Cancer Ther. 2010 Jan;9(1):89-100. doi: 10.1158/1535-7163.MCT-09-0938. Epub 2010 Jan 6. Mol Cancer Ther. 2010. PMID: 20053762 Free article.
Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.
Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, Raynaud FI, Workman P, Eccles SA, Bayliss R, Linardopoulos S, Blagg J. Bavetsias V, et al. Among authors: box g. J Med Chem. 2012 Oct 25;55(20):8721-34. doi: 10.1021/jm300952s. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 23043539 Free PMC article.
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J. Mallinger A, et al. Among authors: box g. J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13. J Med Chem. 2015. PMID: 25680029 Free PMC article.
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, Perkins ND, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Collins I, Garrett MD. Walton MI, et al. Among authors: box g. Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919. Oncotarget. 2016. PMID: 26295308 Free PMC article.
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S. Innocenti P, et al. Among authors: box g. J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7. J Med Chem. 2016. PMID: 27055065 Free article.
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: box g. 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.
Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma.
Ang JE, Pal A, Asad YJ, Henley AT, Valenti M, Box G, de Haven Brandon A, Revell VL, Skene DJ, Venturi M, Rueger R, Meresse V, Eccles SA, de Bono JS, Kaye SB, Workman P, Banerji U, Raynaud FI. Ang JE, et al. Among authors: box g. Mol Cancer Ther. 2017 Oct;16(10):2315-2323. doi: 10.1158/1535-7163.MCT-16-0881. Epub 2017 Jun 21. Mol Cancer Ther. 2017. PMID: 28637716 Free PMC article.
Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736.
Moore AS, Faisal A, Mak GWY, Miraki-Moud F, Bavetsias V, Valenti M, Box G, Hallsworth A, de Haven Brandon A, Xavier CPR, Stronge R, Pearson ADJ, Blagg J, Raynaud FI, Chopra R, Eccles SA, Taussig DC, Linardopoulos S. Moore AS, et al. Among authors: box g. Blood Adv. 2020 Apr 14;4(7):1478-1491. doi: 10.1182/bloodadvances.2019000986. Blood Adv. 2020. PMID: 32282883 Free PMC article.
150 results