Main Menu

Publications Highlights View all by category

Types of Publications

Journal Articles

Moore, A.S. Faisal, A. Mak, G.W. Miraki-Moud, F. Bavetsias, V. Valenti, M. Box, G. Hallsworth, A. de Haven Brandon, A. Xavier, C.P. Stronge, R. Pearson, A.D. Blagg, J. Raynaud, F.I. Chopra, R. Eccles, S.A. Taussig, D.C. Linardopoulos, S. (2020). Quizartinib-resistant FLT3-ITD acute myeloid leukemia cells are sensitive to the FLT3-Aurora kinase inhibitor CCT241736. Blood advances, Vol.4 (7), pp. 1478-1491.  show abstract

Anderhub, S.J. Mak, G.W. Gurden, M.D. Faisal, A. Drosopoulos, K. Walsh, K. Woodward, H.L. Innocenti, P. Westwood, I.M. Naud, S. Hayes, A. Theofani, E. Filosto, S. Saville, H. Burke, R. van Montfort, R.L. Raynaud, F.I. Blagg, J. Hoelder, S. Eccles, S.A. Linardopoulos, S. (2019). High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers. Molecular cancer therapeutics, Vol.18 (10), pp. 1696-1707.

Wood, F.L. Shepherd, S. Hayes, A. Liu, M. Grira, K. Mok, Y. Atrash, B. Faisal, A. Bavetsias, V. Linardopoulos, S. Blagg, J. Raynaud, F.I. (2019). Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species. European journal of pharmaceutical sciences, Vol.139, pp. 104899-104899.

Gurden, M.D. Anderhub, S.J. Faisal, A. Linardopoulos, S. (2018). Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis. Oncotarget, Vol.9 (28), pp. 19525-19542.  show abstract  full text

Woodward, H.L. Innocenti, P. Cheung, K.-. Hayes, A. Roberts, J. Henley, A.T. Faisal, A. Mak, G.W. Box, G. Westwood, I.M. Cronin, N. Carter, M. Valenti, M. De Haven Brandon, A. O'Fee, L. Saville, H. Schmitt, J. Burke, R. Broccatelli, F. van Montfort, R.L. Raynaud, F.I. Eccles, S.A. Linardopoulos, S. Blagg, J. Hoelder, S. (2018). 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). J med chem, Vol.61 (18), pp. 8226-8240.  show abstract

Faisal, A. Mak, G.W. Gurden, M.D. Xavier, C.P. Anderhub, S.J. Innocenti, P. Westwood, I.M. Naud, S. Hayes, A. Box, G. Valenti, M.R. De Haven Brandon, A.K. O'Fee, L. Schmitt, J. Woodward, H.L. Burke, R. vanMontfort, R.L. Blagg, J. Raynaud, F.I. Eccles, S.A. Hoelder, S. Linardopoulos, S. (2017). Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy. British journal of cancer, Vol.116 (9), pp. 1166-1176.

Dolly, S.O. Gurden, M.D. Drosopoulos, K. Clarke, P. de Bono, J. Kaye, S. Workman, P. Linardopoulos, S. (2017). RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses. Br j cancer, Vol.117 (7), pp. 954-964.  show abstract

Gurden, M.D. Anderhub, S.J. Faisal, A. Linardopoulos, S. (2016). Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis. Oncotarget, .  show abstract

Innocenti, P. Woodward, H.L. Solanki, S. Naud, S. Westwood, I.M. Cronin, N. Hayes, A. Roberts, J. Henley, A.T. Baker, R. Faisal, A. Mak, G.W. Box, G. Valenti, M. De Haven Brandon, A. O'Fee, L. Saville, H. Schmitt, J. Matijssen, B. Burke, R. van Montfort, R.L. Raynaud, F.I. Eccles, S.A. Linardopoulos, S. Blagg, J. Hoelder, S. (2016). Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. J med chem, Vol.59 (8), pp. 3671-3688.  show abstract

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, M.T. Celetti, A. (2015). New therapeutic perspectives in CCDC6 deficient lung cancer cells. Int j cancer, Vol.136 (9), pp. 2146-2157.  show abstract

Linardopoulos, S. Blagg, J. (2015). Aurora Kinase Inhibition: A New Light in the Sky?. Journal of medicinal chemistry, Vol.58 (13), pp. 5186-5188.

