A

Aherne, W., Garrett, M., McDonald, T., Workman, P. (2002) Mechanism-based hign-throughput screening for novel anticancer drug discovery. In: AntiCancer Drug Development. Academic Press., New York USA, pp. 249-267. ISBN 978-012072651-6

B

Bavetsias, V., Clauss, R., Henderson, E. A. (2003) Antifolate chemistry: synthesis of 4-[N-[(6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino]benzoic acid via a (propargyl)Co2(CO)6+ complex. ORGANIC & BIOMOLECULAR CHEMISTRY, 1 (11). pp. 1943-1946. ISSN 1477-0520

Dodson, C. A., Kosmopoulou, M., Richards, M. W., Atrash, B., Bavetsias, V., Blagg, J., Bayliss, R. (2010) Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design. BIOCHEMICAL JOURNAL, 427 (Part 1). pp. 19-28. ISSN 0264-6021

Hayes, A., Mok, N. Y., Liu, M. J., Thai, C., Henley, A. T., Atrash, B., Lanigan, R. M., Sejberg, J., Le Bihan, Y. V., Bavetsias, V., Blagg, J., Raynaud, F. I. (2017) Pyrido 3,4-d pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution. XENOBIOTICA, 47 (9). pp. 771-777. ISSN 0049-8254

Bavetsias, V., Faisal, A., Crumpler, S., Brown, N., Kosmopoulou, M., Joshi, A., Atrash, B., Perez-Fuertes, Y., Schmitt, J. A., Boxall, K. J., Burke, R., Sun, C. B., Avery, S., Bush, K., Henley, A., Raynaud, F. I., Workman, P., Bayliss, R., Linardopoulos, S., Blagg, J. (2013) Aurora Isoform Selectivity: Design and Synthesis of Imidazo 4,5-b pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells. JOURNAL OF MEDICINAL CHEMISTRY, 56 (22). pp. 9122-9135. ISSN 0022-2623

Bavetsias, V., Lanigan, R. M., Ruda, G. F., Atrash, B., McLaughlin, M. G., Tumber, A., Mok, N. Y., Le Bihan, Y. V., 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., Muller, S., van Montfort, R. L. M., 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. JOURNAL OF MEDICINAL CHEMISTRY, 59 (4). pp. 1388-1409. ISSN 0022-2623

Fearon, D., Westwood, I. M., van Montfort, R. L. M., Bayliss, R., Jones, K., Bavetsias, V. (2018) Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition. BIOORGANIC & MEDICINAL CHEMISTRY, 26 (11). pp. 3021-3029. ISSN 0968-0896

Bavetsias, V,, Henderson, E. A., McDonald, E. (2004) 2-pivalamido-3H-pyrimidin-4-one derivatives: convenient pivalamide hydrolysis using Fe(NO3)(3) in MeOH. TETRAHEDRON LETTERS, 45 (29). pp. 5643-5644. ISSN 0040-4039

Quevedo, C. E., Bavetsias, V., McDonald, E. (2009) Microwave-assisted synthesis of 2-aminonicotinic acids by reacting 2-chloronicotinic acid with amines. TETRAHEDRON LETTERS, 50 (21). pp. 2481-2483. ISSN 0040-4039

Bavetsias, V., Large, J. M., Sun, C., Bouloc, N., Kosmopoulou, M., Matteucci, M., Wilsher, N. E., Martins, V., Reynisson, J., Atrash, B., Faisal, A., Urban, F., Valenti, M., de Haven Brandon, A., Box, G., Raynaud, F. I., Workman, P., Eccles, S. A., Bayliss, R., Blagg, J., Linardopoulos, S., McDonald, E. (2010) Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidates. JOURNAL OF MEDICINAL CHEMISTRY, 53 (14). pp. 5213-5228. ISSN 0022-2623

Oberoi, J., Richards, M. W., Crumpler, S., Brown, N., Blagg, J., Bayliss, R. (2010) Structural Basis of Poly(ADP-ribose) Recognition by the Multizinc Binding Domain of Checkpoint with Forkhead-associated and RING Domains (CHFR). JOURNAL OF BIOLOGICAL CHEMISTRY, 285 (50). pp. 39348-39358. ISSN 0021-9258

