Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic
WORKMAN, Paul, CLARKE, Paul A, RAYNAUD, Florence I, VAN MONTFORT, Rob L. M
Published in Cancer research (Chicago, Ill.) (15.03.2010)
Published in Cancer research (Chicago, Ill.) (15.03.2010)
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Journal Article
Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B
Jhoti, Harren, van Montfort, Rob L. M, Congreve, Miles, Tisi, Dominic, Carr, Robin
Published in Nature (London) (12.06.2003)
Published in Nature (London) (12.06.2003)
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Journal Article
Structure-Based Design of Orally Bioavailable 1H‑Pyrrolo[3,2‑c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)
Naud, Sébastien, Westwood, Isaac M, Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J, Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A, Raynaud, Florence I, Linardopoulos, Spiros, van Montfort, Rob L. M, Blagg, Julian
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Journal Article
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen
Cheeseman, Matthew D, Chessum, Nicola E. A, Rye, Carl S, Pasqua, A. Elisa, Tucker, Michael J, Wilding, Birgit, Evans, Lindsay E, Lepri, Susan, Richards, Meirion, Sharp, Swee Y, Ali, Salyha, Rowlands, Martin, O’Fee, Lisa, Miah, Asadh, Hayes, Angela, Henley, Alan T, Powers, Marissa, te Poele, Robert, De Billy, Emmanuel, Pellegrino, Loredana, Raynaud, Florence, Burke, Rosemary, van Montfort, Rob L. M, Eccles, Suzanne A, Workman, Paul, Jones, Keith
Published in Journal of medicinal chemistry (12.01.2017)
Published in Journal of medicinal chemistry (12.01.2017)
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Journal Article
Structure of the Epigenetic Oncogene MMSET and Inhibition by N‑Alkyl Sinefungin Derivatives
Tisi, Dominic, Chiarparin, Elisabetta, Tamanini, Emiliano, Pathuri, Puja, Coyle, Joseph E, Hold, Adam, Holding, Finn P, Amin, Nader, Martin, Agnes C. L, Rich, Sharna J, Berdini, Valerio, Yon, Jeff, Acklam, Paul, Burke, Rosemary, Drouin, Ludovic, Harmer, Jenny E, Jeganathan, Fiona, van Montfort, Rob L. M, Newbatt, Yvette, Tortorici, Marcello, Westlake, Maura, Wood, Amy, Hoelder, Swen, Heightman, Tom D
Published in ACS chemical biology (18.11.2016)
Published in ACS chemical biology (18.11.2016)
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Journal Article
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70
Cheeseman, Matthew D, Westwood, Isaac M, Barbeau, Olivier, Rowlands, Martin, Dobson, Sarah, Jones, Alan M, Jeganathan, Fiona, Burke, Rosemary, Kadi, Nadia, Workman, Paul, Collins, Ian, van Montfort, Rob L. M, Jones, Keith
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Journal Article
Aminopyrazine Inhibitors Binding to an Unusual Inactive Conformation of the Mitotic Kinase Nek2: SAR and Structural Characterization
Whelligan, Daniel K, Solanki, Savade, Taylor, Dawn, Thomson, Douglas W, Cheung, Kwai-Ming J, Boxall, Kathy, Mas-Droux, Corine, Barillari, Caterina, Burns, Samantha, Grummitt, Charles G, Collins, Ian, van Montfort, Rob L. M, Aherne, G. Wynne, Bayliss, Richard, Hoelder, Swen
Published in Journal of medicinal chemistry (11.11.2010)
Published in Journal of medicinal chemistry (11.11.2010)
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Journal Article
Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors
Howard, Nigel, Abell, Chris, Blakemore, Wendy, Chessari, Gianni, Congreve, Miles, Howard, Steven, Jhoti, Harren, Murray, Christopher W, Seavers, Lisa C. A, van Montfort, Rob L. M
Published in Journal of medicinal chemistry (23.02.2006)
Published in Journal of medicinal chemistry (23.02.2006)
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Journal Article
Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing
Reader, John C, Matthews, Thomas P, Klair, Suki, Cheung, Kwai-Ming J, Scanlon, Jane, Proisy, Nicolas, Addison, Glynn, Ellard, John, Piton, Nelly, Taylor, Suzanne, Cherry, Michael, Fisher, Martin, Boxall, Kathy, Burns, Samantha, Walton, Michael I, Westwood, Isaac M, Hayes, Angela, Eve, Paul, Valenti, Melanie, de Haven Brandon, Alexis, Box, Gary, van Montfort, Rob L. M, Williams, David H, Aherne, G. Wynne, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian
Published in Journal of medicinal chemistry (22.12.2011)
Published in Journal of medicinal chemistry (22.12.2011)
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Journal Article
Structure-based design of molecular cancer therapeutics
van Montfort, Rob L.M, Workman, Paul
Published in Trends in biotechnology (Regular ed.) (01.05.2009)
Published in Trends in biotechnology (Regular ed.) (01.05.2009)
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Journal Article
Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2
Silva-Santisteban, M Cris, Westwood, Isaac M, Boxall, Kathy, Brown, Nathan, Peacock, Sam, McAndrew, Craig, Barrie, Elaine, Richards, Meirion, Mirza, Amin, Oliver, Antony W, Burke, Rosemary, Hoelder, Swen, Jones, Keith, Aherne, G Wynne, Blagg, Julian, Collins, Ian, Garrett, Michelle D, van Montfort, Rob L M
Published in PloS one (12.06.2013)
Published in PloS one (12.06.2013)
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Journal Article
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders
Bellenie, Benjamin R, Cheung, Kwai-Ming J, Varela, Ana, Pierrat, Olivier A, Collie, Gavin W, Box, Gary M, Bright, Michael D, Gowan, Sharon, Hayes, Angela, Rodrigues, Matthew J, Shetty, Kartika N, Carter, Michael, Davis, Owen A, Henley, Alan T, Innocenti, Paolo, Johnson, Louise D, Liu, Manjuan, de Klerk, Selby, Le Bihan, Yann-Vaï, Lloyd, Matthew G, McAndrew, P. Craig, Shehu, Erald, Talbot, Rachel, Woodward, Hannah L, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M, Raynaud, Florence I, Rossanese, Olivia W, Hoelder, Swen
Published in Journal of medicinal chemistry (23.04.2020)
Published in Journal of medicinal chemistry (23.04.2020)
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Journal Article
Analysis of water patterns in protein kinase binding sites
Barillari, Caterina, Duncan, Anna L., Westwood, Isaac M., Blagg, Julian, van Montfort, Rob L. M.