Bavetsias, V. Pérez-Fuertes, Y. McIntyre, P.J. Atrash, B. Kosmopoulou, M. O’Fee, L. Burke, R. Sun, C. Faisal, A. Bush, K. Avery, S. Henley, A. Raynaud, F.I. Linardopoulos, S. Bayliss, R. Blagg, J. (2015). 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. Bioorganic & medicinal chemistry letters, Vol.25 (19), pp. 4203-4209.

Gurden, M.D. Westwood, I.M. Faisal, A. Naud, S. Cheung, K.-. McAndrew, C. Wood, A. Schmitt, J. Boxall, K. Mak, G. Workman, P. Burke, R. Hoelder, S. Blagg, J. Van Montfort, R.L. Linardopoulos, S. (2015). Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer research, Vol.75 (16), pp. 3340-3354.

Cheeseman, M.D. Faisal, A. Rayter, S. Barbeau, O.R. Kalusa, A. Westlake, M. Burke, R. Swan, M. van Montfort, R. Linardopoulos, S. Jones, K. (2014). Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines. Bioorg med chem lett, Vol.24 (15), pp. 3469-3474.  show abstract

Drosopoulos, K. Tang, C. Chao, W.C. Linardopoulos, S. (2014). APC/C is an essential regulator of centrosome clustering. Nat commun, Vol.5, p. 3686.  show abstract

Aarts, M. Linardopoulos, S. Turner, N.C. (2013). Tumour selective targeting of cell cycle kinases for cancer treatment. Curr opin pharmacol, Vol.13 (4), pp. 529-535.  show abstract

Regan, J.L. Sourisseau, T. Soady, K. Kendrick, H. McCarthy, A. Tang, C. Brennan, K. Linardopoulos, S. White, D.E. Smalley, M.J. (2013). Aurora A kinase regulates mammary epithelial cell fate by determining mitotic spindle orientation in a Notch-dependent manner. Cell rep, Vol.4 (1), pp. 110-123.  show abstract

Couty, S. Westwood, I.M. Kalusa, A. Cano, C. Travers, J. Boxall, K. Chow, C.L. Burns, S. Schmitt, J. Pickard, L. Barillari, C. McAndrew, P.C. Clarke, P.A. Linardopoulos, S. Griffin, R.J. Aherne, G.W. Raynaud, F.I. Workman, P. Jones, K. Van Montfort, R.L. (2013). The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design. Oncotarget, Vol.4, pp. 1-15.  show abstract

Bavetsias, V. Faisal, A. Crumpler, S. Brown, N. Kosmopoulou, M. Joshi, A. Atrash, B. Pérez-Fuertes, Y. Schmitt, J.A. Boxall, K.J. Burke, R. Sun, C. Avery, S. Bush, K. Henley, A. Raynaud, F.I. Workman, P. Bayliss, R. Linardopoulos, S. Blagg, J. (2013). Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells. J med chem, Vol.56 (22), pp. 9122-9135.  show abstract

Drosopoulos, K. Linardopoulos, S. (2013). Integration of RNAi and small molecule screens to identify targets for drug development. Methods mol biol, Vol.986, pp. 97-104.  show abstract

Naud, S. Westwood, I.M. Faisal, A. Sheldrake, P. Bavetsias, V. Atrash, B. Cheung, K.M. 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, S.A. Raynaud, F.I. Linardopoulos, S. Van Montfort, R.L. Blagg, J. (2013). Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of the mitotic kinase monopolar spindle 1 (MPS1). J med chem, Vol.56, pp. 10045-10065.

