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Items: 31


3D growth of cancer cells elicits sensitivity to kinase inhibitors but not lipid metabolism modifiers.

Jones DT, Valli A, Haider S, Zang Q, Smethurst E, Schug ZT, Peck B, Aboagye EO, Critchlow SE, Schulze A, Gottlieb E, Wakelam MJO, Harris AL.

Mol Cancer Ther. 2018 Nov 26. pii: molcanther.0857.2018. doi: 10.1158/1535-7163.MCT-17-0857. [Epub ahead of print]


Statin-induced metabolic reprogramming in head and neck cancer: a biomarker for targeting monocarboxylate transporters.

Mehibel M, Ortiz-Martinez F, Voelxen N, Boyers A, Chadwick A, Telfer BA, Mueller-Klieser W, West CM, Critchlow SE, Williams KJ, Stratford IJ.

Sci Rep. 2018 Nov 14;8(1):16804. doi: 10.1038/s41598-018-35103-1.


Combined Inhibition of PI3Kβ and mTOR Inhibits Growth of PTEN-null Tumors.

Lynch JT, Polanska UM, Hancox U, Delpuech O, Maynard J, Trigwell C, Eberlein C, Lenaghan C, Polanski R, Avivar-Valderas A, Cumberbatch M, Klinowska T, Critchlow SE, Cruzalegui F, Barry ST.

Mol Cancer Ther. 2018 Nov;17(11):2309-2319. doi: 10.1158/1535-7163.MCT-18-0183. Epub 2018 Aug 10.


Quantitation of Endogenous Metabolites in Mouse Tumors Using Mass-Spectrometry Imaging.

Swales JG, Dexter A, Hamm G, Nilsson A, Strittmatter N, Michopoulos F, Hardy C, Morentin-Gutierrez P, Mellor M, Andren PE, Clench MR, Bunch J, Critchlow SE, Goodwin RJA.

Anal Chem. 2018 May 15;90(10):6051-6058. doi: 10.1021/acs.analchem.7b05239. Epub 2018 Apr 26.


Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt's lymphoma anti-tumor activity.

Curtis NJ, Mooney L, Hopcroft L, Michopoulos F, Whalley N, Zhong H, Murray C, Logie A, Revill M, Byth KF, Benjamin AD, Firth MA, Green S, Smith PD, Critchlow SE.

Oncotarget. 2017 May 25;8(41):69219-69236. doi: 10.18632/oncotarget.18215. eCollection 2017 Sep 19.


Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors.

Lynch JT, Polanska UM, Delpuech O, Hancox U, Trinidad AG, Michopoulos F, Lenaghan C, McEwen R, Bradford J, Polanski R, Ellston R, Avivar-Valderas A, Pilling J, Staniszewska A, Cumberbatch M, Critchlow SE, Cruzalegui F, Barry ST.

Clin Cancer Res. 2017 Dec 15;23(24):7584-7595. doi: 10.1158/1078-0432.CCR-17-0676. Epub 2017 Oct 2.


A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors.

St-Gallay SA, Bennett N, Critchlow SE, Curtis N, Davies G, Debreczeni J, Evans N, Hardern I, Holdgate G, Jones NP, Leach L, Maman S, McLoughlin S, Preston M, Rigoreau L, Thomas A, Turnbull AP, Walker G, Walsh J, Ward RA, Wheatley E, Winter-Holt J.

SLAS Discov. 2018 Jan;23(1):11-22. doi: 10.1177/2472555217732289. Epub 2017 Sep 25.


Pyruvate dehydrogenase kinase 4 exhibits a novel role in the activation of mutant KRAS, regulating cell growth in lung and colorectal tumour cells.

Trinidad AG, Whalley N, Rowlinson R, Delpuech O, Dudley P, Rooney C, Critchlow SE.

Oncogene. 2017 Nov 2;36(44):6164-6176. doi: 10.1038/onc.2017.224. Epub 2017 Jul 10.


Inhibition of monocarboxyate transporter 1 by AZD3965 as a novel therapeutic approach for diffuse large B-cell lymphoma and Burkitt lymphoma.

Noble RA, Bell N, Blair H, Sikka A, Thomas H, Phillips N, Nakjang S, Miwa S, Crossland R, Rand V, Televantou D, Long A, Keun HC, Bacon CM, Bomken S, Critchlow SE, Wedge SR.