Rodgers, U. R., Lanyon-Hogg, T., Masumoto, N., Ritzefeld, M., Burke, R., Blagg, J., Magee, A. I., Tate, E. W. (2016) Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. ACS CHEMICAL BIOLOGY, 11 (12). pp. 3256-3262. ISSN 1554-8929

Kaserer, T., Blagg, J. (2018) Combining Mutational Signatures, Clonal Fitness, and Drug Affinity to Define Drug-Specific Resistance Mutations in Cancer. CELL CHEMICAL BIOLOGY, 25 (11). pp. 1359-1371. ISSN 2451-9448

Meyers, J., Brown, N., Blagg, J. (2016) Mapping the 3D structures of small molecule binding sites. Journal of Cheminformatics, 8. p. 13. ISSN 1758-2946

Andrews, M. D., Green, M. P., Allerton, C. M. N., Batchelor, D. V., Blagg, J., Brown, A. D., Gordon, D. W., McMurray, G., Millns, D. J., Nichols, C. L., Watson, L. (2009) Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT2c agonists. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19 (18). pp. 5346-5350. ISSN 0960-894X

Hitchin, J. R., Blagg, J., Burke, R., Burns, S., Cockerill, M. J., Fairweather, E. E., Hutton, C., Jordan, A. M., McAndrew, C., Mirza, A., Mould, D., Thomson, G. J., Waddell, I., Ogilvie, D. J. (2013) Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments. Medchemcomm, 4 (11). pp. 1513-1522. ISSN 2040-2503

Firth, N. C., Atrash, B., Brown, N., Blagg, J. (2015) MOARF, an Integrated Workflow for Multiobjective Optimization: Implementation, Synthesis, and Biological Evaluation. JOURNAL OF CHEMICAL INFORMATION AND MODELING, 55 (6). pp. 1169-1180. ISSN 1549-9596

Price, D. A., Blagg, J., Jones, L., Greene, N., Wager, T. (2009) Physicochemical drug properties associated with in vivo toxicological outcomes: a review. EXPERT OPINION ON DRUG METABOLISM, 5 (8). pp. 921-931. ISSN 1742-5255

Hughes, J. D., Blagg, J., Price, D. A., Bailey, S., DeCrescenzo, G. A., Devraj, R. V., Ellsworth, E., Fobian, Y. M., Gibbs, M. E., Gilles, R. W., Greene, N., Huang, E., Krieger-Burke, T., Loesel, J., Wager, T., Whiteley, L., Zhang, Y. (2008) Physiochemical drug properties associated with in vivo toxicological outcomes. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18 (17). pp. 4872-4875. ISSN 0960-894X

Firth, N. C., Brown, N., Blagg, J. (2012) Plane of Best Fit: A Novel Method to Characterize the Three-Dimensionality of Molecules. JOURNAL OF CHEMICAL INFORMATION AND MODELING, 52 (10). pp. 2516-2525. ISSN 1549-9596

Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., Bountra, C., Brennan, P. E., Brown, P. J., Bunnage, M. E., Buser-Doepner, C., Campbell, R. M., Carter, A. J., Cohen, P., Copeland, R. A., Cravatt, B., Dahlin, J. L., Dhanak, D., Edwards, A. M., Frye, S. V., Gray, N., Grimshaw, C. E., Hepworth, D., Howe, T., Huber, K. V. M., Jin, J., Knapp, S., Kotz, J. D., Kruger, R. G., Lowe, D., Mader, M. M., Marsden, B., Mueller-Fahrnow, A., Muller, S., O'Hagan, R. C., Overington, J. P., Owen, D. R., Rosenberg, S. H., Roth, B., Ross, R., Schapira, M., Schreiber, S. L., Shoichet, B., Sundstrom, M., Superti-Furga, G., Taunton, J., Toledo-Sherman, L., Walpole, C., Walters, M. A., Willson, T. M., Workman, P., Young, R. N., Zuercher, W. J. (2015) The promise and peril of chemical probes. NATURE CHEMICAL BIOLOGY, 11 (8). pp. 536-541. ISSN 1552-4450

