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High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers.

Anderhub SJ, Mak GW, Gurden MD, Faisal A, Drosopoulos K, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, van Montfort RLM, Raynaud FI, Blagg J, Hoelder S, Eccles SA, Linardopoulos S.

Mol Cancer Ther. 2019 Oct;18(10):1696-1707. doi: 10.1158/1535-7163.MCT-18-1203.


Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.

Wood FL, Shepherd S, Hayes A, Liu M, Grira K, Mok Y, Atrash B, Faisal A, Bavetsias V, Linardopoulos S, Blagg J, Raynaud FI.

Eur J Pharm Sci. 2019 Nov 1;139:104899. doi: 10.1016/j.ejps.2019.04.004. Epub 2019 Apr 3.


Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development.

Drosopoulos K, Linardopoulos S.

Methods Mol Biol. 2019;1953:33-42. doi: 10.1007/978-1-4939-9145-7_3.


Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).

Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2018 Sep 27;61(18):8226-8240. doi: 10.1021/acs.jmedchem.8b00690. Epub 2018 Sep 10.


E-Cadherin/ROS1 Inhibitor Synthetic Lethality in Breast Cancer.

Bajrami I, Marlow R, van de Ven M, Brough R, Pemberton HN, Frankum J, Song F, Rafiq R, Konde A, Krastev DB, Menon M, Campbell J, Gulati A, Kumar R, Pettitt SJ, Gurden MD, Cardenosa ML, Chong I, Gazinska P, Wallberg F, Sawyer EJ, Martin LA, Dowsett M, Linardopoulos S, Natrajan R, Ryan CJ, Derksen PWB, Jonkers J, Tutt ANJ, Ashworth A, Lord CJ.

Cancer Discov. 2018 Apr;8(4):498-515. doi: 10.1158/2159-8290.CD-17-0603.


Integrated genomics and functional validation identifies malignant cell specific dependencies in triple negative breast cancer.

Patel N, Weekes D, Drosopoulos K, Gazinska P, Noel E, Rashid M, Mirza H, Quist J, Brasó-Maristany F, Mathew S, Ferro R, Pereira AM, Prince C, Noor F, Francesch-Domenech E, Marlow R, de Rinaldis E, Grigoriadis A, Linardopoulos S, Marra P, Tutt ANJ.

Nat Commun. 2018 Mar 13;9(1):1044. doi: 10.1038/s41467-018-03283-z.


Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells.

Koo CY, Giacomini C, Reyes-Corral M, Olmos Y, Tavares IA, Marson CM, Linardopoulos S, Tutt AN, Morris JDH.

Mol Cancer Ther. 2017 Nov;16(11):2410-2421. doi: 10.1158/1535-7163.MCT-17-0077. Epub 2017 Aug 22.


RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses.

Dolly SO, Gurden MD, Drosopoulos K, Clarke P, de Bono J, Kaye S, Workman P, Linardopoulos S.

Br J Cancer. 2017 Sep 26;117(7):954-964. doi: 10.1038/bjc.2017.277. Epub 2017 Aug 22.


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.

Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23.


Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis.

Gurden MD, Anderhub SJ, Faisal A, Linardopoulos S.

Oncotarget. 2016 Jul 18;9(28):19525-19542. doi: 10.18632/oncotarget.10657. eCollection 2018 Apr 13.


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.

J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7.


Aurora Kinase Inhibitors: Current Status and Outlook.

Bavetsias V, Linardopoulos S.

Front Oncol. 2015 Dec 21;5:278. doi: 10.3389/fonc.2015.00278. eCollection 2015. Review.


7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent.

Bavetsias V, Pérez-Fuertes Y, McIntyre PJ, Atrash B, Kosmopoulou M, O'Fee L, Burke R, Sun C, Faisal A, Bush K, Avery S, Henley A, Raynaud FI, Linardopoulos S, Bayliss R, Blagg J.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4203-9. doi: 10.1016/j.bmcl.2015.08.003. Epub 2015 Aug 6.


Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance.

Gurden MD, Westwood IM, Faisal A, Naud S, Cheung KM, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Van Montfort RL, Linardopoulos S.

Cancer Res. 2015 Aug 15;75(16):3340-54. doi: 10.1158/0008-5472.CAN-14-3272. Epub 2015 Jul 22.


Aurora kinase inhibition: a new light in the sky?

Linardopoulos S, Blagg J.

J Med Chem. 2015 Jul 9;58(13):5186-8. doi: 10.1021/acs.jmedchem.5b00918. Epub 2015 Jun 25.


New therapeutic perspectives in CCDC6 deficient lung cancer cells.

Morra F, Luise C, Visconti R, Staibano S, Merolla F, Ilardi G, Guggino G, Paladino S, Sarnataro D, Franco R, Monaco R, Zitomarino F, Pacelli R, Monaco G, Rocco G, Cerrato A, Linardopoulos S, Muller MT, Celetti A.

