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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. Biochem j, 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. 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

van Montfort, R.L. Workman, P. (2017). Structure-based drug design: aiming for a perfect fit. Essays biochem, 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, Vol.23 (40), pp. 9577-9584.  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. Br j cancer, Vol.116 (9), pp. 1166-1176.  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. Liu, M. Richards, M. McAndrew, C. Yahya, N. Dobson, S.E. Jones, K. Workman, P. Collins, I. van Montfort, R.L. (2016). A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms. Sci rep, Vol.6, 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. Jeganathan, F. Hatch, S.B. Savitsky, P. Velupillai, S. Krojer, T. England, K.S. Sejberg, J. Thai, C. Donovan, A. Pal, A. Scozzafava, G. Bennett, J.M. Kawamura, A. Johansson, C. Szykowska, A. Gileadi, C. Burgess-Brown, N.A. von Delft, F. Oppermann, U. Walters, Z. Shipley, J. Raynaud, F.I. Westaway, S.M. Prinjha, R.K. Fedorov, O. Burke, R. Schofield, C.J. Westwood, I.M. Bountra, C. Müller, S. van Montfort, R.L. Brennan, P.E. Blagg, J. (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. J med chem, Vol.59 (4), pp. 1388-1409.  show abstract

Cheeseman, M.D. Westwood, I.M. Barbeau, O. Rowlands, M. Dobson, S. Jones, A.M. Jeganathan, F. Burke, R. Kadi, N. Workman, P. Collins, I. van Montfort, R.L. Jones, K. (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. 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

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 res, 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. Baralle, D. Dabir, T. Gener, B. Goudie, D. Homfray, T. Kumar, A. Pilz, D.T. Selicorni, A. Temple, I.K. Van Maldergem, L. Yachelevich, N. Childhood Overgrowth Consortium, van Montfort, R. Rahman, N. (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. 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

Silva-Santisteban, M.C. Westwood, I.M. Boxall, K. Brown, N. Peacock, S. McAndrew, C. Barrie, E. Richards, M. Mirza, A. Oliver, A.W. Burke, R. Hoelder, S. Jones, K. Aherne, G.W. Blagg, J. Collins, I. Garrett, M.D. van Montfort, R.L. (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. 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.

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. (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.