Latremoliere, A., Latini, A., Andrews, N., Cronin, S. J., Fujita, M., Gorska, K., Hovius, R., Romero, C., Chuaiphichai, S., Painter, M., Miracca, G., Babaniyi, O., Remor, A. P., Duong, K., Riva, P., Barrett, L. B., Ferreiros, N., Naylor, A., Penninger, J. M., Tegeder, I., Zhong, J., Blagg, J., Channon, K. M., Johnsson, K., Costigan, M., Woolf, C. J. (2015) Reduction of Neuropathic and Inflammatory Pain through Inhibition of the Tetrahydrobiopterin Pathway. NEURON, 86 (6). pp. 1393-1406. ISSN 0896-6273

Langdon, S. R., Brown, N., Blagg, J. (2011) Scaffold Diversity of Exemplified Medicinal Chemistry Space. JOURNAL OF CHEMICAL INFORMATION AND MODELING, 51 (9). pp. 2174-2185. ISSN 1549-9596

Naylor, A. M., Pojasek, K. R., Hopkins, A. L., Blagg, J. (2010) The tetrahydrobiopterin pathway and pain. CURRENT OPINION IN INVESTIGATIONAL DRUGS, 11 (1). pp. 19-30. ISSN 1472-4472

Macdonald, J., Oldfield, V., Bavetsias, V., Blagg, J. (2013) Regioselective C2-arylation of imidazo 4,5-b pyridines. ORGANIC & BIOMOLECULAR CHEMISTRY, 11 (14). pp. 2335-2347. ISSN 1477-0520

Bavetsias, V., Perez-Fuertes, Y., McIntyre, P. J., Atrash, B., Kosmopoulou, M., O'Fee, L., Burke, R., Sun, C. B., Faisal, A., Bush, K., Avery, S., Henley, A., Raynaud, F. I., Linardopoulos, S., Bayliss, R., Blagg, J. (2015) 7-(Pyrazol-4-yl)-3H-imidazo 4,5-b pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 25 (19). pp. 4203-4209. ISSN 0960-894X

Bouloc, N., Large, J. M., Kosmopoulou, M., Sun, C., Faisal, A., Matteucci, M., Reynisson, J., Brown, N., Atrash, B., Blagg, J., McDonald, E., Linardopoulos, S., Bayliss, R., Bavetsias, V. (2010) Structure-based design of imidazo[1,2-a] pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 20 (20). pp. 5988-5993. ISSN 0960-894X

Rowan, F., Richards, M., Widya, M., Bayliss, R., Blagg, J. (2014) Diverse Functionalization of Aurora-A Kinase at Specified Surface and Buried Sites by Native Chemical Modification. PLOS ONE, 9 (8). ISSN 1932-6203

Rowan, F. C., Richards, M., Bibby, R. A., Thompson, A., Bayliss, R., Blagg, J. (2013) Insights into Aurora-A Kinase Activation Using Unnatural Amino Acids Incorporated by Chemical Modification. ACS CHEMICAL BIOLOGY, 8 (10). pp. 2184-2191. ISSN 1554-8929

Faisal, A., Vaughan, L., Bavetsias, V., Sun, C. B., Atrash, B., Avery, S., Jamin, Y., Robinson, S. P., Workman, P., Blagg, J., Raynaud, F. I., Eccles, S. A., Chesler, L., Linardopoulos, S. (2011) The Aurora Kinase Inhibitor CCT137690 Downregulates MYCN and Sensitizes MYCN-Amplified Neuroblastoma In Vivo. MOLECULAR CANCER THERAPEUTICS, 10 (11). pp. 2115-2123. ISSN 1535-7163

