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Journal Articles

McGrath, S., Tortorici, M., Drouin, L., Solanki, S., Vidler, L., Westwood, I., Gimeson, P., Van Montfort, R. & Hoelder, S. (2017). Structure-Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1. Chemistry - a european journal, Vol.23(40), pp. 9577-9584.  show abstract

Jones, A.M., Westwood, I.M., Osborne, J.D., Matthews, T.P., Cheeseman, M.D., Rowlands, M.G., Jeganathan, F., Burke, R., Lee, D., Kadi, N., et al. (2016). A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms. Scientific reports, Vol.6(1), p. 34701.  show abstract

Bavetsias, V., Lanigan, R.M., Ruda, G.F., Atrash, B., McLaughlin, M.G., Tumber, A., Mok, N.Y., Le Bihan, Y.-., Dempster, S., Boxall, K.J., et al. (2016). 8-Substituted Pyrido[3,4- d ]pyrimidin-4(3 H )-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Journal of medicinal chemistry, Vol.59(4), pp. 1388-1409.  show abstract  full text

Cheeseman, M.D., Westwood, I.M., Barbeau, O., Rowlands, M., Dobson, S., Jones, A.M., Jeganathan, F., Burke, R., Kadi, N., Workman, P., et al. (2016). Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70. Journal of medicinal chemistry, Vol.59(10), pp. 4625-4636.  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., et al. (2016). Rapid Discovery of Pyrido[3,4- d ]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. Journal of medicinal chemistry, Vol.59(8), pp. 3671-3688.  show abstract

Gurden, M.D., Westwood, I.M., Faisal, A., Naud, S., Cheung, K.-., McAndrew, C., Wood, A., Schmitt, J., Boxall, K., Mak, G., et al. (2015). Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer research, Vol.75(16), pp. 3340-3354.  show abstract

Tatton-Brown, K., Seal, S., Ruark, E., Harmer, J., Ramsay, E., del Vecchio Duarte, S., Zachariou, A., Hanks, S., O'Brien, E., Aksglaede, L., et al. (2014). Mutations in the DNA methyltransferase gene DNMT3A cause an overgrowth syndrome with intellectual disability. Nature genetics, Vol.46(4), pp. 385-388.  show abstract  full text

Silva-Santisteban, M.C., Westwood, I.M., Boxall, K., Brown, N., Peacock, S., McAndrew, C., Barrie, E., Richards, M., Mirza, A., Oliver, A.W., et al. (2013). Fragment-Based Screening Maps Inhibitor Interactions in the ATP-Binding Site of Checkpoint Kinase 2. Plos one, Vol.8(6), pp. e65689-e65689.  show abstract  full text

Couty, S., Westwood, I.M., Kalusa, A., Cano, C., Travers, J., Boxall, K., Chow, C.L., Burns, S., Schmitt, J., Pickard, L., et al. (2013). The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design. Oncotarget, Vol.4(10), pp. 1647-1661.  show abstract  full text

Naud, S., Westwood, I.M., Faisal, A., Sheldrake, P., Bavetsias, V., Atrash, B., Cheung, K.-., Liu, M., Hayes, A., Schmitt, J., et al. (2013). Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1). Journal of medicinal chemistry, Vol.56(24), pp. 10045-10065.  show abstract  full text

Matijssen, C., Silva-Santisteban, M.C., Westwood, I.M., Siddique, S., Choi, V., Sheldrake, P., van Montfort, R.L. & Blagg, J. (2012). Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography. Bioorganic & medicinal chemistry, Vol.20(22), pp. 6630-6639.  show abstract

Powers, M.V., Jones, K., Barillari, C., Westwood, I., van Montfort, R.L. & Workman, P. (2010). Targeting HSP70 The second potentially druggable heat shock protein and molecular chaperone?. Cell cycle, Vol.9(8), pp. 1542-1550.  show abstract

van Montfort, R.L. & Workman, P. (2009). Structure-based design of molecular cancer therapeutics. Trends biotechnol, Vol.27(5), pp. 315-328.  show abstract

Howard, N., Abell, C., Blakemore, W., Chessari, G., Congreve, M., Howard, S., Jhoti, H., Murray, C.W., Seavers, L.C. & van Montfort, R.L., et al. (2006). Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors. J med chem, Vol.49(4), pp. 1346-1355.  show abstract

van Montfort, R.L., Congreve, M., Tisi, D., Carr, R. & Jhoti, H. (2003). Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B. Nature, Vol.423(6941), pp. 773-777.  show abstract

van Montfort, R.L., Basha, E., Friedrich, K.L., Slingsby, C. & Vierling, E. (2001). Crystal structure and assembly of a eukaryotic small heat shock protein. Nat struct biol, Vol.8(12), pp. 1025-1030.  show abstract


Conferences

Gurden, M.D., Westwood, I., Faisal, A., Naud, S., Cheung, J., McAndrew, C., Wood, A., Schmitt, J., Boxall, K., Mak, G., et al. (2015). Abstract 5450: Naturally occurring mutations in the MPS1 gene predispose cells to kinase inhibitor drug-resistance, Cancer Research, Vol.75(15 Supplement), p.5450.

Innocenti, P., Woodward, H., Cheung, K.J., Naud, S., Solanki, S., Westwood, I.M., Faisal, A., Hayes, A., Schmitt, J., Baker, R., et al. (2015). Abstract 3642: Structure enabled design of inhibitors of the mitotic kinase MPS1, Cancer Research, Vol.75(15 Supplement), p.3642.

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