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
PAK4 promotes kinase-independent stabilization of RhoU to modulate cell adhesion
Dart, Anna E, Box, Gary M, Court, William, Gale, Madeline E, Brown, John P, Pinder, Sarah E, Eccles, Suzanne A, Wells, Claire M
Published in The Journal of cell biology (23.11.2015)
Published in The Journal of cell biology (23.11.2015)
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Journal Article
The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer
Folkes, Adrian J, Ahmadi, Khatereh, Alderton, Wendy K, Alix, Sonia, Baker, Stewart J, Box, Gary, Chuckowree, Irina S, Clarke, Paul A, Depledge, Paul, Eccles, Suzanne A, Friedman, Lori S, Hayes, Angela, Hancox, Timothy C, Kugendradas, Arumugam, Lensun, Letitia, Moore, Pauline, Olivero, Alan G, Pang, Jodie, Patel, Sonal, Pergl-Wilson, Giles H, Raynaud, Florence I, Robson, Anthony, Saghir, Nahid, Salphati, Laurent, Sohal, Sukhjit, Ultsch, Mark H, Valenti, Melanie, Wallweber, Heidi J.A, Wan, Nan Chi, Wiesmann, Christian, Workman, Paul, Zhyvoloup, Alexander, Zvelebil, Marketa J, Shuttleworth, Stephen J
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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Journal Article
NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis
Eccles, Suzanne A, Massey, Andy, Raynaud, Florence I, Sharp, Swee Y, Box, Gary, Valenti, Melanie, Patterson, Lisa, de Haven Brandon, Alexis, Gowan, Sharon, Boxall, Frances, Aherne, Wynne, Rowlands, Martin, Hayes, Angela, Martins, Vanessa, Urban, Frederique, Boxall, Kathy, Prodromou, Chrisostomos, Pearl, Laurence, James, Karen, Matthews, Thomas P, Cheung, Kwai-Ming, Kalusa, Andrew, Jones, Keith, McDonald, Edward, Barril, Xavier, Brough, Paul A, Cansfield, Julie E, Dymock, Brian, Drysdale, Martin J, Finch, Harry, Howes, Rob, Hubbard, Roderick E, Surgenor, Alan, Webb, Paul, Wood, Mike, Wright, Lisa, Workman, Paul
Published in Cancer research (Chicago, Ill.) (15.04.2008)
Published in Cancer research (Chicago, Ill.) (15.04.2008)
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Journal Article
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones
Harnden, Alice C., Davis, Owen A., Box, Gary M., Hayes, Angela, Johnson, Louise D., Henley, Alan T., de Haven Brandon, Alexis K., Valenti, Melanie, Cheung, Kwai-Ming J., Brennan, Alfie, Huckvale, Rosemary, Pierrat, Olivier A., Talbot, Rachel, Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, de Klerk, Selby, McAndrew, Peter Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (27.04.2023)
Published in Journal of medicinal chemistry (27.04.2023)
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Journal Article
Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941
Raynaud, Florence I, Eccles, Suzanne A, Patel, Sonal, Alix, Sonia, Box, Gary, Chuckowree, Irina, Folkes, Adrian, Gowan, Sharon, De Haven Brandon, Alexis, Di Stefano, Francesca, Hayes, Angela, Henley, Alan T, Lensun, Letitia, Pergl-Wilson, Giles, Robson, Anthony, Saghir, Nahid, Zhyvoloup, Alexander, McDonald, Edward, Sheldrake, Peter, Shuttleworth, Stephen, Valenti, Melanie, Wan, Nan Chi, Clarke, Paul A, Workman, Paul
Published in Molecular cancer therapeutics (01.07.2009)
Published in Molecular cancer therapeutics (01.07.2009)
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Journal Article
Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen
