Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 61


Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease.

Colombano G, Caldwell JJ, Matthews TP, Bhatia C, Joshi A, McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R, Collins I.

J Med Chem. 2019 Mar 14;62(5):2447-2465. doi: 10.1021/acs.jmedchem.8b01721. Epub 2019 Mar 5.


Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.

Whittaker SR, Barlow C, Martin MP, Mancusi C, Wagner S, Self A, Barrie E, Te Poele R, Sharp S, Brown N, Wilson S, Jackson W, Fischer PM, Clarke PA, Walton MI, McDonald E, Blagg J, Noble M, Garrett MD, Workman P.

Mol Oncol. 2018 Mar;12(3):287-304. doi: 10.1002/1878-0261.12148. Epub 2018 Jan 28.


DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer.

Kanu N, Cerone MA, Goh G, Zalmas LP, Bartkova J, Dietzen M, McGranahan N, Rogers R, Law EK, Gromova I, Kschischo M, Walton MI, Rossanese OW, Bartek J, Harris RS, Venkatesan S, Swanton C.

Genome Biol. 2016 Sep 15;17(1):185. doi: 10.1186/s13059-016-1042-9.


Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM, Lamers MB, Reader JC, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2016 Jun 9;59(11):5221-37. doi: 10.1021/acs.jmedchem.5b01938. Epub 2016 May 23.


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.

Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919.


Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.

Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2012 Nov 26;55(22):10229-40. doi: 10.1021/jm3012933. Epub 2012 Oct 19.


CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs.

Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD.

Clin Cancer Res. 2012 Oct 15;18(20):5650-61. doi: 10.1158/1078-0432.CCR-12-1322. Epub 2012 Aug 28.


AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.

Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD.

Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 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.

J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23.


CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

Anderson VE, Walton MI, Eve PD, Boxall KJ, Antoni L, Caldwell JJ, Aherne W, Pearl LH, Oliver AW, Collins I, Garrett MD.

Cancer Res. 2011 Jan 15;71(2):463-72. doi: 10.1158/0008-5472.CAN-10-1252.


Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.


AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.

Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD.

Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27.


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.

Mol Cancer Ther. 2010 Jan;9(1):89-100. doi: 10.1158/1535-7163.MCT-09-0938. Epub 2010 Jan 6.


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.

J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j.


Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises.

Yap TA, Garrett MD, Walton MI, Raynaud F, de Bono JS, Workman P.

Curr Opin Pharmacol. 2008 Aug;8(4):393-412. doi: 10.1016/j.coph.2008.08.004. Epub 2008 Aug 27. Review.


The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis.

Whittaker SR, Te Poele RH, Chan F, Linardopoulos S, Walton MI, Garrett MD, Workman P.

Cell Cycle. 2007 Dec 15;6(24):3114-31. Epub 2007 Oct 5.


An evaluation of the ability of pifithrin-alpha and -beta to inhibit p53 function in two wild-type p53 human tumor cell lines.

Walton MI, Wilson SC, Hardcastle IR, Mirza AR, Workman P.

Mol Cancer Ther. 2005 Sep;4(9):1369-77.


In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.

Raynaud FI, Whittaker SR, Fischer PM, McClue S, Walton MI, Barrie SE, Garrett MD, Rogers P, Clarke SJ, Kelland LR, Valenti M, Brunton L, Eccles S, Lane DP, Workman P.

Clin Cancer Res. 2005 Jul 1;11(13):4875-87.


Disruption of WT1 gene expression and exon 5 splicing following cytotoxic drug treatment: antisense down-regulation of exon 5 alters target gene expression and inhibits cell survival.

Renshaw J, Orr RM, Walton MI, Te Poele R, Williams RD, Wancewicz EV, Monia BP, Workman P, Pritchard-Jones K.

Mol Cancer Ther. 2004 Nov;3(11):1467-84.


Magnetic resonance spectroscopic pharmacodynamic markers of the heat shock protein 90 inhibitor 17-allylamino,17-demethoxygeldanamycin (17AAG) in human colon cancer models.

Chung YL, Troy H, Banerji U, Jackson LE, Walton MI, Stubbs M, Griffiths JR, Judson IR, Leach MO, Workman P, Ronen SM.

J Natl Cancer Inst. 2003 Nov 5;95(21):1624-33.


The contemporary drug development process: advances and challenges in preclinical and clinical development.

Garrett MD, Walton MI, McDonald E, Judson I, Workman P.

Prog Cell Cycle Res. 2003;5:145-58. Review.


Assays for HSP90 and inhibitors.

Aherne W, Maloney A, Prodromou C, Rowlands MG, Hardcastle A, Boxall K, Clarke P, Walton MI, Pearl L, Workman P.