Haematologica. 2017 Jul;102(7):1247-1257. doi: 10.3324/haematol.2016.163030. Epub 2017 Apr 6.


Targeted Metabolic Profiling of the Tg197 Mouse Model Reveals Itaconic Acid as a Marker of Rheumatoid Arthritis.

Michopoulos F, Karagianni N, Whalley NM, Firth MA, Nikolaou C, Wilson ID, Critchlow SE, Kollias G, Theodoridis GA.

J Proteome Res. 2016 Dec 2;15(12):4579-4590. Epub 2016 Oct 28.


Inhibition of fatty acid desaturation is detrimental to cancer cell survival in metabolically compromised environments.

Peck B, Schug ZT, Zhang Q, Dankworth B, Jones DT, Smethurst E, Patel R, Mason S, Jiang M, Saunders R, Howell M, Mitter R, Spencer-Dene B, Stamp G, McGarry L, James D, Shanks E, Aboagye EO, Critchlow SE, Leung HY, Harris AL, Wakelam MJO, Gottlieb E, Schulze A.

Cancer Metab. 2016 Apr 1;4:6. doi: 10.1186/s40170-016-0146-8. eCollection 2016.


MCT1 Modulates Cancer Cell Pyruvate Export and Growth of Tumors that Co-express MCT1 and MCT4.

Hong CS, Graham NA, Gu W, Espindola Camacho C, Mah V, Maresh EL, Alavi M, Bagryanova L, Krotee PAL, Gardner BK, Behbahan IS, Horvath S, Chia D, Mellinghoff IK, Hurvitz SA, Dubinett SM, Critchlow SE, Kurdistani SK, Goodglick L, Braas D, Graeber TG, Christofk HR.

Cell Rep. 2016 Feb 23;14(7):1590-1601. doi: 10.1016/j.celrep.2016.01.057. Epub 2016 Feb 11.


Leptin, BMI, and a Metabolic Gene Expression Signature Associated with Clinical Outcome to VEGF Inhibition in Colorectal Cancer.

Pommier AJ, Farren M, Patel B, Wappett M, Michopoulos F, Smith NR, Kendrew J, Frith J, Huby R, Eberlein C, Campbell H, Womack C, Smith PD, Robertson J, Morgan S, Critchlow SE, Barry ST.

Cell Metab. 2016 Jan 12;23(1):77-93. doi: 10.1016/j.cmet.2015.10.015. Epub 2015 Nov 25.


Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.

Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J.

J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13.


Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.

Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D.

J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub 2015 Mar 12.


Acetyl-CoA synthetase 2 promotes acetate utilization and maintains cancer cell growth under metabolic stress.

Schug ZT, Peck B, Jones DT, Zhang Q, Grosskurth S, Alam IS, Goodwin LM, Smethurst E, Mason S, Blyth K, McGarry L, James D, Shanks E, Kalna G, Saunders RE, Jiang M, Howell M, Lassailly F, Thin MZ, Spencer-Dene B, Stamp G, van den Broek NJ, Mackay G, Bulusu V, Kamphorst JJ, Tardito S, Strachan D, Harris AL, Aboagye EO, Critchlow SE, Wakelam MJ, Schulze A, Gottlieb E.

Cancer Cell. 2015 Jan 12;27(1):57-71. doi: 10.1016/j.ccell.2014.12.002.


Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport.

Bola BM, Chadwick AL, Michopoulos F, Blount KG, Telfer BA, Williams KJ, Smith PD, Critchlow SE, Stratford IJ.

Mol Cancer Ther. 2014 Dec;13(12):2805-16. doi: 10.1158/1535-7163.MCT-13-1091. Epub 2014 Oct 3.


Emerging approaches to target tumor metabolism.

Ross SJ, Critchlow SE.

Curr Opin Pharmacol. 2014 Aug;17:22-9. doi: 10.1016/j.coph.2014.07.001. Epub 2014 Jul 19. Review.


Targeted profiling of polar intracellular metabolites using ion-pair-high performance liquid chromatography and -ultra high performance liquid chromatography coupled to tandem mass spectrometry: applications to serum, urine and tissue extracts.

