Search Results - "Saville, Harry"

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers by Anderhub, Simon J, Mak, Grace Wing-Yan, Gurden, Mark D, Faisal, Amir, Drosopoulos, Konstantinos, Walsh, Katie, Woodward, Hannah L, Innocenti, Paolo, Westwood, Isaac M, Naud, Sébastien, Hayes, Angela, Theofani, Efthymia, Filosto, Simone, Saville, Harry, Burke, Rosemary, van Montfort, Rob L M, Raynaud, Florence I, Blagg, Julian, Hoelder, Swen, Eccles, Suzanne A, Linardopoulos, Spiros

“…BOS172722 (CCT289346) is a highly potent, selective, and orally bioavailable inhibitor of spindle assembly checkpoint kinase MPS1. BOS172722 treatment alone…”
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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays by Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios

“…Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted…”
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The effects of adaptive working memory training and mindfulness meditation training on processing efficiency and worry in high worriers by Course-Choi, Jenna, Saville, Harry, Derakshan, Nazanin

“…Worry is the principle characteristic of generalised anxiety disorder, and has been linked to deficient attentional control, a main function of working memory…”
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SF3B1 hotspot mutations confer sensitivity to PARP inhibition by eliciting a defective replication stress response by Bland, Philip, Saville, Harry, Wai, Patty T., Curnow, Lucinda, Muirhead, Gareth, Nieminuszczy, Jadwiga, Ravindran, Nivedita, John, Marie Beatrix, Hedayat, Somaieh, Barker, Holly E., Wright, James, Yu, Lu, Mavrommati, Ioanna, Read, Abigail, Peck, Barrie, Allen, Mark, Gazinska, Patrycja, Pemberton, Helen N., Gulati, Aditi, Nash, Sarah, Noor, Farzana, Guppy, Naomi, Roxanis, Ioannis, Pratt, Guy, Oldreive, Ceri, Stankovic, Tatjana, Barlow, Samantha, Kalirai, Helen, Coupland, Sarah E., Broderick, Ronan, Alsafadi, Samar, Houy, Alexandre, Stern, Marc-Henri, Pettit, Stephen, Choudhary, Jyoti S., Haider, Syed, Niedzwiedz, Wojciech, Lord, Christopher J., Natrajan, Rachael

“…SF3B1 hotspot mutations are associated with a poor prognosis in several tumor types and lead to global disruption of canonical splicing. Through synthetic…”
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Discovery of 2‑(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes by Saint-Dizier, François, Matthews, Thomas P., Gregson, Aaron M., Prevet, Hugues, McHardy, Tatiana, Colombano, Giampiero, Saville, Harry, Rowlands, Martin, Ewens, Caroline, McAndrew, P. Craig, Tomlin, Kathy, Guillotin, Delphine, Mak, Grace Wing-Yan, Drosopoulos, Konstantinos, Poursaitidis, Ioannis, Burke, Rosemary, van Montfort, Rob, Linardopoulos, Spiros, Collins, Ian

“…The existence of multiple centrosomes in some cancer cells can lead to cell death through the formation of multipolar mitotic spindles and consequent aberrant…”
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Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease by Colombano, Giampiero, Caldwell, John J, Matthews, Thomas P, Bhatia, Chitra, Joshi, Amar, McHardy, Tatiana, Mok, Ngai Yi, Newbatt, Yvette, Pickard, Lisa, Strover, Jade, Hedayat, Somaieh, Walton, Michael I, Myers, Stephanie M, Jones, Alan M, Saville, Harry, McAndrew, Craig, Burke, Rosemary, Eccles, Suzanne A, Davies, Faith E, Bayliss, Richard, Collins, Ian

“…A series of imidazo­[1,2-b]­pyridazin-8-amine kinase inhibitors were discovered to allosterically inhibit the endoribonuclease function of the dual…”
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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) by 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

“…Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an…”
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Rapid Discovery of Pyrido[3,4‑d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach by Innocenti, Paolo, Woodward, Hannah L, Solanki, Savade, Naud, Sébastien, Westwood, Isaac M, Cronin, Nora, Hayes, Angela, Roberts, Jennie, Henley, Alan T, Baker, Ross, Faisal, Amir, Mak, Grace Wing-Yan, Box, Gary, Valenti, Melanie, De Haven Brandon, Alexis, O’Fee, Lisa, Saville, Harry, Schmitt, Jessica, Matijssen, Berry, Burke, Rosemary, van Montfort, Rob L. M, Raynaud, Florence I, Eccles, Suzanne A, Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen

