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Journal Articles

Hudson, L. Mui, J. Vázquez, S. Carvalho, D.M. Williams, E. Jones, C. Bullock, A.N. Hoelder, S. (2018). Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept. J med chem, Vol.61 (16), pp. 7261-7272.  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

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.

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

Drouin, L. McGrath, S. Vidler, L.R. Chaikuad, A. Monteiro, O. Tallant, C. Philpott, M. Rogers, C. Fedorov, O. Liu, M. Akhtar, W. Hayes, A. Raynaud, F. Müller, S. Knapp, S. Hoelder, S. (2015). Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. J med chem, Vol.58 (5), pp. 2553-2559.  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 research, Vol.75 (16), pp. 3340-3354.

Innocenti, P. Woodward, H. O'Fee, L. Hoelder, S. (2015). Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines. Org biomol chem, Vol.13 (3), pp. 893-904.  show abstract

Innocenti, P. Cheung, K.-. Solanki, S. Mas-Droux, C. Rowan, F. Yeoh, S. Boxall, K. Westlake, M. Pickard, L. Hardy, T. Baxter, J.E. Aherne, G.W. Bayliss, R. Fry, A.M. Hoelder, S. (2012). Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. J med chem, Vol.55 (7), pp. 3228-3241.  show abstract

Vidler, L.R. Brown, N. Knapp, S. Hoelder, S. (2012). Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. J med chem, Vol.55 (17), pp. 7346-7359.  show abstract

Watts, E. Heidenreich, D. Tucker, E. Raab, M. Strebhardt, K. Chesler, L. Knapp, S. Bellenie, B. Hoelder, S. Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. Journal of medicinal chemistry, .