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Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy.

Willoughby CE, Jiang Y, Thomas HD, Willmore E, Kyle S, Wittner A, Phillips N, Zhao Y, Tudhope SJ, Prendergast L, Junge G, Madia Lourenco L, Finlay MRV, Turner P, Munck JM, Griffin RJ, Rennison T, Pickles J, Cano C, Newell DR, Reeves HL, Ryan AJ, Wedge SR.

J Clin Invest. 2019 Oct 3. pii: 127483. doi: 10.1172/JCI127483. [Epub ahead of print]


Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.

Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C.

Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25.


Glucocorticoids and selumetinib are highly synergistic in RAS pathway-mutated childhood acute lymphoblastic leukemia through upregulation of BIM.

Matheson EC, Thomas H, Case M, Blair H, Jackson RK, Masic D, Veal G, Halsey C, Newell DR, Vormoor J, Irving JAE.

Haematologica. 2019 Sep;104(9):1804-1811. doi: 10.3324/haematol.2017.185975. Epub 2019 Jan 17.


Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma.

Chen L, Pastorino F, Berry P, Bonner J, Kirk C, Wood KM, Thomas HD, Zhao Y, Daga A, Veal GJ, Lunec J, Newell DR, Ponzoni M, Tweddle DA.

Int J Cancer. 2019 Jun 15;144(12):3146-3159. doi: 10.1002/ijc.32058. Epub 2019 Jan 9.


Highly Potent Clickable Probe for Cellular Imaging of MDM2 and Assessing Dynamic Responses to MDM2-p53 Inhibition.

Lebraud H, Noble RA, Phillips N, Heam K, Castro J, Zhao Y, Newell DR, Lunec J, Wedge SR, Heightman TD.

Bioconjug Chem. 2018 Jun 20;29(6):2100-2106. doi: 10.1021/acs.bioconjchem.8b00315. Epub 2018 Jun 12.


Sensitizing Ewing sarcoma to chemo- and radiotherapy by inhibition of the DNA-repair enzymes DNA protein kinase (DNA-PK) and poly-ADP-ribose polymerase (PARP) 1/2.

Vormoor B, Schlosser YT, Blair H, Sharma A, Wilkinson S, Newell DR, Curtin N.

Oncotarget. 2017 Sep 28;8(69):113418-113430. doi: 10.18632/oncotarget.21300. eCollection 2017 Dec 26.


PARP inhibitor rucaparib induces changes in NAD levels in cells and liver tissues as assessed by MRS.

Almeida GS, Bawn CM, Galler M, Wilson I, Thomas HD, Kyle S, Curtin NJ, Newell DR, Maxwell RJ.

NMR Biomed. 2017 Sep;30(9). doi: 10.1002/nbm.3736. Epub 2017 May 22.


Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor.

Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV.

Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24.


Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.

Coxon CR, Anscombe E, Harnor SJ, Martin MP, Carbain B, Golding BT, Hardcastle IR, Harlow LK, Korolchuk S, Matheson CJ, Newell DR, Noble ME, Sivaprakasam M, Tudhope SJ, Turner DM, Wang LZ, Wedge SR, Wong C, Griffin RJ, Endicott JA, Cano C.

J Med Chem. 2017 Mar 9;60(5):1746-1767. doi: 10.1021/acs.jmedchem.6b01254. Epub 2017 Feb 14.


Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037.

Haagensen EJ, Thomas HD, Schmalix WA, Payne AC, Kevorkian L, Allen RA, Bevan P, Maxwell RJ, Newell DR.

Cancer Chemother Pharmacol. 2016 Dec;78(6):1269-1281. doi: 10.1007/s00280-016-3186-4. Epub 2016 Nov 11.


Structure-guided design of purine-based probes for selective Nek2 inhibition.

Coxon CR, Wong C, Bayliss R, Boxall K, Carr KH, Fry AM, Hardcastle IR, Matheson CJ, Newell DR, Sivaprakasam M, Thomas H, Turner D, Yeoh S, Wang LZ, Griffin RJ, Golding BT, Cano C.