Pintzas, A. Zhivotovsky, B. Workman, P. Clarke, P.A. Linardopoulos, S. Martinou, J.-. Lacal, J.C. Robine, S. Nasioulas, G. Andera, L. (2012). Sensitization of (colon) cancer cells to death receptor related therapies: a report from the FP6-ONCODEATH research consortium. Cancer biol ther, Vol.13 (7), pp. 458-466.  show abstract

Moore, A.S. 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, A.D. Workman, P. Blagg, J. Raynaud, F.I. Eccles, S.A. Linardopoulos, S. (2012). Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. Leukemia, Vol.26 (7), pp. 1462-1470.  show abstract

Faisal, A. Naud, S. Schmitt, J. Westwood, I. Hayes, A. Gurden, M. Bavetsias, V. Berry, T. Mak, G. Innocenti, P. Cheung, J. Sheldrake, P. Atrash, B. Sun, C. Matijssen, B. Burke, R. Baker, R. McAndrew, C. Rowlands, M. Workman, P. Eccles, S.A. Hoelder, S. Raynaud, F.I. vanMontfort, R. Blagg, J. Linardopoulos, S. (2012). Abstract 1817: Characterisation of CCT251455, a novel, selective and highly potent Mps1 kinase inhibitor. Experimental and molecular therapeutics, .

Drosopoulos, K. Scott, C. Tang, C. Linardopoulos, S. (2012). Abstract 889: Integration of centrosome-associated and kinase-related screens to identify centrosome amplification-related synthetic lethal interactions. Experimental and molecular therapeutics, .

Bavetsias, V. Crumpler, S. Sun, C. Avery, S. Atrash, B. Faisal, A. Moore, A.S. Kosmopoulou, M. Brown, N. Sheldrake, P.W. Bush, K. Henley, A. Box, G. Valenti, M. de Haven Brandon, A. Raynaud, F.I. Workman, P. Eccles, S.A. Bayliss, R. Linardopoulos, S. Blagg, J. (2012). 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. J med chem, Vol.55 (20), pp. 8721-8734.  show abstract

Brough, R. Frankum, J.R. Sims, D. Mackay, A. Mendes-Pereira, A.M. Bajrami, I. Costa-Cabral, S. Rafiq, R. Ahmad, A.S. Cerone, M.A. Natrajan, R. Sharpe, R. Shiu, K.-. Wetterskog, D. Dedes, K.J. Lambros, M.B. Rawjee, T. Linardopoulos, S. Reis-Filho, J.S. Turner, N.C. Lord, C.J. Ashworth, A. (2011). Functional viability profiles of breast cancer. Cancer discov, Vol.1 (3), pp. 260-273.  show abstract

Podesta, J.E. Sugar, R. Squires, M. Linardopoulos, S. Pearson, A.D. Moore, A.S. (2011). Adaptation of the plasma inhibitory activity assay to detect Aurora, ABL and FLT3 kinase inhibition by AT9283 in pediatric leukemia. Leuk res, Vol.35 (9), pp. 1273-1275.  show abstract

Faisal, A. Vaughan, L. Bavetsias, V. Sun, C. Atrash, B. Avery, S. Jamin, Y. Robinson, S.P. Workman, P. Blagg, J. Raynaud, F.I. Eccles, S.A. Chesler, L. Linardopoulos, S. (2011). The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol cancer ther, Vol.10 (11), pp. 2115-2123.  show abstract

Moore, A.S. Faisal, A. Bavetsias, V. Sun, C. Atrash, B. Valenti, M. de Haven Brandon, A. Avery, S. de Castro, D.G. Raynaud, F.I. Workman, P. Pearson, A.D. Blagg, J. Eccles, S.A. Linardopoulos, S. (2011). Abstract 3554: CCT137690, a dual inhibitor of Aurora and FLT3 kinases, sensitizes FLT3-ITD positive acute myeloid leukemia and overcomes resistance to selective FLT3-inhibition. Experimental and molecular therapeutics, .

Moore, A. Faisal, A. Bavetsias, V. Sun, C. Atrash, B. Valenti, M. Brandon, A. Avery, S. de Castro, D.G. Pearson, A.D. Workman, P. Blagg, J. Raynaud, R.I. Eccles, S.A. Linardopoulos, S. (2011). The dual Aurora-FLT3 inhibitor CCT137690 overcomes resistance to selective FLT3 inhibition in acute myeloid leukemia. Clin can res, .

Moore, A.S. Blagg, J. Linardopoulos, S. Pearson, A.D. (2010). Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias. Leukemia, Vol.24 (4), pp. 671-8.

