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Wagner, S., Vlachogiannis, G., De Haven Brandon, A., Valenti, M., Box, G., Jenkins, L., Mancusi, C., Self, A., Manodoro, F., Assiotis, I., et al. (2019). Suppression of interferon gene expression overcomes resistance to MEK inhibition in KRAS-mutant colorectal cancer. Oncogene, Vol.38 (10), pp. 1717-1733.  show abstract

Whittaker, S.R., Barlow, C., Martin, M.P., Mancusi, C., Wagner, S., Self, A., Barrie, E., Te Poele, R., Sharp, S., Brown, N., et al. (2018). Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor. Mol oncol, Vol.12 (3), pp. 287-304.  show abstract

Whittaker, S.R., Mallinger, A., Workman, P. & Clarke, P.A. (2017). Inhibitors of cyclin-dependent kinases as cancer therapeutics. Pharmacol ther, Vol.173, pp. 83-105.  show abstract

Whittaker, S.R., Cowley, G.S., Wagner, S., Luo, F., Root, D.E. & Garraway, L.A. (2015). Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors. Mol cancer ther, Vol.14 (12), pp. 2700-2711.  show abstract

Girotti, M.R., Lopes, F., Preece, N., Niculescu-Duvaz, D., Zambon, A., Davies, L., Whittaker, S., Saturno, G., Viros, A., Pedersen, M., et al. (2015). Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer cell, Vol.27 (1), pp. 85-96.  show abstract

Van Allen, E.M., Wagle, N., Sucker, A., Treacy, D.J., Johannessen, C.M., Goetz, E.M., Place, C.S., Taylor-Weiner, A., Whittaker, S., Kryukov, G.V., et al. (2014). The Genetic Landscape of Clinical Resistance to RAF Inhibition in Metastatic Melanoma. Cancer discovery, Vol.4 (1), pp. 94-109.

Niculescu-Duvaz, D., Niculescu-Duvaz, I., Suijkerbuijk, B.M., Ménard, D., Zambon, A., Davies, L., Pons, J.-., Whittaker, S., Marais, R. & Springer, C.J., et al. (2013). Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents. Bioorg med chem, Vol.21 (5), pp. 1284-1304.  show abstract

Whittaker, S.R., Theurillat, J.-., Van Allen, E., Wagle, N., Hsiao, J., Cowley, G.S., Schadendorf, D., Root, D.E. & Garraway, L.A. (2013). A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer discov, Vol.3 (3), pp. 350-362.  show abstract

Whittaker, S.R., Luo, F., Hsiao, J., Cowley, G.S., Root, D.E. & Garraway, L.A. (2013). Probing synthetic lethal interactions with RAF inhibition in BRAF-mutant colorectal cancer. Molecular cancer therapeutics, Vol.12 (5).

Wilson, S.C., Atrash, B., Barlow, C., Eccles, S., Fischer, P.M., Hayes, A., Kelland, L., Jackson, W., Jarman, M., Mirza, A., et al. (2011). Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. Bioorg med chem, Vol.19 (22), pp. 6949-6965.  show abstract

Suijkerbuijk, B.M., Niculescu-Duvaz, I., Gaulon, C., Dijkstra, H.P., Niculescu-Duvaz, D., Ménard, D., Zambon, A., Nourry, A., Davies, L., Manne, H.A., et al. (2010). Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group. J med chem, Vol.53 (7), pp. 2741-2756.  show abstract

Whittaker, S., Kirk, R., Hayward, R., Zambon, A., Viros, A., Cantarino, N., Affolter, A., Nourry, A., Niculescu-Duvaz, D., Springer, C., et al. (2010). Gatekeeper mutations mediate resistance to BRAF-targeted therapies. Sci transl med, Vol.2 (35), p. 35ra41.  show abstract

Whittaker, S., Marais, R. & Zhu, A.X. (2010). The role of signaling pathways in the development and treatment of hepatocellular carcinoma. Oncogene, Vol.29 (36), pp. 4989-5005.  show abstract

Nourry, A., Zambon, A., Davies, L., Niculescu-Duvaz, I., Dijkstra, H.P., Ménard, D., Gaulon, C., Niculescu-Duvaz, D., Suijkerbuijk, B.M., Friedlos, F., et al. (2010). BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring. J med chem, Vol.53 (5), pp. 1964-1978.  show abstract

Zambon, A., Ménard, D., Suijkerbuijk, B.M., Niculescu-Duvaz, I., Whittaker, S., Niculescu-Duvaz, D., Nourry, A., Davies, L., Manne, H.A., Lopes, F., et al. (2010). Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors. J med chem, Vol.53 (15), pp. 5639-5655.  show abstract

Whittaker, S., Martin, M. & Marais, R. (2010). All roads lead to the ribosome. Cancer cell, Vol.18 (1), pp. 5-6.  show abstract

Niculescu-Duvaz, D., Niculescu-Duvaz, I., Suijkerbuijk, B.M., Ménard, D., Zambon, A., Nourry, A., Davies, L., Manne, H.A., Friedlos, F., Ogilvie, L., et al. (2010). Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds. Bioorg med chem, Vol.18 (18), pp. 6934-6952.  show abstract

Whittaker, S., Ménard, D., Kirk, R., Ogilvie, L., Hedley, D., Zambon, A., Lopes, F., Preece, N., Manne, H., Rana, S., et al. (2010). A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF. Cancer res, Vol.70 (20), pp. 8036-8044.  show abstract