Oncotarget. 2017 Mar 21;8(12):19089-19124. doi: 10.18632/oncotarget.13249.


Sulfatase-2: a prognostic biomarker and candidate therapeutic target in patients with pancreatic ductal adenocarcinoma.

Alhasan SF, Haugk B, Ogle LF, Beale GS, Long A, Burt AD, Tiniakos D, Televantou D, Coxon F, Newell DR, Charnley R, Reeves HL.

Br J Cancer. 2016 Sep 27;115(7):797-804. doi: 10.1038/bjc.2016.264. Epub 2016 Aug 25.


Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer.

Beale G, Haagensen EJ, Thomas HD, Wang LZ, Revill CH, Payne SL, Golding BT, Hardcastle IR, Newell DR, Griffin RJ, Cano C.

Br J Cancer. 2016 Sep 6;115(6):682-90. doi: 10.1038/bjc.2016.238. Epub 2016 Aug 16.


High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors.

Myers SM, Bawn RH, Bisset LC, Blackburn TJ, Cottyn B, Molyneux L, Wong AC, Cano C, Clegg W, Harrington RW, Leung H, Rigoreau L, Vidot S, Golding BT, Griffin RJ, Hammonds T, Newell DR, Hardcastle IR.

ACS Comb Sci. 2016 Aug 8;18(8):444-55. doi: 10.1021/acscombsci.5b00155. Epub 2016 Jul 20.


TP53 mutant MDM2-amplified cell lines selected for resistance to MDM2-p53 binding antagonists retain sensitivity to ionizing radiation.

Drummond CJ, Esfandiari A, Liu J, Lu X, Hutton C, Jackson J, Bennaceur K, Xu Q, Makimanejavali AR, Del Bello F, Piergentili A, Newell DR, Hardcastle IR, Griffin RJ, Lunec J.

Oncotarget. 2016 Jul 19;7(29):46203-46218. doi: 10.18632/oncotarget.10073.


Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases.

Reuillon T, Alhasan SF, Beale GS, Bertoli A, Brennan A, Cano C, Reeves HL, Newell DR, Golding BT, Miller DC, Griffin RJ.

Chem Sci. 2016 Apr 21;7(4):2821-2826. doi: 10.1039/c5sc03612g. Epub 2016 Jan 11.


Tumor cells with KRAS or BRAF mutations or ERK5/MAPK7 amplification are not addicted to ERK5 activity for cell proliferation.

Lochhead PA, Clark J, Wang LZ, Gilmour L, Squires M, Gilley R, Foxton C, Newell DR, Wedge SR, Cook SJ.

Cell Cycle. 2016;15(4):506-18. doi: 10.1080/15384101.2015.1120915.


Pre-clinical use of isogenic cell lines and tumours in vitro and in vivo for predictive biomarker discovery; impact of KRAS and PI3KCA mutation status on MEK inhibitor activity is model dependent.

Haagensen EJ, Thomas HD, Mudd C, Tsonou E, Wiggins CM, Maxwell RJ, Moore JD, Newell DR.

Eur J Cancer. 2016 Mar;56:69-76. doi: 10.1016/j.ejca.2015.12.012. Epub 2016 Jan 25.


Identification and Characterization of an Irreversible Inhibitor of CDK2.

Anscombe E, Meschini E, Mora-Vidal R, Martin MP, Staunton D, Geitmann M, Danielson UH, Stanley WA, Wang LZ, Reuillon T, Golding BT, Cano C, Newell DR, Noble ME, Wedge SR, Endicott JA, Griffin RJ.

Chem Biol. 2015 Sep 17;22(9):1159-64. doi: 10.1016/j.chembiol.2015.07.018. Epub 2015 Aug 27.


Regioselective sulfamoylation at low temperature enables concise syntheses of putative small molecule inhibitors of sulfatases.

Miller DC, Carbain B, Beale GS, Alhasan SF, Reeves HL, Baisch U, Newell DR, Golding BT, Griffin RJ.