Mallinger, A., Crumpler, S., Pichowicz, M., Waalboer, D., Stubbs, M., Adeniji-Popoola, O., Wood, B., Smith, E., Thai, C., Henley, A. T., Georgi, K., Court, W., Hobbs, S., Box, G., Ortiz-Ruiz, M. J., Valenti, M., Brandon, A. D. H., TePoele, R., Leuthner, B., Workman, P., Aherne, W., Poeschke, O., Dale, T., Wienke, D., Esdar, C., Rohdich, F., Raynaud, F., Clarke, P. A., Eccles, S. A., Stieber, F., Schiemann, K., Blagg, J. (2015) Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen. JOURNAL OF MEDICINAL CHEMISTRY, 58 (4). pp. 1717-1735. ISSN 0022-2623

Lubbe, S. J., Pittman, A. M., Matijssen, C., Twiss, P., Olver, B., Lloyd, A., Qureshi, M., Brown, N., Nye, E., Stamp, G., Blagg, J., Houlston, R. S. (2011) Evaluation of Germline BMP4 Mutation as a Cause of Colorectal Cancer. HUMAN MUTATION, 32 (1). E1928-E1938. ISSN 1059-7794

Linardopoulos, S., Blagg, J. (2015) Aurora Kinase Inhibition: A New Light in the Sky? JOURNAL OF MEDICINAL CHEMISTRY, 58 (13). pp. 5186-5188. ISSN 0022-2623

Pichowicz, M., Crumpler, S., McDonald, E., Blagg, J. (2010) Microwave-assisted synthesis of 4-amino-3,5-dihalopyridines. TETRAHEDRON, 66 (13). pp. 2398-2403. ISSN 0040-4020

Hatch, S. B., Yapp, C., Montenegro, R. C., Savitsky, P., Gamble, V., Tumber, A., Ruda, G. F., Bavetsias, V., Fedorov, O., Atrash, B., Raynaud, F., Lanigan, R., Carmichael, L., Tomlin, K., Burke, R., Westaway, S. M., Brown, J. A., Prinjha, R. K., Martinez, E. D., Oppermann, U., Schofield, C. J., Bountra, C., Kawamura, A., Blagg, J., Brennan, P. E., Rossanese, O., Muller, S. (2017) Assessing histone demethylase inhibitors in cells: lessons learned. Epigenetics & Chromatin, 10. ISSN 1756-8935

Matijssen, C., Silva-Santisteban, M. C., Westwood, I. M., Siddique, S., Choi, V., Sheldrake, P., van Montfort, R. L. M., 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, 20 (22). pp. 6630-6639. ISSN 0968-0896

Liu, M. J., Mallinger, A., Tortorici, M., Newbatt, Y., Richards, M., Mirza, A., van Montfort, R. L. M., Burke, R., Blagg, J., Kaserer, T. (2018) Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates. ACS CHEMICAL BIOLOGY, 13 (9). pp. 2427-2432. ISSN 1554-8929

Naud, S., Westwood, I. M., Faisal, A., Sheldrake, P., Bavetsias, V., Atrash, B., Cheung, K. M. J., Liu, M. J., Hayes, A., Schmitt, J., Wood, A., Choi, V., Boxall, K., Mak, G., Gurden, M., Valenti, M., Brandon, A. D., Henley, A., Baker, R., McAndrew, C., Matijssen, B., Burke, R., Hoelder, S., Eccles, S. A., Raynaud, F. I., Linardopoulos, S., van Montfort, R. L. M., Blagg, J. (2013) Structure-Based Design of Orally Bioavailable 1H-Pyrrolo 3,2-c pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1). JOURNAL OF MEDICINAL CHEMISTRY, 56 (24). pp. 10045-10065. ISSN 0022-2623

Blagg, J., Workman, P. (2017) Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology. CANCER CELL, 32 (1). pp. 9-25. ISSN 1535-6108

Blagg, J., Workman, P. (2014) Chemical biology approaches to target validation in cancer. CURRENT OPINION IN PHARMACOLOGY, 17. pp. 87-100. ISSN 1471-4892

Travers, J., Blagg, J., Workman, P. (2011) EPIGENETICS Targeting leukemia on the DOT. NATURE CHEMICAL BIOLOGY, 7 (10). pp. 663-665. ISSN 1552-4450

