Search Results - "Walton, Michael I"

Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor by Whittaker, Steven R., Barlow, Clare, Martin, Mathew P., Mancusi, Caterina, Wagner, Steve, Self, Annette, Barrie, Elaine, Te Poele, Robert, Sharp, Swee, Brown, Nathan, Wilson, Stuart, Jackson, Wayne, Fischer, Peter M., Clarke, Paul A., Walton, Michael I., McDonald, Edward, Blagg, Julian, Noble, Martin, Garrett, Michelle D., Workman, Paul

“…Deregulation of the cyclin‐dependent kinases (CDKs) has been implicated in the pathogenesis of multiple cancer types. Consequently, CDKs have garnered intense…”
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The Cyclin-Dependent Kinase Inhibitor Seliciclib (R-roscovitine; CYC202) Decreases the Expression of Mitotic Control Genes and Prevents Entry into Mitosis by Whittaker, Steven R., te Poele, Robert H., Chan, Florence, Linardopoulos, Spiros, Walton, Michael I., Garrett, Michelle D., Workman, Paul

“…The cyclin-dependent kinase (CDK) inhibitor seliciclib (R-roscovitine, CYC202) shows promising antitumor activity in preclinical models and is currently…”
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In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine and CYC202 by RAYNAUD, Florence I, WHITTAKER, Steven R, VALENTI, Melanie, BRUNTON, Lisa, ECCLES, Suzanne, LANE, David P, WORKMAN, Paul, FISCHER, Peter M, MCCLUE, Steven, WALTON, Michael I, BARRIE, S. Elaine, GARRETT, Michelle D, ROGERS, Paul, CLARKE, Simon J, KELLAND, Lloyd R

“…Purpose: To investigate pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine,…”
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CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA Polymerase Function in Human Lung and Colorectal Cancer Cells by Rogers, Rebecca F, Walton, Michael I, Cherry, Daniel L, Collins, Ian, Clarke, Paul A, Garrett, Michelle D, Workman, Paul

“…Checkpoint kinase 1 (CHK1) is a key mediator of the DNA damage response that regulates cell-cycle progression, DNA damage repair, and DNA replication…”
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DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer by Kanu, Nnennaya, Cerone, Maria Antonietta, Goh, Gerald, Zalmas, Lykourgos-Panagiotis, Bartkova, Jirina, Dietzen, Michelle, McGranahan, Nicholas, Rogers, Rebecca, Law, Emily K, Gromova, Irina, Kschischo, Maik, Walton, Michael I, Rossanese, Olivia W, Bartek, Jiri, Harris, Reuben S, Venkatesan, Subramanian, Swanton, Charles

“…The APOBEC3 family of cytidine deaminases mutate the cancer genome in a range of cancer types. Although many studies have documented the downstream effects of…”
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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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CCT241533 Is a Potent and Selective Inhibitor of CHK2 that Potentiates the Cytotoxicity of PARP Inhibitors by ANDERSON, Victoria E, WALTON, Michael I, GARRETT, Michelle D, EVE, Paul D, BOXALL, Katherine J, ANTONI, Laurent, CALDWELL, John J, AHERNE, Wynne, PEARL, Laurence H, OLIVER, Antony W, COLLINS, Ian

“…CHK2 is a checkpoint kinase involved in the ATM-mediated response to double-strand DNA breaks. Its potential as a drug target is still unclear, but inhibitors…”
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Disruption of WT1 gene expression and exon 5 splicing following cytotoxic drug treatment: Antisense down-regulation of exon 5 alters target gene expression and inhibits cell survival by Renshaw, Jane, Orr, Rosanne M, Walton, Michael I, Te Poele, Robert, Williams, Richard D, Wancewicz, Edward V, Monia, Brett P, Workman, Paul, Pritchard-Jones, Kathryn

“…Deregulated expression of the Wilms' tumor gene ( WT1 ) has been implicated in the maintenance of a malignant phenotype in leukemias and a wide range of solid…”
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Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)‑5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737) by Osborne, James D, Matthews, Thomas P, McHardy, Tatiana, Proisy, Nicolas, Cheung, Kwai-Ming J, Lainchbury, Michael, Brown, Nathan, Walton, Michael I, Eve, Paul D, Boxall, Katherine J, Hayes, Angela, Henley, Alan T, Valenti, Melanie R, De Haven Brandon, Alexis K, Box, Gary, Jamin, Yann, Robinson, Simon P, Westwood, Isaac M, van Montfort, Rob L. M, Leonard, Philip M, Lamers, Marieke B. A. C, Reader, John C, Aherne, G. Wynne, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian

