Search Results - "Durant, Stephen"

Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates degenerative disease by Tebay, Lauren E., Robertson, Holly, Durant, Stephen T., Vitale, Steven R., Penning, Trevor M., Dinkova-Kostova, Albena T., Hayes, John D.

“…Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) regulates the basal and stress-inducible expression of a battery of genes encoding key components of the…”
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Small molecule inhibitors uncover synthetic genetic interactions of human flap endonuclease 1 (FEN1) with DNA damage response genes by Ward, Thomas A, McHugh, Peter J, Durant, Stephen T

“…Flap endonuclease 1 (FEN1) is a structure selective endonuclease required for proficient DNA replication and the repair of DNA damage. Cellularly active…”
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Arginine methylation regulates the p53 response by Jansson, Martin, Durant, Stephen T., Cho, Er-Chieh, Sheahan, Sharon, Edelmann, Mariola, Kessler, Benedikt, La Thangue, Nicholas B.

“…The tumour suppressor p53 is subject to complex regulation and arginine methylation is now shown to provide an additional level of control. The protein…”
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The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro‑2H‑pyran-4-yl)-1,3-dihydro‑2H‑imidazo[4,5‑c]quinolin-2-one) by Pike, Kurt G, Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Chen, Yingxue, Colclough, Nicola, Davies, Nichola L, de-Almeida, Camila, Degorce, Sebastien L, Didelot, Myriam, Dishington, Allan, Ducray, Richard, Durant, Stephen T, Hassall, Lorraine A, Holmes, Jane, Hughes, Gareth D, MacFaul, Philip A, Mulholland, Keith R, McGuire, Thomas M, Ouvry, Gilles, Pass, Martin, Robb, Graeme, Stratton, Natalie, Wang, Zhenhua, Wilson, Joanne, Zhai, Baochang, Zhao, Kang, Al-Huniti, Nidal

“…ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse…”
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Complete loss of ATM function augments replication catastrophe induced by ATR inhibition and gemcitabine in pancreatic cancer models by Dunlop, Charles R., Wallez, Yann, Johnson, Timothy Isaac, Bernaldo de Quirós Fernández, Sandra, Durant, Stephen T., Cadogan, Elaine B., Lau, Alan, Richards, Frances M., Jodrell, Duncan I.

“…Background Personalised medicine strategies may improve outcomes in pancreatic ductal adenocarcinoma (PDAC), but validation of predictive biomarkers is…”
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ATM-Inhibitor AZD1390 Is a Radiosensitizer for Breast Cancer CNS Metastasis by Tew, Ben Yi, Kalfa, Alex J, Yang, Zeyi, Hurth, Kyle M, Simon, Thomas, Abnoosian, Eric, Durant, Stephen T, Hamerlik, Petra, Salhia, Bodour

“…Limited effective treatments are currently available for central nervous system (CNS) metastasis (CM). This is largely driven by the inability of current…”
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ALT neuroblastoma chemoresistance due to telomere dysfunction-induced ATM activation is reversible with ATM inhibitor AZD0156 by Koneru, Balakrishna, Farooqi, Ahsan, Nguyen, Thinh H, Chen, Wan Hsi, Hindle, Ashly, Eslinger, Cody, Makena, Monish Ram, Burrow, Trevor A, Wilson, Joanne, Smith, Aaron, Pilla Reddy, Venkatesh, Cadogan, Elaine, Durant, Stephen T, Reynolds, C Patrick

“…Cancers overcome replicative immortality by activating either telomerase or an alternative lengthening of telomeres (ALT) mechanism. ALT occurs in ~25% of…”
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Structures of the human poly (ADP-ribose) glycohydrolase catalytic domain confirm catalytic mechanism and explain inhibition by ADP-HPD derivatives by Tucker, Julie A, Bennett, Neil, Brassington, Claire, Durant, Stephen T, Hassall, Giles, Holdgate, Geoff, McAlister, Mark, Nissink, J Willem M, Truman, Caroline, Watson, Martin