Knapp, S., Arruda, P., Blagg, J., Burley, S., Drewry, D. H., Edwards, A., Fabbro, D., Gillespie, P., Gray, N. S., Kuster, B., Lackey, K. E., Mazzafera, P., Tomkinson, N. C. O., Willson, T. M., Workman, P., Zuercher, W. J. (2013) A public-private partnership to unlock the untargeted kinome. NATURE CHEMICAL BIOLOGY, 9 (1). pp. 3-7. ISSN 1552-4450

Gurden, M. D., Westwood, I. M., Faisal, A., Naud, S., Cheung, K. M. J., McAndrew, C., Wood, A., Schmitt, J., Boxall, K., Mak, G., Workman, P., Burke, R., Hoelder, S., Blagg, J., Van Montfort, R. L. M., Linardopoulos, S. (2015) Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. CANCER RESEARCH, 75 (16). pp. 3340-3354. ISSN 0008-5472

Barillari, C., Duncan, A. L., Westwood, I. M., Blagg, J., van Montfort, R. L. M. (2011) Analysis of water patterns in protein kinase binding sites. PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS, 79 (7). pp. 2109-2121. ISSN 0887-3585

C

Dale, T., Clarke, P. A., Esdar, C., Waalboer, D., Adeniji-Popoola, O., Ortiz-Ruiz, M. J., Mallinger, A., Samant, R. S., Czodrowski, P., Musil, D., Schwarz, D., Schneider, K., Stubbs, M., Ewan, K., Fraser, E., TePoele, R., Court, W., Box, G., Valenti, M., Brandon, A. D., Gowan, S., Rohdich, F., Raynaud, F., Schneider, R., Poeschke, O., Blaukat, A., Workman, P., Schiemann, K., Eccles, S. A., Wienke, D., Blagg, J. (2015) A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. NATURE CHEMICAL BIOLOGY, 11 (12). pp. 973-980. ISSN 1552-4450

D

Sharp, A., Welti, J., Blagg, J., de Bono, J. S. (2016) Targeting Androgen Receptor Aberrations in Castration-Resistant Prostate Cancer. CLINICAL CANCER RESEARCH, 22 (17). pp. 4280-4282. ISSN 1078-0432

E

Czodrowski, P., Mallinger, A., Wienke, D., Esdar, C., Poschke, O., Busch, M., Rohdich, F., Eccles, S. A., Ortiz-Ruiz, M. J., Schneider, R., Raynaud, F. I., Clarke, P. A., Musil, D., Schwarz, D., Dale, T., Urbahns, K., Blagg, J., Schiemann, K. (2016) Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. JOURNAL OF MEDICINAL CHEMISTRY, 59 (20). pp. 9337-9349. ISSN 0022-2623

Schiemann, K., Mallinger, A., Wienke, D., Esdar, C., Poeschke, O., Busch, M., Rohdich, F., Eccles, S. A., Schneider, R., Raynaud, F. I., Czodrowski, P., Musil, D., Schwarz, D., Urbahns, K., Blagg, J. (2016) Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26 (5). pp. 1443-1451. ISSN 0960-894X

Wilson, S. C., Atrash, B., Barlow, C., Eccles, S., Fischer, P. M., Hayes, A., Kelland, L., Jackson, W., Jarman, M., Mirza, A., Moreno, J., Nutley, B. P., Raynaud, F. I., Sheldrake, P., Walton, M., Westwood, R., Whittaker, S., Workman, P., McDonald, E. (2011) Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. BIOORGANIC & MEDICINAL CHEMISTRY, 19 (22). pp. 6949-6965. ISSN 0968-0896

H

Woodward, H. L., Innocenti, P., Cheung, K. M. J., Hayes, A., Roberts, J., Henley, A. T., Faisal, A., Mak, G. W. Y., Box, G., Westwood, I. M., Cronin, N., Carter, M., Valenti, M., Brandon, A. D., O'Fee, L., Saville, H., Schmitt, J., Burke, R., Broccatelli, F., van Montfort, R. L. M., 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 N-2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N-8-neo pentylpyrido 3,4-d pyrimidine-2,8-diamine (BOS172722). JOURNAL OF MEDICINAL CHEMISTRY, 61 (18). pp. 8226-8240. ISSN 0022-2623