Sourisseau, T. Maniotis, D. McCarthy, A. Tang, C. Lord, C.J. Ashworth, A. Linardopoulos, S. (2010). Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition. Embo mol med, Vol.2 (4), pp. 130-142.  show abstract

Lambros, M.B. Natrajan, R. Geyer, F.C. Lopez-Garcia, M.A. Dedes, K.J. Savage, K. Lacroix-Triki, M. Jones, R.L. Lord, C.J. Linardopoulos, S. Ashworth, A. Reis-Filho, J.S. (2010). PPM1D gene amplification and overexpression in breast cancer: a qRT-PCR and chromogenic in situ hybridization study. Mod pathol, Vol.23 (10), pp. 1334-1345.  show abstract

Bouloc, N. Large, J.M. Kosmopoulou, M. Sun, C. Faisal, A. Matteucci, M. Reynisson, J. Brown, N. Atrash, B. Blagg, J. McDonald, E. Linardopoulos, S. Bayliss, R. Bavetsias, V. (2010). Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells. Bioorg med chem lett, Vol.20 (20), pp. 5988-5993.  show abstract

Bavetsias, V. Large, J.M. Sun, C. Bouloc, N. Kosmopoulou, M. Matteucci, M. Wilsher, N.E. Martins, V. Reynisson, J. Atrash, B. Faisal, A. Urban, F. Valenti, M. de Haven Brandon, A. Box, G. Raynaud, F.I. Workman, P. Eccles, S.A. Bayliss, R. Blagg, J. Linardopoulos, S. McDonald, E. (2010). Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J med chem, Vol.53 (14), pp. 5213-5228.  show abstract

Bibby, R.A. Tang, C. Faisal, A. Drosopoulos, K. Lubbe, S. Houlston, R. Bayliss, R. Linardopoulos, S. (2009). A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2. J biol chem, Vol.284 (48), pp. 33177-33184.  show abstract

Rayter, S. Elliott, R. Travers, J. Rowlands, M.G. Richardson, T.B. Boxall, K. Jones, K. Linardopoulos, S. Workman, P. Aherne, W. Lord, C.J. Ashworth, A. (2008). A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D. Oncogene, Vol.27 (8), pp. 1036-1044.  show abstract

Bavetsias, V. Sun, C. Bouloc, N. Reynisson, J. Workman, P. Linardopoulos, S. McDonald, E. (2007). Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases. Bioorg med chem lett, Vol.17 (23), pp. 6567-6571.  show abstract

Sun, C. Chan, F. Briassouli, P. Linardopoulos, S. (2007). Aurora kinase inhibition downregulates NF-kappaB and sensitises tumour cells to chemotherapeutic agents. Biochem biophys res commun, Vol.352 (1), pp. 220-225.  show abstract

Linardopoulos, S. (2007). Aurora-A kinase regulates NF-kappaB activity: lessons from combination studies. J buon, Vol.12 Suppl 1, pp. S67-S70.  show abstract

Chan, F. Sun, C. Perumal, M. Nguyen, Q.-. Bavetsias, V. McDonald, E. Martins, V. Wilsher, N.E. Raynaud, F.I. Valenti, M. Eccles, S. Te Poele, R. Workman, P. Aboagye, E.O. Linardopoulos, S. (2007). Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol cancer ther, Vol.6 (12 Pt 1), pp. 3147-3157.  show abstract

Briassouli, P. Chan, F. Savage, K. Reis-Filho, J.S. Linardopoulos, S. (2007). Aurora-A regulation of nuclear factor-kappaB signaling by phosphorylation of IkappaBalpha. Cancer res, Vol.67 (4), pp. 1689-1695.  show abstract

Whittaker, S.R. Te Poele, R.H. Chan, F. Linardopoulos, S. Walton, M.I. Garrett, M.D. Workman, P. (2007). The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis. Cell cycle, Vol.6 (24), pp. 3114-3131.  show abstract

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. (2006). Aurora B expression directly correlates with prostate cancer malignancy and influence prostate cell proliferation. Prostate, Vol.66 (3), pp. 326-333.  show abstract

Briassouli, P. Chan, F. Linardopoulos, S. (2006). The N-terminal domain of the Aurora-A Phe-31 variant encodes an E3 ubiquitin ligase and mediates ubiquitination of IkappaBalpha. Hum mol genet, Vol.15 (22), pp. 3343-3350.  show abstract