“…Monopolar spindle 1 (MPS1) plays a central role in the transition of cells from metaphase to anaphase and is one of the main components of the spindle assembly…”
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Abstract 1651: In vitro and in vivo profile of the preclinical candidate and MPS1 kinase inhibitor CCT289346 by Woodward, Hannah, Innocenti, Paolo, Cheung, Kwai-Ming J., Naud, Sébastien, Faisal, Amir, Mak, Grace W., Hayes, Angela, O'Fee, Lisa, Saville, Harry, Brandon, Alexis De Haven, Roberts, Jennie, Box, Gary, Valenti, Melanie, Heneley, Alan T., Walsh, Katie, Burke, Rosemary, Eccles, Suzanne A., Raynaud, Florence I., Montfort, Rob L. van, Blagg, Julian, Linardopoulos, Spiros, Hoelder, Swen

“…Abstract The mitotic kinase MPS1 (also known as TTK) is one of the main components of the spindle assembly checkpoint. MPS1 is required for chromosome…”
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Abstract 4036: Induction of detrimental aneuploidy in basal breast cancer cells treated by MPS1 inhibitors in combination with paclitaxel by Anderhub, Simon J., Mak, Grace WY, Faisal, Amir, Walsh, Katie, Gurden, Mark, Day, Liz, Innocenti, Paolo, Woodward, Hannah L., Westwood, Isaac M., Cheung, Kwai-Ming J., Naud, Sebastien, Hayes, Angela, Box, Gary, Brandon, Alexis de Haven, Valenti, Melanie R., O’Fee, Lisa, Saville, Harry, Burke, Rosemary, Montfort, Rob LM van, Raynaud, Florence I., Eccles, Suzanne A., Blagg, Julian, Hoelder, Swen, Linardopoulos, Spiros

“…Abstract Basal-like breast cancer has received considerable attention in recent years, but despite all efforts, conventional chemotherapy remains the main…”
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Abstract 193: Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidate by Woodward, Hannah L., Innocenti, Paolo, Cheung, Kwai-Ming J., Naud, Sébastien, Hayes, Angela, Henley, Alan T., Faisal, Amir, Mak, Grace, Box, Gary, Westwood, Isaac M., Carter, Michael, Valenti, Melanie, Brandon, Alexis De Haven, O’Fee, Lisa, Saville, Harry, Burke, Rosemary, Montfort, Rob van, Raynaud, Florence, Eccles, Suzanne A., Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen

“…Abstract MPS1 (also known as TTK), is a dual-specificity protein kinase and one of the main components of the spindle assembly checkpoint. Cancer cells heavily…”
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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-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722) by 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

“…Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an…”
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Abstract P6-10-05: Mutations in the RNA Splicing Factor SF3B1 drive endocrine therapy resistance and confer a targetable replication stress response defect through PARP inhibition by Bland, Phil, Saville, Harry, Read, Abigail, Wai, Patty, Muirhead, Gareth, Curnow, Lucinda, Nieminuszczy, Jadwiga, Ravindran, Nivedita, John, Marie, Hedayat, Somaieh, Barker, Holly, Wright, James, Yu, Lu, Mavrommati, Ioanna, Peck, Barrie, Allen, Mark, Gazinska, Patrycja, Pemberton, Helen, Gulati, Aditi, Nash, Sarah, Noor, Farzana, Guppy, Naomi, Roxanis, Ioannis, Barlow, Samantha, Kalirai, Helen, Coupland, Sarah, Broderick, Ronan, Alsafadi, Samar, Houy, Alexandre, Stern, Marc-Henri, Pettit, Stephen, Choudhary, Jyoti, Haider, Syed, Niedzwiedz, Wojciech, Lord, Christopher, Natrajan, Rachael

“…Abstract Background: Heterozygous hotspot mutations in the RNA splicing factor SF3B1, occur in 3% of unselected breast cancers and are associated with…”
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