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. M. (2013) Fragment-Based Screening Maps Inhibitor Interactions in the ATP-Binding Site of Checkpoint Kinase 2. PLOS ONE, 8 (6). ISSN 1932-6203

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. Y., Box, G., Valenti, M., Brandon, A. D. H., O'Fee, L., Saville, H., Schmitt, J., Matijssen, B., Burke, R., van Montfort, R. L. M., 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. JOURNAL OF MEDICINAL CHEMISTRY, 59 (8). pp. 3671-3688. ISSN 0022-2623

M

Stockwell, S. R., Platt, G., Barrie, S. E., Zoumpoulidou, G., Poele, R. H. T., Aherne, G. W., Wilson, S. C., Sheldrake, P., McDonald, E., Venet, M., Soudy, C., Elustondo, F., Rigoreau, L., Blagg, J., Workman, P., Garrett, M. D., Mittnacht, S. (2012) Mechanism-Based Screen for G1/S Checkpoint Activators Identifies a Selective Activator of EIF2AK3/PERK Signalling. PLOS ONE, 7 (1). ISSN 1932-6203

Gutierrez, C. D., Bavetsias, V., McDonald, E. (2008) ClTi((OPr)-Pr-i)(3)-promoted reductive amination on the solid phase: Combinatorial synthesis of a biaryl-based sulfonamide library. JOURNAL OF COMBINATORIAL CHEMISTRY, 10 (2). pp. 280-284. ISSN 1520-4766

Bavetsias, V., Henderson, E.A., McDonald, E. (2007) Cyclopenta[g]quinazolinone-based inhibitors of thymidylate synthase targeting alpha-folate receptor overexpressing tumours: synthetic approaches to 4-{N-[(6RS)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino}benzoic acid. TETRAHEDRON, 63 (7). pp. 1537-1543. ISSN 0040-4020

McDonald, E., Bavetsias, V. (2005) Discovery of small molecules as anticancer agents: the role of the medicinal chemist in the discovery of new cancer therapeutics. FORUM OF CLINICAL ONCOLOGY, 4. pp. 51-57.

Gutierrez, C. D., Bavetsias, V., McDonald, E. (2005) TiCl((OPr)-Pr-i)(3) and NaBH(OAc)(3): an efficient reagent combination for the reductive amination of aldehydes by electron-deficient amines. TETRAHEDRON LETTERS, 46 (20). pp. 3595-3597. ISSN 0040-4039

Sheldrake, P. W., Matteucci, M., McDonald, E. (2006) Facile generation of a library of 5-aryl-2-arylsulfonyl-1,3-thiazoles. SYNLETT, 3. pp. 460-462. ISSN 0936-5214

P

Moore, A. S., Blagg, J., Linardopoulos, S., Pearson, A. D. J. (2010) Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias. LEUKEMIA, 24 (4). pp. 671-678. ISSN 0887-6924

Moore, A. S., Faisal, A., de Castro, D. G., Bavetsias, V., Sun, C., Atrash, B., Valenti, M., Brandon, A. D., Avery, S., Mair, D., Mirabella, F., Swansbury, J., Pearson, A. D. J., Workman, P., Blagg, J., Raynaud, F. I., Eccles, S. A., Linardopoulos, S. (2012) Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns. LEUKEMIA, 26 (7). pp. 1462-1470. ISSN 0887-6924

R

Large, J. M., Torr, J. E., Raynaud, F. I., Clarke, P. A., Hayes, A., di Stefano, F., Urban, F., Shuttleworth, S. J., Saghir, N., Sheldrake, P., Workman, P., McDonald, E. (2011) Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements. BIOORGANIC & MEDICINAL CHEMISTRY, 19 (2). pp. 836-851. ISSN 0968-0896