Michopoulos F, Whalley N, Theodoridis G, Wilson ID, Dunkley TP, Critchlow SE.

J Chromatogr A. 2014 Jul 4;1349:60-8. doi: 10.1016/j.chroma.2014.05.019. Epub 2014 May 12.


Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer.

Polański R, Hodgkinson CL, Fusi A, Nonaka D, Priest L, Kelly P, Trapani F, Bishop PW, White A, Critchlow SE, Smith PD, Blackhall F, Dive C, Morrow CJ.

Clin Cancer Res. 2014 Feb 15;20(4):926-937. doi: 10.1158/1078-0432.CCR-13-2270. Epub 2013 Nov 25.


AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo.

Loddick SA, Ross SJ, Thomason AG, Robinson DM, Walker GE, Dunkley TP, Brave SR, Broadbent N, Stratton NC, Trueman D, Mouchet E, Shaheen FS, Jacobs VN, Cumberbatch M, Wilson J, Jones RD, Bradbury RH, Rabow A, Gaughan L, Womack C, Barry ST, Robson CN, Critchlow SE, Wedge SR, Brooks AN.

Mol Cancer Ther. 2013 Sep;12(9):1715-27. doi: 10.1158/1535-7163.MCT-12-1174. Epub 2013 Jul 16.


Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.

Finlay MR, Buttar D, Critchlow SE, Dishington AP, Fillery SM, Fisher E, Glossop SC, Graham MA, Johnson T, Lamont GM, Mutton S, Perkins P, Pike KG, Slater AM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4163-8. doi: 10.1016/j.bmcl.2012.04.036. Epub 2012 Apr 13.


CD147 subunit of lactate/H+ symporters MCT1 and hypoxia-inducible MCT4 is critical for energetics and growth of glycolytic tumors.

Le Floch R, Chiche J, Marchiq I, Naiken T, Ilc K, Murray CM, Critchlow SE, Roux D, Simon MP, Pouysségur J.

Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16663-8. doi: 10.1073/pnas.1106123108. Epub 2011 Sep 19. Erratum in: Proc Natl Acad Sci U S A. 2012 Dec 4;109(49):20166. Naïken, Tanesha [corrected to Naiken, Tanesha]; Ilk, Karine [corrected to Ilc, Karine].


AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity.

Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M.

Cancer Res. 2010 Jan 1;70(1):288-98. doi: 10.1158/0008-5472.CAN-09-1751. Epub 2009 Dec 22.


Crystal structure of an Xrcc4-DNA ligase IV complex.

Sibanda BL, Critchlow SE, Begun J, Pei XY, Jackson SP, Blundell TL, Pellegrini L.

Nat Struct Biol. 2001 Dec;8(12):1015-9.


Identification of a defect in DNA ligase IV in a radiosensitive leukaemia patient.

Riballo E, Critchlow SE, Teo SH, Doherty AJ, Priestley A, Broughton B, Kysela B, Beamish H, Plowman N, Arlett CF, Lehmann AR, Jackson SP, Jeggo PA.

Curr Biol. 1999 Jul 1;9(13):699-702.


DNA end-joining: from yeast to man.

Critchlow SE, Jackson SP.

Trends Biochem Sci. 1998 Oct;23(10):394-8. Review.


The interaction of the F plasmid killer protein, CcdB, with DNA gyrase: induction of DNA cleavage and blocking of transcription.

Critchlow SE, O'Dea MH, Howells AJ, Couturier M, Gellert M, Maxwell A.

J Mol Biol. 1997 Nov 7;273(4):826-39.


Mammalian DNA double-strand break repair protein XRCC4 interacts with DNA ligase IV.

Critchlow SE, Bowater RP, Jackson SP.

Curr Biol. 1997 Aug 1;7(8):588-98.


DNA cleavage is not required for the binding of quinolone drugs to the DNA gyrase-DNA complex.

Critchlow SE, Maxwell A.

Biochemistry. 1996 Jun 11;35(23):7387-93.


The complex of DNA gyrase and quinolone drugs with DNA forms a barrier to transcription by RNA polymerase.

Willmott CJ, Critchlow SE, Eperon IC, Maxwell A.

J Mol Biol. 1994 Sep 30;242(4):351-63.


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