Sorrentino, R. Libertini, S. Pallante, P.L. Troncone, G. Palombini, L. Bavetsias, V. Spalletti-Cernia, D. Laccetti, P. Linardopoulos, S. Chieffi, P. Fusco, A. Portella, G. (2005). Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation. J clin endocrinol metab, Vol.90 (2), pp. 928-935.  show abstract

Chieffi, P. Troncone, G. Caleo, A. Libertini, S. Linardopoulos, S. Tramontano, D. Portella, G. (2004). Aurora B expression in normal testis and seminomas. J endocrinol, Vol.181 (2), pp. 263-270.  show abstract

Sun, C. Newbatt, Y. Douglas, L. Workman, P. Aherne, W. Linardopoulos, S. (2004). High-throughput screening assay for identification of small molecule inhibitors of Aurora2/STK15 kinase. J biomol screen, Vol.9 (5), pp. 391-397.  show abstract

Ewart-Toland, A. Briassouli, P. de Koning, J.P. Mao, J.-. Yuan, J. Chan, F. MacCarthy-Morrogh, L. Ponder, B.A. Nagase, H. Burn, J. Ball, S. Almeida, M. Linardopoulos, S. Balmain, A. (2003). Identification of Stk6/STK15 as a candidate low-penetrance tumor-susceptibility gene in mouse and human. Nat genet, Vol.34 (4), pp. 403-412.  show abstract

Linardopoulos, S. Silva, S. Klein, G. Balmain, A. (2000). Allele-specific loss or imbalance of chromosomes 9, 15, and 16 in B-cell tumors from interspecific F1 hybrid mice carrying Emu-c-myc or N-myc transgenes. Int j cancer, Vol.88 (6), pp. 920-927.  show abstract

Zoumpourlis, V. Papassava, P. Linardopoulos, S. Gillespie, D. Balmain, A. Pintzas, A. (2000). High levels of phosphorylated c-Jun, Fra-1, Fra-2 and ATF-2 proteins correlate with malignant phenotypes in the multistage mouse skin carcinogenesis model. Oncogene, Vol.19 (35), pp. 4011-4021.  show abstract

Frame, S. Crombie, R. Liddell, J. Stuart, D. Linardopoulos, S. Nagase, H. Portella, G. Brown, K. Street, A. Akhurst, R. Balmain, A. (1998). Epithelial carcinogenesis in the mouse: correlating the genetics and the biology. Philos trans r soc lond b biol sci, Vol.353 (1370), pp. 839-845.  show abstract

Tsopanomichalou, M. Ergazaki, M. Linardopoulos, S. Kouroumalis, E. Spandidos, D.A. (1997). Detection of hepatitis C virus in sera and genotyping according to the 5' non-coding region. Oncology reports, Vol.4 (6), pp. 1171-4.

Karachristos, A. Linardopoulos, S. Ergazaki, M. Spandidos, D.A. (1995). Detection and analysis of hepatitis C virus by a combined RT-PCR method: variation in the 5' non-coding region of the viral genome. J med microbiol, Vol.42 (5), pp. 367-371.  show abstract

Linardopoulos, S. Street, A.J. Quelle, D.E. Parry, D. Peters, G. Sherr, C.J. Balmain, A. (1995). Deletion and altered regulation of p16INK4a and p15INK4b in undifferentiated mouse skin tumors. Cancer res, Vol.55 (22), pp. 5168-5172.  show abstract


Linardopoulos, S. Papadakis, E. Delakas, D. Theodosiou, V. Cranidis, A. Spandidos, D.A. (1993). Human lung and bladder carcinoma tumors as compared to their adjacent normal tissue have elevated AP-1 activity associated with the retinoblastoma gene promoter. Anticancer res, Vol.13 (1), pp. 257-262.  show abstract

Linardopoulos, S. Gonos, E.S. Spandidos, D.A. (1993). Abnormalities of retinoblastoma gene structure in human lung tumors. Cancer lett, Vol.71 (1-3), pp. 67-74.  show abstract