Int J Cancer. 2015 May 1;136(9):2146-57. doi: 10.1002/ijc.29263. Epub 2014 Oct 24.


Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines.

Cheeseman MD, Faisal A, Rayter S, Barbeau OR, Kalusa A, Westlake M, Burke R, Swan M, van Montfort R, Linardopoulos S, Jones K.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3469-74. doi: 10.1016/j.bmcl.2014.05.067. Epub 2014 May 29.


APC/C is an essential regulator of centrosome clustering.

Drosopoulos K, Tang C, Chao WC, Linardopoulos S.

Nat Commun. 2014 Apr 22;5:3686. doi: 10.1038/ncomms4686.


Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).

Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, Valenti M, de Haven Brandon A, Henley A, Baker R, McAndrew C, Matijssen B, Burke R, Hoelder S, Eccles SA, Raynaud FI, Linardopoulos S, van Montfort RL, Blagg J.

J Med Chem. 2013 Dec 27;56(24):10045-65. doi: 10.1021/jm401395s. Epub 2013 Dec 2.


Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.

Bavetsias V, Faisal A, Crumpler S, Brown N, Kosmopoulou M, Joshi A, Atrash B, Pérez-Fuertes Y, Schmitt JA, Boxall KJ, Burke R, Sun C, Avery S, Bush K, Henley A, Raynaud FI, Workman P, Bayliss R, Linardopoulos S, Blagg J.

J Med Chem. 2013 Nov 27;56(22):9122-35. doi: 10.1021/jm401115g. Epub 2013 Nov 6.


The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

Couty S, Westwood IM, Kalusa A, Cano C, Travers J, Boxall K, Chow CL, Burns S, Schmitt J, Pickard L, Barillari C, McAndrew PC, Clarke PA, Linardopoulos S, Griffin RJ, Aherne GW, Raynaud FI, Workman P, Jones K, van Montfort RL.

Oncotarget. 2013 Oct;4(10):1647-61.


Aurora A kinase regulates mammary epithelial cell fate by determining mitotic spindle orientation in a Notch-dependent manner.

Regan JL, Sourisseau T, Soady K, Kendrick H, McCarthy A, Tang C, Brennan K, Linardopoulos S, White DE, Smalley MJ.

Cell Rep. 2013 Jul 11;4(1):110-23. doi: 10.1016/j.celrep.2013.05.044. Epub 2013 Jun 27.


Tumour selective targeting of cell cycle kinases for cancer treatment.

Aarts M, Linardopoulos S, Turner NC.

Curr Opin Pharmacol. 2013 Aug;13(4):529-35. doi: 10.1016/j.coph.2013.03.012. Epub 2013 Apr 15. Review.


Integration of RNAi and small molecule screens to identify targets for drug development.

Drosopoulos K, Linardopoulos S.

Methods Mol Biol. 2013;986:97-104. doi: 10.1007/978-1-62703-311-4_7.


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.

J Med Chem. 2012 Oct 25;55(20):8721-34. doi: 10.1021/jm300952s. Epub 2012 Oct 8.


Sensitization of (colon) cancer cells to death receptor related therapies: a report from the FP6-ONCODEATH research consortium.

Pintzas A, Zhivotovsky B, Workman P, Clarke PA, Linardopoulos S, Martinou JC, Lacal JC, Robine S, Nasioulas G, Andera L.

Cancer Biol Ther. 2012 May;13(7):458-66. doi: 10.4161/cbt.19600. Epub 2012 May 1. Review.


Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S.

Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52. Epub 2012 Feb 22.


Functional viability profiles of breast cancer.

Brough R, Frankum JR, Sims D, Mackay A, Mendes-Pereira AM, Bajrami I, Costa-Cabral S, Rafiq R, Ahmad AS, Cerone MA, Natrajan R, Sharpe R, Shiu KK, Wetterskog D, Dedes KJ, Lambros MB, Rawjee T, Linardopoulos S, Reis-Filho JS, Turner NC, Lord CJ, Ashworth A.

Cancer Discov. 2011 Aug;1(3):260-73. doi: 10.1158/2159-8290.CD-11-0107. Epub 2011 Aug 2.


The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo.

Faisal A, Vaughan L, Bavetsias V, Sun C, Atrash B, Avery S, Jamin Y, Robinson SP, Workman P, Blagg J, Raynaud FI, Eccles SA, Chesler L, Linardopoulos S.

Mol Cancer Ther. 2011 Nov;10(11):2115-23. doi: 10.1158/1535-7163.MCT-11-0333. Epub 2011 Sep 1.


Adaptation of the plasma inhibitory activity assay to detect Aurora, ABL and FLT3 kinase inhibition by AT9283 in pediatric leukemia.

Podesta JE, Sugar R, Squires M, Linardopoulos S, Pearson AD, Moore AS.