Mallinger, Aurélie, Crumpler, Simon, Pichowicz, Mark, Waalboer, Dennis, Stubbs, Mark, Adeniji-Popoola, Olajumoke, Wood, Bozena, Smith, Elizabeth, Thai, Ching, Henley, Alan T, Georgi, Katrin, Court, William, Hobbs, Steve, Box, Gary, Ortiz-Ruiz, Maria-Jesus, Valenti, Melanie, De Haven Brandon, Alexis, TePoele, Robert, Leuthner, Birgitta, Workman, Paul, Aherne, Wynne, Poeschke, Oliver, Dale, Trevor, Wienke, Dirk, Esdar, Christina, Rohdich, Felix, Raynaud, Florence, Clarke, Paul A, Eccles, Suzanne A, Stieber, Frank, Schiemann, Kai, Blagg, Julian
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
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Journal Article
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo
Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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Journal Article
Theranostic Attributes of Acoustic Cluster Therapy and Its Use for Enhancing the Effectiveness of Liposomal Doxorubicin Treatment of Human Triple Negative Breast Cancer in Mice
Bush, Nigel, Healey, Andrew, Shah, Anant, Box, Gary, Kirkin, Vladimir, Eccles, Sue, Sontum, Per Christian, Kotopoulis, Spiros, Kvåle, Svein, van Wamel, Annemieke, Davies, Catharina de Lange, Bamber, Jeffrey
Published in Frontiers in pharmacology (20.02.2020)
Published in Frontiers in pharmacology (20.02.2020)
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Journal Article
Therapeutic Dose Response of Acoustic Cluster Therapy in Combination With Irinotecan for the Treatment of Human Colon Cancer in Mice
Bush, Nigel, Healey, Andrew, Shah, Anant, Box, Gary, Kirkin, Vladimir, Kotopoulis, Spiros, Kvåle, Svein, Sontum, Per Christian, Bamber, Jeffrey
Published in Frontiers in pharmacology (19.11.2019)
Published in Frontiers in pharmacology (19.11.2019)
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Journal Article
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases
Clarke, Paul A, Ortiz-Ruiz, Maria-Jesus, TePoele, Robert, Adeniji-Popoola, Olajumoke, Box, Gary, Court, Will, Czasch, Stephanie, El Bawab, Samer, Esdar, Christina, Ewan, Ken, Gowan, Sharon, De Haven Brandon, Alexis, Hewitt, Phillip, Hobbs, Stephen M, Kaufmann, Wolfgang, Mallinger, Aurélie, Raynaud, Florence, Roe, Toby, Rohdich, Felix, Schiemann, Kai, Simon, Stephanie, Schneider, Richard, Valenti, Melanie, Weigt, Stefan, Blagg, Julian, Blaukat, Andree, Dale, Trevor C, Eccles, Suzanne A, Hecht, Stefan, Urbahns, Klaus, Workman, Paul, Wienke, Dirk
Published in eLife (09.12.2016)
Published in eLife (09.12.2016)
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Journal Article
Evaluation of the Response of Intracranial Xenografts to VEGF Signaling Inhibition Using Multiparametric MRI
Boult, Jessica K.R., Box, Gary, Vinci, Maria, Perryman, Lara, Eccles, Suzanne A., Jones, Chris, Robinson, Simon P.
Published in Neoplasia (New York, N.Y.) (01.09.2017)
Published in Neoplasia (New York, N.Y.) (01.09.2017)
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Journal Article
FGF7–FGFR2 autocrine signaling increases growth and chemoresistance of fusion‐positive rhabdomyosarcomas
Milton, Christopher I., Selfe, Joanna, Aladowicz, Ewa, Man, Stella Y. K., Bernauer, Carolina, Missiaglia, Edoardo, Walters, Zoë S., Gatz, Susanne A., Kelsey, Anna, Generali, Melanie, Box, Gary, Valenti, Melanie, Haven‐Brandon, Alexis, Galiwango, David, Hayes, Angela, Clarke, Matthew, Izquierdo, Elisa, Gonzalez De Castro, David, Raynaud, Florence I., Kirkin, Vladimir, Shipley, Janet M.