Spandidos, D.A. Karaiossifidi, H. Malliri, A. Linardopoulos, S. Vassilaros, S. Tsikkinis, A. Field, J.K. (1992). Expression of ras Rb1 and p53 proteins in human breast cancer. Anticancer res, Vol.12 (1), pp. 81-89.  show abstract


Linardopoulos, S. Corrigall, V. Panayi, G.S. (1992). Activation of HLA-DR and interleukin-6 gene transcription in resting T cells via the CD2 molecule: relevance to chronic immune-mediated inflammation. Scand j immunol, Vol.36 (3), pp. 469-477.  show abstract

Symonds, R.P. Habeshaw, T. Paul, J. Kerr, D.J. Darling, A. Burnett, R.A. Sotsiou, F. Linardopoulos, S. Spandidos, D.A. (1992). No correlation between ras, c-myc and c-jun proto-oncogene expression and prognosis in advanced carcinoma of cervix. Eur j cancer, Vol.28A (10), pp. 1615-1617.  show abstract

Arvanitis, D. Malliri, A. Antoniou, D. Linardopoulos, S. Field, J.K. Spandidos, D.A. (1991). Ras p21 expression in brain tumors: elevated expression in malignant astrocytomas and glioblastomas multiforme. In vivo, Vol.5 (4), pp. 317-321.  show abstract

Tosca, A. Linardopoulos, S. Malliri, A. Hatziolou, E. Nicolaidou, A. Spandidos, D.A. (1991). Implication of the ras and myc oncoproteins in the pathogenesis of mycosis fungoides. Anticancer res, Vol.11 (4), pp. 1433-1438.  show abstract

Linardopoulos, S. Malliri, A. Pintzas, A. Vassilaros, S. Tsikkinis, A. Spandidos, D.A. (1990). Elevated expression of AP-1 activity in human breast tumors as compared to normal adjacent tissue. Anticancer res, Vol.10 (6), pp. 1711-1713.  show abstract

Bavetsias, V. Linardopoulos, S. Aurora Kinase Inhibitors: Current Status and Outlook. Frontiers in oncology, Vol.5.

morris, J. koo, C. gianomini, C. reyes-corral, M. olmos, Y. tavares, I. marson, C. linardopoulos, S. tutt, A. Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells. Molecular cancer therapeutics, .

Bajrami, I. Marlow, R. van de Ven, M. Brough, R. Pemberton, H. Frankum, J. Song, F. Raquif, R. Konde, A. Krastev, D. Menon, M. Campbell, J. Gulati, A. Kumar, R. Pettitt, S. Gurden, M. Cardenosa, M. Chong, I. Gazinska, P. Wallberg, F. Sawyer, E. Martin, L. Dowsett, M. Linardopoulos, S. Natrajan, R. Ryan, C. Derksen, P. Jonkers, J. Tutt, A. Ashworth, A. Lord, C. E-cadherin/ROS1 inhibitor synthetic lethality in breast cancer. Cancer discovery, .

Nirmesh, P. Weekes, D. Drosopoulos, K. Gazinska, P. Noel, E. Rashid, M. Mirza, H. Quist, J. Brasó-Maristany, F. Sumi, M. Ferro, R. Pereira, A. Prince, C. Noor, F. Francesch-Domenech, E. Marlow, R. de Rinaldis, E. Grigoriadis, A. Linardopoulos, S. Marra, P. Tutt, A. Integrated genomics and functional validation identifies malignant cell specific dependencies in Triple Negative Breast Cancer. Nature communications, .

Book Chapters

Drosopoulos, K. Linardopoulos, S. (2019). Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development. Target Identification and Validation in Drug Discovery. (pp. 33-42). Springer New York, ISBN: 9781493991440.


Woodward, H.Innocenti, P.Cheung, K.-.Naud, S.Faisal, A.Mak, G.W.Hayes, A.O'Fee, L.Saville, H.Brandon, A.D.Roberts, J.Box, G.Valenti, M.Heneley, A.T.Walsh, K.Burke, R.Eccles, S.A.Raynaud, F.I.Montfort, R.L.Blagg, J.Linardopoulos, S.Hoelder, S. (2018). Abstract 1651: In vitro and in vivo profile of the preclinical candidate and MPS1 kinase inhibitor CCT289346, Presented at Proceedings: AACR Annual Meeting 2018; April 14-18, 2018; Chicago, IL, Cancer Chemistry, .