Leuk Res. 2011 Sep;35(9):1273-5. doi: 10.1016/j.leukres.2011.05.022. Epub 2011 Jun 12.


Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21.


Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E.

J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j.


PPM1D gene amplification and overexpression in breast cancer: a qRT-PCR and chromogenic in situ hybridization study.

Lambros MB, Natrajan R, Geyer FC, Lopez-Garcia MA, Dedes KJ, Savage K, Lacroix-Triki M, Jones RL, Lord CJ, Linardopoulos S, Ashworth A, Reis-Filho JS.

Mod Pathol. 2010 Oct;23(10):1334-45. doi: 10.1038/modpathol.2010.121. Epub 2010 Jun 11.


Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition.

Sourisseau T, Maniotis D, McCarthy A, Tang C, Lord CJ, Ashworth A, Linardopoulos S.

EMBO Mol Med. 2010 Apr;2(4):130-42. doi: 10.1002/emmm.201000068.


Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias.

Moore AS, Blagg J, Linardopoulos S, Pearson AD.

Leukemia. 2010 Apr;24(4):671-8. doi: 10.1038/leu.2010.15. Epub 2010 Feb 11. Review.


A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2.

Bibby RA, Tang C, Faisal A, Drosopoulos K, Lubbe S, Houlston R, Bayliss R, Linardopoulos S.

J Biol Chem. 2009 Nov 27;284(48):33177-84. doi: 10.1074/jbc.M109.032722. Epub 2009 Oct 2.


Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity.

Chan F, Sun C, Perumal M, Nguyen QD, Bavetsias V, McDonald E, Martins V, Wilsher NE, Raynaud FI, Valenti M, Eccles S, Te Poele R, Workman P, Aboagye EO, Linardopoulos S.

Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57.


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.


Aurora-A kinase regulates NF-kappaB activity: lessons from combination studies.

Linardopoulos S.

J BUON. 2007 Sep;12 Suppl 1:S67-70.


Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.

Bavetsias V, Sun C, Bouloc N, Reynisson J, Workman P, Linardopoulos S, McDonald E.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6567-71. Epub 2007 Oct 22.


A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D.

Rayter S, Elliott R, Travers J, Rowlands MG, Richardson TB, Boxall K, Jones K, Linardopoulos S, Workman P, Aherne W, Lord CJ, Ashworth A.

Oncogene. 2008 Feb 14;27(8):1036-44. Epub 2007 Aug 13.


Aurora-A regulation of nuclear factor-kappaB signaling by phosphorylation of IkappaBalpha.

Briassouli P, Chan F, Savage K, Reis-Filho JS, Linardopoulos S.

Cancer Res. 2007 Feb 15;67(4):1689-95.


Aurora kinase inhibition downregulates NF-kappaB and sensitises tumour cells to chemotherapeutic agents.

Sun C, Chan F, Briassouli P, Linardopoulos S.

Biochem Biophys Res Commun. 2007 Jan 5;352(1):220-5. Epub 2006 Nov 10.


The N-terminal domain of the Aurora-A Phe-31 variant encodes an E3 ubiquitin ligase and mediates ubiquitination of IkappaBalpha.

Briassouli P, Chan F, Linardopoulos S.

Hum Mol Genet. 2006 Nov 15;15(22):3343-50. Epub 2006 Oct 23.


Aurora B expression directly correlates with prostate cancer malignancy and influence prostate cell proliferation.

Chieffi P, Cozzolino L, Kisslinger A, Libertini S, Staibano S, Mansueto G, De Rosa G, Villacci A, Vitale M, Linardopoulos S, Portella G, Tramontano D.

Prostate. 2006 Feb 15;66(3):326-33.


Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation.

Sorrentino R, Libertini S, Pallante PL, Troncone G, Palombini L, Bavetsias V, Spalletti-Cernia D, Laccetti P, Linardopoulos S, Chieffi P, Fusco A, Portella G.

J Clin Endocrinol Metab. 2005 Feb;90(2):928-35. Epub 2004 Nov 23.


High-throughput screening assay for identification of small molecule inhibitors of Aurora2/STK15 kinase.

Sun C, Newbatt Y, Douglas L, Workman P, Aherne W, Linardopoulos S.

J Biomol Screen. 2004 Aug;9(5):391-7.


Aurora B expression in normal testis and seminomas.

Chieffi P, Troncone G, Caleo A, Libertini S, Linardopoulos S, Tramontano D, Portella G.

J Endocrinol. 2004 May;181(2):263-70.


Identification of Stk6/STK15 as a candidate low-penetrance tumor-susceptibility gene in mouse and human.

Ewart-Toland A, Briassouli P, de Koning JP, Mao JH, Yuan J, Chan F, MacCarthy-Morrogh L, Ponder BA, Nagase H, Burn J, Ball S, Almeida M, Linardopoulos S, Balmain A.

Nat Genet. 2003 Aug;34(4):403-12.


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