“…Poly(ADP-ribose) glycohydrolase (PARG) is the only enzyme known to catalyse hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, thereby reversing…”
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CRISPR metabolic screen identifies ATM and KEAP1 as targetable genetic vulnerabilities in solid tumors by Li, Haojian, Liu, Yue, Xiao, Yunjie, Wilson, Crystal N, Bai, Hui Jen, Jones, Maxwell D, Wang, Shihchun, DeVore, Jennie E, Maier, Esther Y, Durant, Stephen T, Boufraqech, Myriem, Weyemi, Urbain

“…Cancer treatments targeting DNA repair deficiencies often encounter drug resistance, possibly due to alternative metabolic pathways that counteract the most…”
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H2AX promotes replication fork degradation and chemosensitivity in BRCA-deficient tumours by Dibitetto, Diego, Liptay, Martin, Vivalda, Francesca, Dogan, Hülya, Gogola, Ewa, González Fernández, Martín, Duarte, Alexandra, Schmid, Jonas A., Decollogny, Morgane, Francica, Paola, Przetocka, Sara, Durant, Stephen T., Forment, Josep V., Klebic, Ismar, Siffert, Myriam, de Bruijn, Roebi, Kousholt, Arne N., Marti, Nicole A., Dettwiler, Martina, Sørensen, Claus S., Tille, Jean-Christophe, Undurraga, Manuela, Labidi-Galy, Intidhar, Lopes, Massimo, Sartori, Alessandro A., Jonkers, Jos, Rottenberg, Sven

“…Histone H2AX plays a key role in DNA damage signalling in the surrounding regions of DNA double-strand breaks (DSBs). In response to DNA damage, H2AX becomes…”
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ATM kinase inhibitor AZD0156 in combination with irinotecan and 5-fluorouracil in preclinical models of colorectal cancer by Davis, S. Lindsey, Hartman, Sarah J, Bagby, Stacey M, Schlaepfer, Marina, Yacob, Betelehem W, Tse, Tonia, Simmons, Dennis M, Diamond, Jennifer R, Lieu, Christopher H, Leal, Alexis D, Cadogan, Elaine B, Hughes, Gareth D, Durant, Stephen T, Messersmith, Wells A, Pitts, Todd M

“…Abstract Background AZD0156 is an oral inhibitor of ATM, a serine threonine kinase that plays a key role in DNA damage response (DDR) associated with…”
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Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site by Exell, Jack C, Thompson, Mark J, Finger, L David, Shaw, Steven J, Debreczeni, Judit, Ward, Thomas A, McWhirter, Claire, Siöberg, Catrine L B, Molina, Daniel Martinez, Abbott, W Mark, Jones, Clifford D, Nissink, J Willem M, Durant, Stephen T, Grasby, Jane A

“…Structural, enzymatic and cellular target engagement studies reveal the mechanism of action by N -hydroxyurea small molecule inhibitors of the DNA repair…”
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The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one) by Pike, Kurt G, Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Chen, Yingxue, Colclough, Nicola, Davies, Nichola L, de-Almeida, Camila, Degorce, Sebastien L, Didelot, Myriam, Dishington, Allan, Ducray, Richard, Durant, Stephen T, Hassall, Lorraine A, Holmes, Jane, Hughes, Gareth D, MacFaul, Philip A, Mulholland, Keith R, McGuire, Thomas M, Ouvry, Gilles, Pass, Martin, Robb, Graeme, Stratton, Natalie, Wang, Zhenhua, Wilson, Joanne, Zhai, Baochang, Zhao, Kang, Al-Huniti, Nidal

“…ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse…”
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Telomerase-independent paths to immortality in predictable cancer subtypes by Durant, Stephen T

“…The vast majority of cancers commandeer the activity of telomerase - the remarkable enzyme responsible for prolonging cellular lifespan by maintaining the…”
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The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models by Durant, Stephen T, Zheng, Li, Wang, Yingchun, Chen, Kan, Zhang, Lingli, Zhang, Tianwei, Yang, Zhenfan, Riches, Lucy, Trinidad, Antonio G, Fok, Jacqueline H L, Hunt, Tom, Pike, Kurt G, Wilson, Joanne, Smith, Aaron, Colclough, Nicola, Reddy, Venkatesh Pilla, Sykes, Andrew, Janefeldt, Annika, Johnström, Peter, Varnäs, Katarina, Takano, Akihiro, Ling, Stephanie, Orme, Jonathan, Stott, Jonathan, Roberts, Caroline, Barrett, Ian, Jones, Gemma, Roudier, Martine, Pierce, Andrew, Allen, Jasmine, Kahn, Jenna, Sule, Amrita, Karlin, Jeremy, Cronin, Anna, Chapman, Melissa, Valerie, Kristoffer, Illingworth, Ruth, Pass, Martin

