Search Results - "Bellenie, Benjamin"

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders by 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

“…Deregulation of the transcriptional repressor BCL6 enables tumorigenesis of germinal center B-cells, and hence BCL6 has been proposed as a therapeutic target…”
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Determination of Ligand-Binding Affinity (K d) Using Transverse Relaxation Rate (R 2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery by Liu, Manjuan, Mirza, Amin, McAndrew, P. Craig, Thapaliya, Arjun, Pierrat, Olivier A., Stubbs, Mark, Hahner, Tamas, Chessum, Nicola E. A., Innocenti, Paolo, Caldwell, John, Cheeseman, Matthew D., Bellenie, Benjamin R., van Montfort, Rob L. M., Newton, Gary K., Burke, Rosemary, Collins, Ian, Hoelder, Swen

“…High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no…”
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Degradation by Design: New Cyclin K Degraders from Old CDK Inhibitors by Thomas, Katie L., Bouguenina, Habib, Miller, Daniel S. J., Sialana, Fernando J., Hayhow, Thomas G., Choudhary, Jyoti S., Rossanese, Olivia W., Bellenie, Benjamin R.

“…Small molecules that induce protein degradation hold the potential to overcome several limitations of the currently available inhibitors. Monovalent or…”
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Determination of Ligand-Binding Affinity ( K d ) Using Transverse Relaxation Rate ( R 2 ) in the Ligand-Observed 1 H NMR Experiment and Applications to Fragment-Based Drug Discovery by Liu, Manjuan, Mirza, Amin, McAndrew, P Craig, Thapaliya, Arjun, Pierrat, Olivier A, Stubbs, Mark, Hahner, Tamas, Chessum, Nicola E A, Innocenti, Paolo, Caldwell, John, Cheeseman, Matthew D, Bellenie, Benjamin R, van Montfort, Rob L M, Newton, Gary K, Burke, Rosemary, Collins, Ian, Hoelder, Swen

“…High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no…”
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Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ by Bellenie, Benjamin R, Hall, Edward, Bruce, Ian, Spendiff, Matthew, Culshaw, Andrew, McDonald, Sarah, Ambarkhane, Ameet, Chinn, Colin, Thomas, Matthew, Rosner, Elisabeth, Bracher, Marguerite, Nicklin, Paul, Marshall, Stephen, Coote, Julie, Cullen, Eva, Tessier, Clemence, Wuersch, Kuno, Lal, Ajay, Wallis, Gillian, Hollingworth, Gregory J, Neef, James

“…Using a novel physiologically relevant in vitro human whole blood neutrophil shape change assay, an aminopyrazine series of selective PI3Kγ inhibitors was…”
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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays by 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.

“…By suppressing gene transcription through the recruitment of corepressor proteins, B-cell lymphoma 6 (BCL6) protein controls a transcriptional network required…”
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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors by Davis, Owen A., Cheung, Kwai-Ming J., Brennan, Alfie, Lloyd, Matthew G., Rodrigues, Matthew J., Pierrat, Olivier A., Collie, Gavin W., Le Bihan, Yann-Vaï, Huckvale, Rosemary, Harnden, Alice C., Varela, Ana, Bright, Michael D., Eve, Paul, Hayes, Angela, Henley, Alan T., Carter, Michael D., McAndrew, P. Craig, Talbot, Rachel, Burke, Rosemary, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Meniconi, Mirco, Bellenie, Benjamin R., Hoelder, Swen

“…To identify new chemical series with enhanced binding affinity to the BTB domain of B-cell lymphoma 6 protein, we targeted a subpocket adjacent to Val18. With…”
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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket by 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

“…We describe the optimization of modestly active starting points to potent inhibitors of BCL6 by growing into a subpocket, which was occupied by a network of…”
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Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones by 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

“…B-cell lymphoma 6 (BCL6) is a transcriptional repressor and oncogenic driver of diffuse large B-cell lymphoma (DLBCL). Here, we report the optimization of our…”
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Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo by 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

“…The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our…”
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Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design by Bellenie, Benjamin R., Barton, Nicholas P., Emmons, Amanda J., Heer, Jag P., Salvagno, Cristian

“…A novel oxytocin antagonist was identified by ‘scaffold-hopping’ using Cresset FieldScreen molecular field similarity searching. A single cycle of optimization…”
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Theoretical Study on the Selectivity of Asymmetric Sulfur Ylide Epoxidation Reaction by Silva, María A, Bellenie, Benjamin R, Goodman, Jonathan M

“…We report the first theoretical studies on the asymmetric sulfonium ylide epoxidation reaction using a chiral sulfide that successfully reproduces the…”
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Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist by Barton, Nicholas P., Bellenie, Benjamin R., Doran, Andrew T., Emmons, Amanda J., Heer, Jag P., Salvagno, Cristian M.