Org Biomol Chem. 2015 May 14;13(18):5279-84. doi: 10.1039/c5ob00211g.


Pre-clinical evaluation of the MDM2-p53 antagonist RG7388 alone and in combination with chemotherapy in neuroblastoma.

Chen L, Rousseau RF, Middleton SA, Nichols GL, Newell DR, Lunec J, Tweddle DA.

Oncotarget. 2015 Apr 30;6(12):10207-21.


SKP2 is a direct transcriptional target of MYCN and a potential therapeutic target in neuroblastoma.

Evans L, Chen L, Milazzo G, Gherardi S, Perini G, Willmore E, Newell DR, Tweddle DA.

Cancer Lett. 2015 Jul 10;363(1):37-45. doi: 10.1016/j.canlet.2015.03.044. Epub 2015 Apr 2.


Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach.

Zaytsev A, Dodd B, Magnani M, Ghiron C, Golding BT, Griffin RJ, Liu J, Lu X, Micco I, Newell DR, Padova A, Robertson G, Lunec J, Hardcastle IR.

Chem Biol Drug Des. 2015 Aug;86(2):180-9. doi: 10.1111/cbdd.12474. Epub 2014 Dec 19.


Structurally diverse MDM2-p53 antagonists act as modulators of MDR-1 function in neuroblastoma.

Chen L, Zhao Y, Halliday GC, Berry P, Rousseau RF, Middleton SA, Nichols GL, Del Bello F, Piergentili A, Newell DR, Lunec J, Tweddle DA.

Br J Cancer. 2014 Aug 12;111(4):716-25. doi: 10.1038/bjc.2014.325. Epub 2014 Jun 12.


Pharmacologic biomarkers in the development of stratified cancer medicine.

Figg WD, Newell DR.

Clin Cancer Res. 2014 May 15;20(10):2525-9. doi: 10.1158/1078-0432.CCR-14-0511.


The enhanced in vivo activity of the combination of a MEK and a PI3K inhibitor correlates with [18F]-FLT PET in human colorectal cancer xenograft tumour-bearing mice.

Haagensen EJ, Thomas HD, Wilson I, Harnor SJ, Payne SL, Rennison T, Smith KM, Maxwell RJ, Newell DR.

PLoS One. 2013 Dec 10;8(12):e81763. doi: 10.1371/journal.pone.0081763. eCollection 2013.


8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.

Carbain B, Paterson DJ, Anscombe E, Campbell AJ, Cano C, Echalier A, Endicott JA, Golding BT, Haggerty K, Hardcastle IR, Jewsbury PJ, Newell DR, Noble ME, Roche C, Wang LZ, Griffin RJ.

J Med Chem. 2014 Jan 9;57(1):56-70. doi: 10.1021/jm401555v. Epub 2013 Dec 23.


1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.

Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA, Newell DR, Richardson CJ, Shea K, Smith GC, Thommes P, Ting A, Griffin RJ.

J Med Chem. 2013 Aug 22;56(16):6386-401. doi: 10.1021/jm400915j. Epub 2013 Aug 1.


Preclinical evaluation of a novel ATM inhibitor, KU59403, in vitro and in vivo in p53 functional and dysfunctional models of human cancer.

Batey MA, Zhao Y, Kyle S, Richardson C, Slade A, Martin NM, Lau A, Newell DR, Curtin NJ.

Mol Cancer Ther. 2013 Jun;12(6):959-67. doi: 10.1158/1535-7163.MCT-12-0707. Epub 2013 Mar 19.


Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer.

Coffey K, Blackburn TJ, Cook S, Golding BT, Griffin RJ, Hardcastle IR, Hewitt L, Huberman K, McNeill HV, Newell DR, Roche C, Ryan-Munden CA, Watson A, Robson CN.

PLoS One. 2012;7(10):e45539. doi: 10.1371/journal.pone.0045539. Epub 2012 Oct 8.


Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.