“…Multiparameter optimization of a series of 5-((4-aminopyridin-2-yl)­amino)­pyrazine-2-carbonitriles resulted in the identification of a potent and selective…”
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The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106 by Walton, Michael I, Eve, Paul D, Hayes, Angela, Valenti, Melanie, De Haven Brandon, Alexis, Box, Gary, Boxall, Kathy J, Aherne, G Wynne, Eccles, Suzanne A, Raynaud, Florence I, Williams, David H, Reader, John C, Collins, Ian, Garrett, Michelle D

“…Genotoxic antitumor agents continue to be the mainstay of current cancer chemotherapy. These drugs cause DNA damage and activate numerous cell cycle…”
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Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing by 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

“…Pyrazolopyridine inhibitors with low micromolar potency for CHK1 and good selectivity against CHK2 were previously identified by fragment-based screening. The…”
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Discovery of 3‑Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors by Lainchbury, Michael, Matthews, Thomas P, McHardy, Tatiana, Boxall, Kathy J, Walton, Michael I, Eve, Paul D, Hayes, Angela, Valenti, Melanie R, de Haven Brandon, Alexis K, Box, Gary, Aherne, G. Wynne, Reader, John C, Raynaud, Florence I, Eccles, Suzanne A, Garrett, Michelle D, Collins, Ian

“…Inhibitors of checkpoint kinase 1 (CHK1) are of current interest as potential antitumor agents, but the most advanced inhibitor series reported to date are not…”
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Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening by Matthews, Thomas P, Klair, Suki, Burns, Samantha, Boxall, Kathy, Cherry, Michael, Fisher, Martin, Westwood, Isaac M, Walton, Michael I, McHardy, Tatiana, Cheung, Kwai-Ming J, Van Montfort, Rob, Williams, David, Aherne, G. Wynne, Garrett, Michelle D, Reader, John, Collins, Ian

“…Checkpoint kinase 1 (CHK1) is an oncology target of significant current interest. Inhibition of CHK1 abrogates DNA damage-induced cell cycle checkpoints and…”
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Molecular profiling and combinatorial activity of CCT 068127: a potent CDK 2 and CDK 9 inhibitor by Whittaker, Steven R., Barlow, Clare, Martin, Mathew P., Mancusi, Caterina, Wagner, Steve, Self, Annette, Barrie, Elaine, Te Poele, Robert, Sharp, Swee, Brown, Nathan, Wilson, Stuart, Jackson, Wayne, Fischer, Peter M., Clarke, Paul A., Walton, Michael I., McDonald, Edward, Blagg, Julian, Noble, Martin, Garrett, Michelle D., Workman, Paul

“…Deregulation of the cyclin‐dependent kinases ( CDK s) has been implicated in the pathogenesis of multiple cancer types. Consequently, CDK s have garnered…”
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Effect of p53 status on sensitivity to platinum complexes in a human ovarian cancer cell line by Pestell, K E, Hobbs, S M, Titley, J C, Kelland, L R, Walton, M I

“…Wild-type p53 is frequently mutated in late-stage ovarian cancer and has been proposed as a determinant of cisplatin chemosensitivity. We have therefore…”
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Assays for HSP90 and inhibitors by Aherne, Wynne, Maloney, Alison, Prodromou, Chris, Rowlands, Martin G, Hardcastle, Anthea, Boxall, Katherine, Clarke, Paul, Walton, Michael I, Pearl, Laurence, Workman, Paul

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Pilot study of nimorazole as a hypoxic-cell sensitizer with the "chart" regimen in head and neck cancer by Cottrill, C P, Bishop, K, Walton, M I, Henk, J M

“…A potential disadvantage of accelerated fractionation in radiotherapy is the lack of time for reoxygenation, so that hypoxia becomes a more potent cause of…”
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Abstract 4447: Generation of an acquired resistance model to the novel AKT inhibitor CCT129254 by Akan, Denis T., Walton, Michael I., Garrett, Michelle D.

“…Abstract The PI3K/AKT pathway is a key driver of cell growth, proliferation and survival, and deregulation at many levels of the pathway is observed in…”
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Decreased NADPH:cytochrome P-450 reductase activity and impaired drug activation in a mammalian cell line resistant to mitomycin C under aerobic but not hypoxic conditions by Hoban, P R, Walton, M I, Robson, C N, Godden, J, Stratford, I J, Workman, P, Harris, A L, Hickson, I D

“…Mitomycin C (MMC) is regarded as the prototype bioreductive alkylating agent in clinical use. To elucidate the biochemical basis of MMC resistance, we isolated…”
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CCT241533 is a potent and selective inhibitor of CHK2 which potentiates the cytotoxicity of PARP inhibitors by Anderson, Victoria E, Walton, Michael I, Eve, Paul D, Boxall, Katherine J, Antoni, Laurent, Caldwell, John J, Pearl, Laurence H, Oliver, Antony W, Collins, Ian, Garrett, Michelle D

“…CHK2 is a checkpoint kinase involved in the ATM-mediated response to double strand DNA breaks. Its potential as a drug target is still unclear but inhibitors…”
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