Search Results - "ALISON, J. A"

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery by Davies, Thomas G, Wixted, William E, Coyle, Joseph E, Griffiths-Jones, Charlotte, Hearn, Keisha, McMenamin, Rachel, Norton, David, Rich, Sharna J, Richardson, Caroline, Saxty, Gordon, Willems, Henriëtte M. G, Woolford, Alison J.-A, Cottom, Joshua E, Kou, Jen-Pyng, Yonchuk, John G, Feldser, Heidi G, Sanchez, Yolanda, Foley, Joseph P, Bolognese, Brian J, Logan, Gregory, Podolin, Patricia L, Yan, Hongxing, Callahan, James F, Heightman, Tom D, Kerns, Jeffrey K

“…KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress…”
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Design and Synthesis of 56 Shape‐Diverse 3D Fragments by Downes, Thomas D., Jones, S. Paul, Klein, Hanna F., Wheldon, Mary C., Atobe, Masakazu, Bond, Paul S., Firth, James D., Chan, Ngai S., Waddelove, Laura, Hubbard, Roderick E., Blakemore, David C., De Fusco, Claudia, Roughley, Stephen D., Vidler, Lewis R., Whatton, Maria Ann, Woolford, Alison J.‐A., Wrigley, Gail L., O'Brien, Peter

“…Fragment‐based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often…”
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Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction by Heightman, Tom D, Callahan, James F, Chiarparin, Elisabetta, Coyle, Joseph E, Griffiths-Jones, Charlotte, Lakdawala, Ami S, McMenamin, Rachel, Mortenson, Paul N, Norton, David, Peakman, Torren M, Rich, Sharna J, Richardson, Caroline, Rumsey, William L, Sanchez, Yolanda, Saxty, Gordon, Willems, Henriëtte M. G, Wolfe, Lawrence, Woolford, Alison J.-A, Wu, Zining, Yan, Hongxing, Kerns, Jeffrey K, Davies, Thomas G

“…The KEAP1–NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be…”
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Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP by Chessari, Gianni, Buck, Ildiko M, Day, James E. H, Day, Philip J, Iqbal, Aman, Johnson, Christopher N, Lewis, Edward J, Martins, Vanessa, Miller, Darcey, Reader, Michael, Rees, David C, Rich, Sharna J, Tamanini, Emiliano, Vitorino, Marc, Ward, George A, Williams, Pamela A, Williams, Glyn, Wilsher, Nicola E, Woolford, Alison J.-A

“…Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with…”
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Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency by Murray, Christopher W, Carr, Maria G, Callaghan, Owen, Chessari, Gianni, Congreve, Miles, Cowan, Suzanna, Coyle, Joseph E, Downham, Robert, Figueroa, Eva, Frederickson, Martyn, Graham, Brent, McMenamin, Rachel, O’Brien, M. Alistair, Patel, Sahil, Phillips, Theresa R, Williams, Glyn, Woodhead, Andrew J, Woolford, Alison J.-A

“…Inhibitors of the chaperone Hsp90 are potentially useful as chemotherapeutic agents in cancer. This paper describes an application of fragment screening to…”
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Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design by Woodhead, Andrew J, Angove, Hayley, Carr, Maria G, Chessari, Gianni, Congreve, Miles, Coyle, Joseph E, Cosme, Jose, Graham, Brent, Day, Philip J, Downham, Robert, Fazal, Lynsey, Feltell, Ruth, Figueroa, Eva, Frederickson, Martyn, Lewis, Jonathan, McMenamin, Rachel, Murray, Christopher W, O’Brien, M. Alistair, Parra, Lina, Patel, Sahil, Phillips, Theresa, Rees, David C, Rich, Sharna, Smith, Donna-Michelle, Trewartha, Gary, Vinkovic, Mladen, Williams, Brian, Woolford, Alison J.-A

“…Inhibitors of the molecular chaperone heat shock protein 90 (Hsp90) are currently generating significant interest in clinical development as potential…”
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Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2 by Heightman, Tom D, Berdini, Valerio, Braithwaite, Hannah, Buck, Ildiko M, Cassidy, Megan, Castro, Juan, Courtin, Aurélie, Day, James E. H, East, Charlotte, Fazal, Lynsey, Graham, Brent, Griffiths-Jones, Charlotte M, Lyons, John F, Martins, Vanessa, Muench, Sandra, Munck, Joanne M, Norton, David, O’Reilly, Marc, Palmer, Nick, Pathuri, Puja, Reader, Michael, Rees, David C, Rich, Sharna J, Richardson, Caroline, Saini, Harpreet, Thompson, Neil T, Wallis, Nicola G, Walton, Hugh, Wilsher, Nicola E, Woolford, Alison J.-A, Cooke, Michael, Cousin, David, Onions, Stuart, Shannon, Jonathan, Watts, John, Murray, Christopher W

“…Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of…”
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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction by Norton, David, Bonnette, William G, Callahan, James F, Carr, Maria G, Griffiths-Jones, Charlotte M, Heightman, Tom D, Kerns, Jeffrey K, Nie, Hong, Rich, Sharna J, Richardson, Caroline, Rumsey, William, Sanchez, Yolanda, Verdonk, Marcel L, Willems, Henriëtte M. G, Wixted, William E, Woolford, Alison J.-A, Wu, Zining, Davies, Thomas G

“…The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this…”
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Maintaining benefits following pulmonary rehabilitation: a randomised controlled trial by Spencer, L. M, Alison, J. A, McKeough, Z. J