Munck JM, Batey MA, Zhao Y, Jenkins H, Richardson CJ, Cano C, Tavecchio M, Barbeau J, Bardos J, Cornell L, Griffin RJ, Menear K, Slade A, Thommes P, Martin NM, Newell DR, Smith GC, Curtin NJ.

Mol Cancer Ther. 2012 Aug;11(8):1789-98. doi: 10.1158/1535-7163.MCT-11-0535. Epub 2012 May 10.


The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition.

Haagensen EJ, Kyle S, Beale GS, Maxwell RJ, Newell DR.

Br J Cancer. 2012 Apr 10;106(8):1386-94. doi: 10.1038/bjc.2012.70. Epub 2012 Mar 13.


MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.

Watson AF, Liu J, Bennaceur K, Drummond CJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Lu X, McDonnell JM, Newell DR, Noble ME, Revill CH, Riedinger C, Xu Q, Zhao Y, Lunec J, Hardcastle IR.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5916-9. doi: 10.1016/j.bmcl.2011.07.084. Epub 2011 Aug 9.


Potent, selective inhibitors of fibroblast growth factor receptor define fibroblast growth factor dependence in preclinical cancer models.

Squires M, Ward G, Saxty G, Berdini V, Cleasby A, King P, Angibaud P, Perera T, Fazal L, Ross D, Jones CG, Madin A, Benning RK, Vickerstaffe E, O'Brien A, Frederickson M, Reader M, Hamlett C, Batey MA, Rich S, Carr M, Miller D, Feltell R, Thiru A, Bethell S, Devine LA, Graham BL, Pike A, Cosme J, Lewis EJ, Freyne E, Lyons J, Irving J, Murray C, Newell DR, Thompson NT.

Mol Cancer Ther. 2011 Sep;10(9):1542-52. doi: 10.1158/1535-7163.MCT-11-0426. Epub 2011 Jul 15.


Compromised CDK1 activity sensitizes BRCA-proficient cancers to PARP inhibition.

Johnson N, Li YC, Walton ZE, Cheng KA, Li D, Rodig SJ, Moreau LA, Unitt C, Bronson RT, Thomas HD, Newell DR, D'Andrea AD, Curtin NJ, Wong KK, Shapiro GI.

Nat Med. 2011 Jun 26;17(7):875-82. doi: 10.1038/nm.2377.


Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination.

Tavecchio M, Munck JM, Cano C, Newell DR, Curtin NJ.

Cancer Chemother Pharmacol. 2012 Jan;69(1):155-64. doi: 10.1007/s00280-011-1662-4. Epub 2011 Jun 1.


Thiothymidine combined with UVA as a potential novel therapy for bladder cancer.

Pridgeon SW, Heer R, Taylor GA, Newell DR, O'Toole K, Robinson M, Xu YZ, Karran P, Boddy AV.

Br J Cancer. 2011 Jun 7;104(12):1869-76. doi: 10.1038/bjc.2011.180. Epub 2011 May 24.


Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301.

Thomas HD, Wang LZ, Roche C, Bentley J, Cheng Y, Hardcastle IR, Golding BT, Griffin RJ, Curtin NJ, Newell DR.

Eur J Cancer. 2011 Sep;47(13):2052-9. doi: 10.1016/j.ejca.2011.04.008. Epub 2011 May 12.


Nucleoside transport inhibitors: structure-activity relationships for pyrimido[5,4-d]pyrimidine derivatives that potentiate pemetrexed cytotoxicity in the presence of α1-acid glycoprotein.

Saravanan K, Barlow HC, Barton M, Calvert AH, Golding BT, Newell DR, Northen JS, Curtin NJ, Thomas HD, Griffin RJ.

J Med Chem. 2011 Mar 24;54(6):1847-59. doi: 10.1021/jm101493z. Epub 2011 Mar 2.


Comparative pre-clinical evaluation of receptor tyrosine kinase inhibitors for the treatment of multiple myeloma.

de Brito LR, Batey MA, Zhao Y, Squires MS, Maitland H, Leung HY, Hall AG, Jackson G, Newell DR, Irving JA.