Methods Mol Med. 2003;85:149-61. Review. No abstract available.


Effect of p53 status on sensitivity to platinum complexes in a human ovarian cancer cell line.

Pestell KE, Hobbs SM, Titley JC, Kelland LR, Walton MI.

Mol Pharmacol. 2000 Mar;57(3):503-11.


Pilot study of nimorazole as a hypoxic-cell sensitizer with the "chart" regimen in head and neck cancer.

Cottrill CP, Bishop K, Walton MI, Henk JM.

Int J Radiat Oncol Biol Phys. 1998 Nov 1;42(4):807-10.


The renal effects of the water-soluble, non-folylpolyglutamate synthetase-dependent thymidylate synthase inhibitor ZD9331 in mice.

Walton MI, Mitchell F, Aherne GW, Medlow CJ, Boyle FT, Jackman AL.

Br J Cancer. 1998 Dec;78(11):1457-63.


Preclinical pharmacology of CB30900, a novel dipeptide inhibitor of thymidylate synthase, in mice.

Walton MI, Gibson W, Aherne GW, Lawrence N, Stephens TC, Smith MN, Jackman AL.

J Pharmacol Exp Ther. 1996 May;277(2):909-16.


Preclinical pharmacology and antitumour activity of the novel sequence-selective DNA minor-groove cross-linking agent DSB-120.

Walton MI, Goddard P, Kelland LR, Thurston DE, Harrap KR.

Cancer Chemother Pharmacol. 1996;38(5):431-8.


Preclinical pharmacology of 1069C85, a novel tubulin binder.

Raynaud FI, Kelland LR, Walton MI, Judson IR.

Cancer Chemother Pharmacol. 1994;35(2):169-73.


Constitutive expression of human Bcl-2 modulates nitrogen mustard and camptothecin induced apoptosis.

Walton MI, Whysong D, O'Connor PM, Hockenbery D, Korsmeyer SJ, Kohn KW.

Cancer Res. 1993 Apr 15;53(8):1853-61.


Structure-activity relationships for DT-diaphorase reduction of hypoxic cell directed agents: indoloquinones and diaziridinyl benzoquinones.

Bailey SM, Suggett N, Walton MI, Workman P.

Int J Radiat Oncol Biol Phys. 1992;22(4):649-53.


The role of human and rodent DT-diaphorase in the reductive metabolism of hypoxic cell cytotoxins.

Walton MI, Sugget N, Workman P.

Int J Radiat Oncol Biol Phys. 1992;22(4):643-7.


DT-diaphorase activity correlates with sensitivity to the indoloquinone EO9 in mouse and human colon carcinomas.

Walton MI, Bibby MC, Double JA, Plumb JA, Workman P.

Eur J Cancer. 1992;28A(10):1597-600.


Decreased NADPH:cytochrome P-450 reductase activity and impaired drug activation in a mammalian cell line resistant to mitomycin C under aerobic but not hypoxic conditions.

Hoban PR, Walton MI, Robson CN, Godden J, Stratford IJ, Workman P, Harris AL, Hickson ID.

Cancer Res. 1990 Aug 1;50(15):4692-7.


DT-diaphorase: questionable role in mitomycin C resistance, but a target for novel bioreductive drugs?

Workman P, Walton MI, Powis G, Schlager JJ.

Br J Cancer. 1989 Nov;60(5):800-2; discussion 803. No abstract available. Erratum in: Br J Cancer 1990 Mar;61(3):492.


Molecular enzymology of the reductive bioactivation of hypoxic cell cytotoxins.

Walton MI, Wolf CR, Workman P.

Int J Radiat Oncol Biol Phys. 1989 Apr;16(4):983-6.


A microcomputer controlled, local hyperthermia system for uniform tumour heating in unanaesthetized mice.

Walton MI, Cattermole DM, Bleehen NM.

Int J Hyperthermia. 1989 Jan-Feb;5(1):53-8. No abstract available.


Pharmacokinetics and metabolism of the mixed-function hypoxic cell sensitizer prototype RSU 1069 in mice.

Walton MI, Workman P.

Cancer Chemother Pharmacol. 1988;22(4):275-81.


Interactions of hyperthermia with hypoxic cell sensitisers.

Bleehen NM, Walton MI, Workman P.

Recent Results Cancer Res. 1988;109:136-48. No abstract available.


Heat-stimulated nitroreductive bioactivation of the 2-nitroimidazole benznidazole in vitro.

Walton MI, Bleehen NM, Workman P.

Biochem Pharmacol. 1987 Aug 15;36(16):2627-32.


Supplemental Content

Loading ...
Support Center