Woodward, H.L.Innocenti, P.Cheung, K.-.Naud, S.Hayes, A.Henley, A.T.Faisal, A.Mak, G.Box, G.Westwood, I.M.Carter, M.Valenti, M.Brandon, A.D.O’Fee, L.Saville, H.Burke, R.Montfort, R.V.Raynaud, F.Eccles, S.A.Linardopoulos, S.Blagg, J.Hoelder, S. (2017). Abstract 193: Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidate, Presented at Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC, Cancer Chemistry, .

Anderhub, S.J.Mak, G.W.Faisal, A.Walsh, K.Gurden, M.Day, L.Innocenti, P.Woodward, H.L.Westwood, I.M.Cheung, K.-.Naud, S.Hayes, A.Box, G.Brandon, A.D.Valenti, M.R.O’Fee, L.Saville, H.Burke, R.Montfort, R.L.Raynaud, F.I.Eccles, S.A.Blagg, J.Hoelder, S.Linardopoulos, S. (2017). Abstract 4036: Induction of detrimental aneuploidy in basal breast cancer cells treated by MPS1 inhibitors in combination with paclitaxel, Presented at Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC, Experimental and Molecular Therapeutics, .

Linardopoulos, S. (2016). MPS1 inhibition in breast cancer, INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE, Vol.38, p.S80.

Innocenti, P.Woodward, H.Cheung, K.J.Naud, S.Solanki, S.Westwood, I.M.Faisal, A.Hayes, A.Schmitt, J.Baker, R.Matijssen, B.Burke, R.Eccles, S.A.Raynaud, F.I.Linardopoulos, S.Blagg, J.van Montfort, R.L.Hoelder, S. (2015). Abstract 3642: Structure enabled design of inhibitors of the mitotic kinase MPS1, Presented at Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA, Cancer Chemistry, .

Gurden, M.D.Westwood, I.Faisal, A.Naud, S.Cheung, J.McAndrew, C.Wood, A.Schmitt, J.Boxall, K.Mak, G.Workman, P.Burke, R.Hoelder, S.Blagg, J.Van Montfort, R.Linardopoulos, S. (2015). Abstract 5450: Naturally occurring mutations in the MPS1 gene predispose cells to kinase inhibitor drug-resistance, Presented at Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA, Experimental and Molecular Therapeutics, .

Howes, J.Lu, B.-.Powers, M.Mitsopoulos, C.Al-Lazikani, B.Linardopoulos, S.Clarke, P.Workman, P. (2014). Abstract 2730: RNAi knockdown or chemical inhibition of anaphase-promoting complex components is synthetic lethal with HSP90 inhibition, Presented at Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA, Experimental and Molecular Therapeutics, .

Faisal, A.Innocenti, P.Westwood, I.Naud, S.Schmitt, J.Hayes, A.Mak, G.Gurden, M.Bavetsias, V.Cheung, J.Woodward, H.Sheldrake, P.Atrash, B.Burke, R.Baker, R.McAndrew, C.Rowlands, M.Valenti, M.Workman, P.Eccles, S.Raynaud, F.vanMontfort, R.Hoelder, S.Blagg, J.Linardopoulos, S. (2013). CCT271850, a novel, selective, highly potent and orally bioavailable Mps1 kinase inhibitor., CANCER RESEARCH, Vol.73 (8).

Moore, A.S.Faisal, A.Bavetsias, Castro, D.G.Sun, C.Atrash, B.Valenti, M.Brandon, A.D.Avery, S.Pearson, A.D.Workman, P.Blagg, J.Raynaud, F.I.Eccles, S.A.Linardopoulos, S. (2011). Resistance to Selective FLT3 Inhibitors, Driven by FLT3 Ligand and FLT3 Point Mutations, Can Be Overcome with the Dual FLT3-Aurora Kinase Inhibitor CCT241736, BLOOD, Vol.118 (21), p.1490.