“…The aim of this study was to determine if weekly, supervised, outpatient-based exercise plus unsupervised home exercise following an 8-week pulmonary…”
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Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design by Wyatt, Paul G, Woodhead, Andrew J, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Davis, Deborah J, Devine, Lindsay A, Early, Theresa R, Feltell, Ruth E, Lewis, E. Jonathan, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Reule, Matthias, Saxty, Gordon, Seavers, Lisa C. A, Smith, Donna-Michelle, Squires, Matt S, Trewartha, Gary, Walker, Margaret T, Woolford, Alison J.-A

“…The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small…”
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Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor by Tamanini, Emiliano, Miyamura, Shin, Buck, Ildiko M., Cons, Benjamin D., Dawson, Lee, East, Charlotte, Futamura, Takashi, Goto, Shintaro, Griffiths-Jones, Charlotte, Hashimoto, Tetsuya, Heightman, Tom D., Ishikawa, Shunpei, Ito, Hideki, Kaneko, Yosuke, Kawato, Tatsuya, Kondo, Kazumi, Kurihara, Naoki, McCarthy, James M., Mori, Yukiko, Nagase, Tsuyoshi, Nakaishi, Yuichiro, Reeks, Judith, Sato, Akimasa, Schöpf, Patrick, Tai, Kuninori, Tamai, Taichi, Tisi, Dominic, Woolford, Alison J.-A.

“…Fragment-based ligand discovery was successfully applied to histone deacetylase HDAC2. In addition to the anticipated hydroxamic acid- and benzamide-based…”
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Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) by Woolford, Alison J.-A, Day, Philip J, Bénéton, Véronique, Berdini, Valerio, Coyle, Joseph E, Dudit, Yann, Grondin, Pascal, Huet, Pascal, Lee, Lydia Y. W, Manas, Eric S, McMenamin, Rachel L, Murray, Christopher W, Page, Lee W, Patel, Vipulkumar K, Potvain, Florent, Rich, Sharna J, Sang, Yingxia, Somers, Don O, Trottet, Lionel, Wan, Zehong, Zhang, Xiaomin

“…Lp-PLA2 has been explored as a target for a number of inflammation associated diseases, including cardiovascular disease and dementia. This article describes…”
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Physiological effects of vibration in subjects with cystic fibrosis by McCarren, B, Alison, J. A

“…The physiological mechanisms by which vibration and other physiotherapy interventions may clear secretions in subjects with cystic fibrosis are unknown. The…”
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Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X‑ray Fragment Screening by Woolford, Alison J.-A, Pero, Joseph E, Aravapalli, Sridhar, Berdini, Valerio, Coyle, Joseph E, Day, Philip J, Dodson, Andrew M, Grondin, Pascal, Holding, Finn P, Lee, Lydia Y. W, Li, Peng, Manas, Eric S, Marino, Joseph, Martin, Agnes C. L, McCleland, Brent W, McMenamin, Rachel L, Murray, Christopher W, Neipp, Christopher E, Page, Lee W, Patel, Vipulkumar K, Potvain, Florent, Rich, Sharna, Rivero, Ralph A, Smith, Kirsten, Somers, Donald O, Trottet, Lionel, Velagaleti, Ranganadh, Williams, Glyn, Xie, Ren

“…Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA2) are associated with cardiovascular disease and dementia. A fragment screen was…”
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Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates by Jones, S. Paul, Firth, James D, Wheldon, Mary C, Atobe, Masakazu, Hubbard, Roderick E, Blakemore, David C, De Fusco, Claudia, Lucas, Simon C. C, Roughley, Stephen D, Vidler, Lewis R, Whatton, Maria Ann, Woolford, Alison J.-A, Wrigley, Gail L, O'Brien, Peter

“…Fragment-based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often…”
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Six-minute walk test as an outcome measure: are two six-minute walk tests necessary immediately after pulmonary rehabilitation and at three-month follow-up? by Spencer, Lissa M, Alison, J A, McKeough, Z J

“…A 3-mo prospective, longitudinal, repeated-measures study was undertaken in subjects with chronic obstructive pulmonary disease (COPD). The study aimed to…”
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Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors by Cho, Young Shin, Angove, Hayley, Brain, Christopher, Chen, Christine Hiu-Tung, Cheng, Hong, Cheng, Robert, Chopra, Rajiv, Chung, Kristy, Congreve, Miles, Dagostin, Claudio, Davis, Deborah J, Feltell, Ruth, Giraldes, John, Hiscock, Steven D, Kim, Sunkyu, Kovats, Steven, Lagu, Bharat, Lewry, Kim, Loo, Alice, Lu, Yipin, Luzzio, Michael, Maniara, Wiesia, McMenamin, Rachel, Mortenson, Paul N, Benning, Rajdeep, O'Reilly, Marc, Rees, David C, Shen, Junqing, Smith, Troy, Wang, Yaping, Williams, Glyn, Woolford, Alison J.-A, Wrona, Wojciech, Xu, Mei, Yang, Fan, Howard, Steven

“…Herein, we describe the discovery of potent and highly selective inhibitors of both CDK4 and CDK6 via structure-guided optimization of a fragment-based…”
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Handgrip strength: potential of a simple test to aid management in chronic obstructive pulmonary disease by Alison, J. A.

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High- and low-level pressure support during walking in people with severe kyphoscoliosis by MENADUE, C, ALISON, J. A, PIPER, A. J, WONG, K. K, HOLLIER, C, ELLIS, E. R

“…To determine whether the level of pressure support (PS) provided during exercise influences endurance time in people with severe kyphoscoliosis, a double-blind…”
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Synthesis of the thapsigargins by Ley, S.V, Antonello, A, Balskus, E.P, Booth, D.T, Christensen, S.B, Cleator, E, Gold, H, Hogenauer, K, Hunger, U, Myers, R.M

“…The thapsigargins are a family of complex guaianolides with potent and selective Ca2+-modulating properties. This article documents the evolution of a…”
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