Leuk Res. 2011 Sep;35(9):1233-40. doi: 10.1016/j.leukres.2011.01.011. Epub 2011 Feb 11.


Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.

Hardcastle IR, Liu J, Valeur E, Watson A, Ahmed SU, Blackburn TJ, Bennaceur K, Clegg W, Drummond C, Endicott JA, Golding BT, Griffin RJ, Gruber J, Haggerty K, Harrington RW, Hutton C, Kemp S, Lu X, McDonnell JM, Newell DR, Noble ME, Payne SL, Revill CH, Riedinger C, Xu Q, Lunec J.

J Med Chem. 2011 Mar 10;54(5):1233-43. doi: 10.1021/jm1011929. Epub 2011 Feb 11.


DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotype.

Cano C, Barbeau OR, Bailey C, Cockcroft XL, Curtin NJ, Duggan H, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Knights C, Menear KA, Newell DR, Richardson CJ, Smith GC, Spittle B, Griffin RJ.

J Med Chem. 2010 Dec 23;53(24):8498-507. doi: 10.1021/jm100608j. Epub 2010 Nov 16.


Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors.

Marchetti F, Cano C, Curtin NJ, Golding BT, Griffin RJ, Haggerty K, Newell DR, Parsons RJ, Payne SL, Wang LZ, Hardcastle IR.

Org Biomol Chem. 2010 May 21;8(10):2397-407. doi: 10.1039/b925481a. Epub 2010 Mar 18.


Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells.

Johnson N, Bentley J, Wang LZ, Newell DR, Robson CN, Shapiro GI, Curtin NJ.

Br J Cancer. 2010 Jan 19;102(2):342-50. doi: 10.1038/sj.bjc.6605479. Epub 2009 Dec 15.


Preclinical evaluation of a novel pyrimidopyrimidine for the prevention of nucleoside and nucleobase reversal of antifolate cytotoxicity.

Thomas HD, Saravanan K, Wang LZ, Lin MJ, Northen JS, Barlow H, Barton M, Newell DR, Griffin RJ, Golding BT, Curtin NJ.

Mol Cancer Ther. 2009 Jul;8(7):1828-37. doi: 10.1158/1535-7163.MCT-08-1208. Epub 2009 Jun 9.


The kinase inhibitor O6-cyclohexylmethylguanine (NU2058) potentiates the cytotoxicity of cisplatin by mechanisms that are independent of its effect upon CDK2.

Harrison LR, Ottley CJ, Pearson DG, Roche C, Wedge SR, Dolan ME, Newell DR, Tilby MJ.

Biochem Pharmacol. 2009 May 15;77(10):1586-92. doi: 10.1016/j.bcp.2009.02.018. Epub 2009 Mar 5.


Transient treatment with CDK inhibitors eliminates proliferative potential even when their abilities to evoke apoptosis and DNA damage are blocked.

Scrace SF, Kierstan P, Borgognoni J, Wang LZ, Denny S, Wayne J, Bentley C, Cansfield AD, Jackson PS, Lockie AM, Curtin NJ, Newell DR, Williamson DS, Moore JD.

Cell Cycle. 2008 Dec 15;7(24):3898-907. Epub 2008 Dec 4.


Pharmacokinetic investigation of imatinib using accelerator mass spectrometry in patients with chronic myeloid leukemia.

Boddy AV, Sludden J, Griffin MJ, Garner C, Kendrick J, Mistry P, Dutreix C, Newell DR, O'Brien SG.

Clin Cancer Res. 2007 Jul 15;13(14):4164-9.


Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2.

Marchetti F, Sayle KL, Bentley J, Clegg W, Curtin NJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Harrington RW, Mesguiche V, Newell DR, Noble ME, Parsons RJ, Pratt DJ, Wang LZ, Hardcastle IR.

Org Biomol Chem. 2007 May 21;5(10):1577-85. Epub 2007 Apr 23.


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