Moore, A.S.Faisal, A.Bavetsias, V.Sun, C.B.Atrash, B.Valenti, M.Brandon, A.D.Avery, S.Raynaud, F.I.Workman, P.Pearson, A.D.Blagg, J.Eccles, S.A.Linardopoulos, S. (2010). Dual Inhibition of Aurora and FLT3 Kmases by CCT137690 A Novel Treatment Strategy Against FLT3 ITD Positive AML In Vitro and In Vivo, Presented at 52nd Annual Meeting of the American-Society-of-Hematology (ASH), Orlando, FL. BLOOD, Vol.116 (21), pp.1347-1348.

Moore, A.S.Faisal, A.Bavetsias, V.Sun, C.Atrash, B.Valenti, M.Brandon, A.D.Avery, S.Raynaud, F.I.Workman, P.Pearson, A.D.Blagg, J.Eccles, S.A.Linardopoulos, S. (2010). Dual Inhibition of Aurora and FLT3 Kinases by CCT137690: A Novel Treatment Strategy Against FLT3-ITD Positive AML In Vitro and In Vivo, Presented at 52nd Annual Meeting of the American-Society-of-Hematology (ASH), Orlando, FL. BLOOD, Vol.116 (21), pp.1347-2.

Podesta, J.E.Griffin, M.J.Sugar, R.Squires, M.S.Boddy, A.Linardopoulos, S.Pearson, A.D.Moore, A.S. (2010). Adaptation and Validation of the Plasma Inhibitory Activity (PIA) Assay to Detect Inhibition of Aurora, ABL and FLT3 kinases by AT9283 In Children and Adolescents with Leukaemia., Presented at 52nd Annual Meeting of the American-Society-of-Hematology (ASH), Orlando, FL. BLOOD, Vol.116 (21), pp.759-1.

Kosmopoulou, M.Faisal, A.Sun, C.Bavetsias, V.Atrash, B.Bouloc, N.Matteucci, M.Blagg, J.Linardopoulos, S.Bayliss, R. (2009). How to design aurora kinase A selective inhibitors, Acta Crystallographica Section A Foundations of Crystallography, Vol.65 (a1), pp.s148-s149.

Chan, F.Sun, C.Perumal, M.Nguyen, Q.-.Bavetsias, V.McDonald, E.Martins, V.Wilsher, N.Raynaud, F.Valenti, M.Eccles, S.TePoele, R.Workman, P.Aboagye, E.Linardopoulos, S. (2007). Characterization of CCT129202, a novel Aurora kinase inhibitor and in vivo quantification of biological activity, MOLECULAR CANCER THERAPEUTICS, Vol.6 (12), pp.3413S-1.

Sun, C.Chan, F.Linardopoulos, S. (2006). Aurora kinase inhibition downregulates NF-kappaB and sensitises human tumour cells to chemotherapeutic agents, CANCER RESEARCH, Vol.66 (8).

Linardopoulos, S.Sun,, (2005). High-throughput screening assay for identification of small molecule inhibitors of STK15/AuroraA kinase., Presented at AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics, Philadelphia, PA. CLINICAL CANCER RESEARCH, Vol.11 (24), p.9162S.

Linardopoulos, S.Briassouli, P.Balmain, A.Chan, F. (2003). A cancer susceptibility associated polymorphism, in Aurora2/STK15 alters binding to the UBE2N ubiquitin ligase and oncogenicity., Presented at AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, BOSTON, MASSACHUSETTS. CLINICAL CANCER RESEARCH, Vol.9 (16), pp.6218S-1.


Linardopoulos, S.Faisal,, Characterisation of CCT137690 a Novel Aurora Kinase Inhibitor that Inhibits N-MYC-Induced Neuroblastoma, Presented at Cell Cycle Regulators / Inhibitors and Cancer, Vienna. .

Patents and patent applications

Linardopoulos, S.Bavetsias, V.McDonald, E. Enzyme inhibitors.WO 2007/072017 A2.

Linardopoulos, S. Enzyme inhibitors. International Publication Number.WO 2009001021 A1.

Linardopoulos, S.S. Fused heterocyclic compounds and their use.WO 2014/030001 A1.

Linardopoulos, S.S. MPS1 Resistance patent.GB Application No: 1506248.2.

In this section

Professional activities Publications