“…Poor survival rates of patients with tumors arising from or disseminating into the brain are attributed to an inability to excise all tumor tissue (if…”
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Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390 by Pike, Kurt G., Hunt, Thomas A., Barlaam, Bernard, Benstead, David, Cadogan, Elaine, Chen, Kan, Cook, Calum R., Colclough, Nicola, Deng, Chao, Durant, Stephen T., Eatherton, Andrew, Goldberg, Kristin, Johnström, Peter, Liu, Libin, Liu, Zhaoqun, Nissink, J. Willem M., Pang, Chengling, Pass, Martin, Robb, Graeme R., Roberts, Caroline, Schou, Magnus, Steward, Oliver, Sykes, Andy, Yan, Yumei, Zhai, Baochang, Zheng, Li

“…The inhibition of ataxia-telangiectasia mutated (ATM) has been shown to chemo- and radio-sensitize human glioma cells in vitro and therefore might provide an…”
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Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice by Karlin, Jeremy, Allen, Jasmine, Ahmad, Syed F, Hughes, Gareth, Sheridan, Victoria, Odedra, Rajesh, Farrington, Paul, Cadogan, Elaine B, Riches, Lucy C, Garcia-Trinidad, Antonio, Thomason, Andrew G, Patel, Bhavika, Vincent, Jennifer, Lau, Alan, Pike, Kurt G, Hunt, Thomas A, Sule, Amrita, Valerie, Nicholas C K, Biddlestone-Thorpe, Laura, Kahn, Jenna, Beckta, Jason M, Mukhopadhyay, Nitai, Barlaam, Bernard, Degorce, Sebastien L, Kettle, Jason, Colclough, Nicola, Wilson, Joanne, Smith, Aaron, Barrett, Ian P, Zheng, Li, Zhang, Tianwei, Wang, Yingchun, Chen, Kan, Pass, Martin, Durant, Stephen T, Valerie, Kristoffer

“…Inhibition of ataxia-telangiectasia mutated (ATM) during radiotherapy of glioblastoma multiforme (GBM) may improve tumor control by short-circuiting the…”
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ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks by Balmus, Gabriel, Pilger, Domenic, Coates, Julia, Demir, Mukerrem, Sczaniecka-Clift, Matylda, Barros, Ana C., Woods, Michael, Fu, Beiyuan, Yang, Fengtang, Chen, Elisabeth, Ostermaier, Matthias, Stankovic, Tatjana, Ponstingl, Hannes, Herzog, Mareike, Yusa, Kosuke, Martinez, Francisco Munoz, Durant, Stephen T., Galanty, Yaron, Beli, Petra, Adams, David J., Bradley, Allan, Metzakopian, Emmanouil, Forment, Josep V., Jackson, Stephen P.

“…Mutations in the ATM tumor suppressor gene confer hypersensitivity to DNA-damaging chemotherapeutic agents. To explore genetic resistance mechanisms, we…”
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Development of a high-throughput fluorescence polarization DNA cleavage assay for the identification of FEN1 inhibitors by McWhirter, Claire, Tonge, Michael, Plant, Helen, Hardern, Ian, Nissink, Willem, Durant, Stephen T

“…Flap endonuclease-1 (FEN1) is a highly conserved metallonuclease and is the main human flap endonuclease involved in the recognition and cleavage of…”
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The SET Domain Protein Metnase Mediates Foreign DNA Integration and Links Integration to Nonhomologous End-Joining Repair by Lee, Suk-Hee, Masahiko Oshige, Stephen T. Durant, Kanwaldeep Kaur Rasila, Williamson, Elizabeth A., Ramsey, Heather, Lori Kwan, Nickoloff, Jac A., Robert Hrornas

“…The molecular mechanism by which foreign DNA integrates into the human genome is poorly understood yet critical to many disease processes, including retroviral…”
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