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Journal Articles

Felisberto-Rodrigues, C., Thomas, J.C., McAndrew, C., Le Bihan, Y.-., Burke, R., Workman, P. & van Montfort, R.L. (2019). Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release. Biochemical journal, Vol.476 (18), pp. 2521-2543.  show abstract

Woodward, H.L., Innocenti, P., Cheung, K.-., Hayes, A., Roberts, J., Henley, A.T., Faisal, A., Mak, G.W., Box, G., Westwood, I.M., et al. (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., et al. (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.

van Montfort, R.L. & Workman, P. (2017). Structure-based drug design: aiming for a perfect fit. Essays in biochemistry, Vol.61 (5), pp. 431-437.  show abstract

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.

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).

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(3H)-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.

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. J med chem, 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. J med chem, 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.

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. Nat genet, Vol.46 (4), pp. 385-388.  show abstract

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, pp. 1-15.  show abstract

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), p. e65689.  show abstract

Naud, S., Westwood, I.M., Faisal, A., Sheldrake, P., Bavetsias, V., Atrash, B., Cheung, K.M., Liu, M., Hayes, A., Schmitt, J., et al. (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.

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. Bioorg med chem, 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).  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.


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, Presented at Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA, Experimental and Molecular Therapeutics, .

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, Presented at Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA, Cancer Chemistry, .