Published in Proteins, structure, function, and bioinformatics (01.07.2011)
Published in Proteins, structure, function, and bioinformatics (01.07.2011)
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Journal Article
A Degron Blocking Strategy Towards Improved CRL4CRBN Recruiting PROTAC Selectivity
Habib Bouguenina, Scarpino, Andrea, O'Hanlon, Jack A, Warne, Justin, Wang, Hannah Z, Laura Chan Wah Hak, Sadok, Amine, McAndrew, P Craig, Stubbs, Mark, Pierrat, Olivier A, Hahner, Tamas, Cabry, Marc P, Yann‐Vaï Le Bihan, Mitsopoulos, Costas, Sialana, Fernando J, Roumeliotis, Theodoros I, Burke, Rosemary, Rob L M van Montfort, Choudhari, Jyoti, Chopra, Rajesh, Caldwell, John J, Collins, Ian
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
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Journal Article
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket
Lloyd, Matthew G, Huckvale, Rosemary, Cheung, Kwai-Ming J, Rodrigues, Matthew J, Collie, Gavin W, Pierrat, Olivier A, Gatti Iou, Mahad, Carter, Michael, Davis, Owen A, McAndrew, P. Craig, Gunnell, Emma, Le Bihan, Yann-Vaï, Talbot, Rachel, Henley, Alan T, Johnson, Louise D, Hayes, Angela, Bright, Michael D, Raynaud, Florence I, Meniconi, Mirco, Burke, Rosemary, van Montfort, Rob L. M, Rossanese, Olivia W, Bellenie, Benjamin R, Hoelder, Swen
Published in Journal of medicinal chemistry (09.12.2021)
Published in Journal of medicinal chemistry (09.12.2021)
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Journal Article
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‑neopentylpyrido[3,4‑d]pyrimidine-2,8-diamine (BOS172722)
Woodward, Hannah L, Innocenti, Paolo, Cheung, Kwai-Ming J, Hayes, Angela, Roberts, Jennie, Henley, Alan T, Faisal, Amir, Mak, Grace Wing-Yan, Box, Gary, Westwood, Isaac M, Cronin, Nora, Carter, Michael, Valenti, Melanie, De Haven Brandon, Alexis, O’Fee, Lisa, Saville, Harry, Schmitt, Jessica, Burke, Rosemary, Broccatelli, Fabio, van Montfort, Rob L. M, Raynaud, Florence I, Eccles, Suzanne A, Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen
Published in Journal of medicinal chemistry (27.09.2018)
Published in Journal of medicinal chemistry (27.09.2018)
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Journal Article
Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays
Pierrat, Olivier A., Liu, Manjuan, Collie, Gavin W., Shetty, Kartika, Rodrigues, Matthew J., Le Bihan, Yann-Vaï, Gunnell, Emma A., McAndrew, P. Craig, Stubbs, Mark, Rowlands, Martin G., Yahya, Norhakim, Shehu, Erald, Talbot, Rachel, Pickard, Lisa, Bellenie, Benjamin R., Cheung, Kwai-Ming J., Drouin, Ludovic, Innocenti, Paolo, Woodward, Hannah, Davis, Owen A., Lloyd, Matthew G., Varela, Ana, Huckvale, Rosemary, Broccatelli, Fabio, Carter, Michael, Galiwango, David, Hayes, Angela, Raynaud, Florence I., Bryant, Christopher, Whittaker, Steven, Rossanese, Olivia W., Hoelder, Swen, Burke, Rosemary, van Montfort, Rob L. M.
Published in Scientific reports (03.11.2022)
Published in Scientific reports (03.11.2022)
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Journal Article
Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates
Liu, Manjuan, Mallinger, Aurélie, Tortorici, Marcello, Newbatt, Yvette, Richards, Meirion, Mirza, Amin, van Montfort, Rob L. M, Burke, Rosemary, Blagg, Julian, Kaserer, Teresa
Published in ACS chemical biology (21.09.2018)
Published in ACS chemical biology (21.09.2018)
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