Heidorn, S.J., Milagre, C., Whittaker, S., Nourry, A., Niculescu-Duvas, I., Dhomen, N., Hussain, J., Reis-Filho, J.S., Springer, C.J., Pritchard, C., et al. (2010). Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell, Vol.140 (2), pp. 209-221.  show abstract

Ménard, D., Niculescu-Duvaz, I., Dijkstra, H.P., Niculescu-Duvaz, D., Suijkerbuijk, B.M., Zambon, A., Nourry, A., Roman, E., Davies, L., Manne, H.A., et al. (2009). Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. J med chem, Vol.52 (13), pp. 3881-3891.  show abstract

Niculescu-Duvaz, D., Gaulon, C., Dijkstra, H.P., Niculescu-Duvaz, I., Zambon, A., Ménard, D., Suijkerbuijk, B.M., Nourry, A., Davies, L., Manne, H., et al. (2009). Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF). J med chem, Vol.52 (8), pp. 2255-2264.  show abstract

Niculescu-Duvaz, D., Gaulon, C., Dijkstra, H.P., Niculescu-Duvaz, I., Zambon, A., Menard, D., Suijkerbuijk, B.M., Nourry, A., Davies, L., Manne, H., et al. (2009). Pyridoimidazolones as Novel Potent Inhibitors of v-Raf Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) (vol 52, pg 2255, 2009). Journal of medicinal chemistry, Vol.52 (18), pp. 5770-5770.

Niculescu-Duvaz, I., Roman, E., Whittaker, S.R., Friedlos, F., Kirk, R., Scanlon, I.J., Davies, L.C., Niculescu-Duvaz, D., Marais, R. & Springer, C.J., et al. (2008). Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold. J med chem, Vol.51 (11), pp. 3261-3274.  show abstract

Ahmed, M., Barbachano, Y., Riddell, A.M., Whittaker, S., Newbold, K., Harrington, K., Marais, R. & Nutting, C.M. (2008). Preliminary results of an open labelled phase 2 study evaluating the safety and efficacy of sorafenib in metastatic advanced thyroid cancer. Journal of clinical oncology, Vol.26 (15).

Niculescu-Duvaz, D., Whittaker, S., Springer, C. & Marais, R. (2007). The EGF receptor Hokey-Cokey. Cancer cell, Vol.11 (3), pp. 209-211.  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

Newbatt, Y., Burns, S., Hayward, R., Whittaker, S., Kirk, R., Marshall, C., Springer, C., McDonald, E., Marais, R., Workman, P., et al. (2006). Identification of inhibitors of the kinase activity of oncogenic (V600E)BRAF in an enzyme cascade high-throughput screen. J biomol screen, Vol.11 (2), pp. 145-154.  show abstract

Niculescu-Duvaz, I., Roman, E., Whittaker, S.R., Friedlos, F., Kirk, R., Scanlon, I.J., Davies, L.C., Niculescu-Duvaz, D., Marais, R. & Springer, C.J., et al. (2006). Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold Generation of a nanomolar lead. J med chem, Vol.49 (1), pp. 407-416.  show abstract

Raynaud, F.I., Whittaker, S.R., Fischer, P.M., McClue, S., Walton, M.I., Barrie, S.E., Garrett, M.D., Rogers, P., Clarke, S.J., Kelland, L.R., et al. (2005). In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clin cancer res, Vol.11 (13), pp. 4875-4887.  show abstract

Whittaker, S.R., Walton, M.I., Garrett, M.D. & Workman, P. (2004). The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway. Cancer res, Vol.64 (1), pp. 262-272.  show abstract


Conferences

Girotti, M.R., Lopes, F., Preece, N., Niculescu-Duvaz, D., Zambon, A., Davies, L., Whittaker, S., Saturno, G., Viros, A., Pedersen, M., et al. (2014). Novel panRAF inhibitors active in melanomas that are resistant to BRAF-selective, or BRAF-selective/MEK inhibitor combinations, CANCER RESEARCH, Vol.74 (19).

Ahmed, M., Barbachano, Y., Riddell, A.M., Whittaker, S., Newbold, K., Harrington, K., Marais, R. & Nutting, C. (2008). AN OPEN LABELLED PHASE 2 STUDY EVALUATING THE SAFETY AND EFFICACY OF SORAFENIB IN METASTATIC ADVANCED THYROID CANCER, Presented at 33rd European-Society-for-Medical-Oncology Congress, Stockholm, SWEDEN. ANNALS OF ONCOLOGY, Vol.19, p.218.

Niculescu-Duvaz, I., Whittaker, S., Friedlos, F., Kirk, R., Scanlon, I.J., Davies, L., Niculescu-Duvaz, D., Roman, E., Marais, R. & Springer, C.J., et al. (2006). A pyrazyne scaffold for the generation of novel inhibitors of B-RAF, EJC SUPPL, Vol.4 (12), p.53.

Whittaker, S.R., Te Poele, R., Walton, M.I., Garrett, M.D. & Workman, P. (2002). Gene expression profiling of the cyclin-dependent kinase inhibitor CYC202 (R-Roscovitine), Presented at 14th EORTC/NCI/AACR Symposium on Molecular Targets and Cancer Therapeutics, FRANKFURT, GERMANY. EUROPEAN JOURNAL OF CANCER, Vol.38, p.S50.