Ewan, K., Pajak, B., Stubbs, M., Todd, H., Barbeau, O., Quevedo, C., Botfield, H., Young, R., Ruddle, R., Samuel, L., Battersby, A., Raynaud, F., Allen, N., Wilson, S., Latinkic, B., Workman, P., McDonald, E., Blagg, J., Aherne, W., Dale, T. (2010) A Useful Approach to Identify Novel Small-Molecule Inhibitors of Wnt-Dependent Transcription. CANCER RESEARCH, 70 (14). pp. 5963-5973. ISSN 0008-5472

S

Gilburt, J. A. H., Sarkar, H., Sheldrake, P., Blagg, J., Ying, L. M., Dodson, C. A. (2017) Dynamic Equilibrium of the Aurora A Kinase Activation Loop Revealed by Single-Molecule Spectroscopy. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 56 (38). pp. 11409-11414. ISSN 1433-7851

Bavetsias, V., Crumpler, S., Sun, C. B., Avery, S., Atrash, B., Faisal, A., Moore, A. S., Kosmopoulou, M., Brown, N., Sheldrake, P. W., Bush, K., Henley, A., Box, G., Valenti, M., Brandon, A. D., Raynaud, F. I., Workman, P., Eccles, S. A., Bayliss, R., Linardopoulos, S., Blagg, J. (2012) Optimization of Imidazo 4,5-b pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia. JOURNAL OF MEDICINAL CHEMISTRY, 55 (20). pp. 8721-8734. ISSN 0022-2623

Walters, Z. S., Villarejo-Balcells, B., Olmos, D., Buist, T. W. S., Missiaglia, E., Allen, R., Al-Lazikani, B., Garrett, M. D., Blagg, J., Shipley, J. (2014) JARID2 is a direct target of the PAX3-FOXO1 fusion protein and inhibits myogenic differentiation of rhabdomyosarcoma cells. ONCOGENE, 33 (9). pp. 1148-1157. ISSN 0950-9232

V

Langdon, S. R., Westwood, I. M., van Montfort, R. L. M., Brown, N., Blagg, J. (2013) Scaffold-Focused Virtual Screening: Prospective Application to the Discovery of TTK Inhibitors. JOURNAL OF CHEMICAL INFORMATION AND MODELING, 53 (5). pp. 1100-1112. ISSN 1549-9596

W

Whittaker, S. R., Barlow, C., Martin, M. P., Mancusi, C., Wagner, S., Self, A., Barrie, E., Te Poele, R., Sharp, S., Brown, N., Wilson, S., Jackson, W., Fischer, P. M., Clarke, P. A., Walton, M. I., McDonald, E., Blagg, J., Noble, M., Garrett, M. D., Workman, P. (2018) Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor. MOLECULAR ONCOLOGY, 12 (3). pp. 287-304. ISSN 1574-7891

Mallinger, A., Schiemann, K., Rink, C., Sejberg, J., Honey, M. A., Czodrowski, P., Stubbs, M., Poeschke, O., Busch, M., Schneider, R., Schwarz, D., Musil, D., Burke, R., Urbahns, K., Workman, P., Wienke, D., Clarke, P. A., Raynaud, F. I., Eccles, S. A., Esdar, C., Rohdich, F., Blagg, J. (2016) 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. Acs Medicinal Chemistry Letters, 7 (6). pp. 573-578. ISSN 1948-5875

Mallinger, A., Schiemann, K., Rink, C., Stieber, F., Calderini, M., Crumpler, S., Stubbs, M., Adeniji-Popoola, O., Poeschke, O., Busch, M., Czodrowski, P., Musil, D., Schwarz, D., Ortiz-Ruiz, M. J., Schneider, R., Thai, C., Valenti, M., Brandon, A. D., Burke, R., Workman, P., Dale, T., Wienke, D., Clarke, P. A., Esdar, C., Raynaud, F. I., Eccles, S. A., Rohdich, F., Blagg, J. (2016) Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. JOURNAL OF MEDICINAL CHEMISTRY, 59 (3). pp. 1078-1101. ISSN 0022-2623