“…The optimisation of a tertiary sulfonamide high-throughput screening hit is described. A combination of high-throughput chemistry, pharmacophore analysis and…”
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Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor by Witherington, Jason, Abberley, Lee, Bellenie, Benjamin R., Boatman, Rio, Collis, Katharine, Dean, David K., Gaiba, Alessandra, Paul King, N., Shuker, Nicola, Steadman, Jon G.A., Takle, Andrew K., Sanger, Gareth, Butler, Sharon, McKay, Fiona, Muir, Alison, Winborn, Kim, Ward, Robert W., Heightman, Tom D.

“…As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent…”
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Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain‑4 (BRD4) by Tuning Kinase Selectivity by Watts, Ellen, Heidenreich, David, Tucker, Elizabeth, Raab, Monika, Strebhardt, Klaus, Chesler, Louis, Knapp, Stefan, Bellenie, Benjamin, Hoelder, Swen

“…Concomitant inhibition of anaplastic lymphoma kinase (ALK) and bromodomain-4 (BRD4) is a potential therapeutic strategy for targeting two key oncogenic drivers…”
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The stereochemistry of glabrescol by Bellenie, Benjamin R, Goodman, Jonathan M

“…The structure of glabrescol has been proposed and revised. Could the revised structure have been predicted without the need for total synthesis? Molecular…”
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A highly enantioselective one-pot sulfur ylide epoxidation reaction by Winn, Caroline L., Bellenie, Benjamin R., Goodman, Jonathan M.

“…Enantiomerically pure tricyclic C 2-symmetric sulfide 1 can be prepared in high yield and only three steps from d-mannitol. When used in a one-pot sulfur ylide…”
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The Chemical Probes Portal – 2024: update on this public resource to support best-practice selection and use of small molecules in biomedical research by Sanfelice, Domenico, Antolin, Albert A, Crisp, Alisa, Chen, Yi, Bellenie, Benjamin, Brennan, Paul E, Edwards, Aled, Müller, Susanne, Al-Lazikani, Bissan, Workman, Paul

“…The Chemical Probes Portal (www.chemicalprobes.org) is a free, public resource, based on expert-reviews, that supports the assessment, selection and use of…”
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A RIPK1-specific PROTAC degrader achieves potent antitumor activity by enhancing immunogenic cell death by Mannion, Jonathan, Gifford, Valentina, Bellenie, Benjamin, Fernando, Winnie, Ramos Garcia, Laura, Wilson, Rebecca, John, Sidonie Wicky, Udainiya, Savita, Patin, Emmanuel C, Tiu, Crescens, Smith, Angel, Goicoechea, Maria, Craxton, Andrew, Moraes de Vasconcelos, Nathalia, Guppy, Naomi, Cheung, Kwai-Ming J, Cundy, Nicholas J, Pierrat, Olivier, Brennan, Alfie, Roumeliotis, Theodoros I, Benstead-Hume, Graeme, Alexander, John, Muirhead, Gareth, Layzell, Scott, Lyu, Wenxin, Roulstone, Victoria, Allen, Mark, Baldock, Holly, Legrand, Arnaud, Gabel, Florian, Serrano-Aparicio, Natalia, Starling, Chris, Guo, Hongyan, Upton, Jason, Gyrd-Hansen, Mads, MacFarlane, Marion, Seddon, Benedict, Raynaud, Florence, Roxanis, Ioannis, Harrington, Kevin, Haider, Syed, Choudhary, Jyoti S, Hoelder, Swen, Tenev, Tencho, Meier, Pascal

“…Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) functions as a critical stress sentinel that coordinates cell survival, inflammation, and…”
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Abstract 3879: SETD2 is a novel and druggable dependency in IMiD/CELMoD resistant multiple myeloma models by Bird, Sarah Anne, Licciardello, Marco, Chrisochoidou, Yakinthi, Smith, James, Barber, Amy, Cheung, Jack, Grabovska, Yura, Martin, Shannon, Sialana, Fernando, Che, Harvey, Bouguenina, Habib, Bellenie, Benjamin, Walker, Brian, Clarke, Paul, Pawlyn, Charlotte

“…Immunomodulatory agents (IMiDs) and cereblon E3 ligase modulators (CELMoDs) are a cornerstone of Multiple Myeloma (MM) treatment. They bind to the cereblon…”
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