Published in Molecular oncology (01.03.2022)
Published in Molecular oncology (01.03.2022)
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Journal Article
Value of combining dynamic contrast enhanced ultrasound and optoacoustic tomography for hypoxia imaging
Shah, Anant, Bush, Nigel, Box, Gary, Eccles, Suzanne, Bamber, Jeffrey
Published in Photoacoustics (Munich) (01.12.2017)
Published in Photoacoustics (Munich) (01.12.2017)
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Journal Article
Small-Molecule Activation of p53 Blocks Hypoxia-Inducible Factor 1α and Vascular Endothelial Growth Factor Expression In Vivo and Leads to Tumor Cell Apoptosis in Normoxia and Hypoxia
Yang, Jun, Ahmed, Afshan, Poon, Evon, Perusinghe, Nina, de Haven Brandon, Alexis, Box, Gary, Valenti, Melanie, Eccles, Suzanne, Rouschop, Kasper, Wouters, Brad, Ashcroft, Margaret
Published in Molecular and Cellular Biology (15.04.2009)
Published in Molecular and Cellular Biology (15.04.2009)
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Journal Article
Breast Tumour Kinase (Brk/PTK6) Contributes to Breast Tumour Xenograft Growth and Modulates Chemotherapeutic Responses In Vitro
Burmi, Rajpal S, Box, Gary M, Wazir, Umar, Hussain, Haroon A, Davies, Julie A, Court, William J, Eccles, Suzanne A, Jiang, Wen G, Mokbel, Kefah, Harvey, Amanda J
Published in Genes (24.02.2022)
Published in Genes (24.02.2022)
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Journal Article
Enhanced efficacy of IGF1R inhibition in pediatric glioblastoma by combinatorial targeting of PDGFRα/β
Bielen, Aleksandra, Perryman, Lara, Box, Gary M, Valenti, Melanie, de Haven Brandon, Alexis, Martins, Vanessa, Jury, Alexa, Popov, Sergey, Gowan, Sharon, Jeay, Sebastien, Raynaud, Florence I, Hofmann, Francesco, Hargrave, Darren, Eccles, Suzanne A, Jones, Chris
Published in Molecular cancer therapeutics (01.08.2011)
Published in Molecular cancer therapeutics (01.08.2011)
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Journal Article
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease
Dale, Trevor, Clarke, Paul A, Esdar, Christina, Waalboer, Dennis, Adeniji-Popoola, Olajumoke, Ortiz-Ruiz, Maria-Jesus, Mallinger, Aurélie, Samant, Rahul S, Czodrowski, Paul, Musil, Djordje, Schwarz, Daniel, Schneider, Klaus, Stubbs, Mark, Ewan, Ken, Fraser, Elizabeth, TePoele, Robert, Court, Will, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Gowan, Sharon, Rohdich, Felix, Raynaud, Florence, Schneider, Richard, Poeschke, Oliver, Blaukat, Andree, Workman, Paul, Schiemann, Kai, Eccles, Suzanne A, Wienke, Dirk, Blagg, Julian
Published in Nature chemical biology (26.10.2015)
Published in Nature chemical biology (26.10.2015)
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Journal Article
Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation
Ang, Joo Ern, Pandher, Rupinder, Ang, Joo Chew, Asad, Yasmin J, Henley, Alan T, Valenti, Melanie, Box, Gary, de Haven Brandon, Alexis, Baird, Richard D, Friedman, Lori, Derynck, Mika, Vanhaesebroeck, Bart, Eccles, Suzanne A, Kaye, Stan B, Workman, Paul, de Bono, Johann S, Raynaud, Florence I
Published in Molecular cancer therapeutics (01.06.2016)
Published in Molecular cancer therapeutics (01.06.2016)
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Journal Article
Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues
Sharp, Swee Y, Prodromou, Chrisostomos, Boxall, Kathy, Powers, Marissa V, Holmes, Joanna L, Box, Gary, Matthews, Thomas P, Cheung, Kwai-Ming J, Kalusa, Andrew, James, Karen, Hayes, Angela, Hardcastle, Anthea, Dymock, Brian, Brough, Paul A, Barril, Xavier, Cansfield, Julie E, Wright, Lisa, Surgenor, Allan, Foloppe, Nicolas, Hubbard, Roderick E, Aherne, Wynne, Pearl, Laurence, Jones, Keith, McDonald, Edward, Raynaud, Florence, Eccles, Sue, Drysdale, Martin, Workman, Paul
Published in Molecular cancer therapeutics (01.04.2007)
Published in Molecular cancer therapeutics (01.04.2007)
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Journal Article