Search Results - "Graham Smith, F."

The Landscape of Potential Small and Drug Substance Related Nitrosamines in Pharmaceuticals by Schlingemann, Joerg, Burns, Michael J, Ponting, David J, Martins Avila, Carolina, Romero, Naiffer E, Jaywant, Mrunal A, Smith, Graham F, Ashworth, Ian W, Simon, Stephanie, Saal, Christoph, Wilk, Andrzej

“…This article reports the outcome of an in silico analysis of more than 12,000 small molecule drugs and drug impurities, identifying the nitrosatable…”
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Discovery of Selective RNA-Binding Small Molecules by Affinity-Selection Mass Spectrometry by Rizvi, Noreen F, Howe, John A, Nahvi, Ali, Klein, Daniel J, Fischmann, Thierry O, Kim, Hai-Young, McCoy, Mark A, Walker, Scott S, Hruza, Alan, Richards, Matthew P, Chamberlin, Chad, Saradjian, Peter, Butko, Margaret T, Mercado, Gabriel, Burchard, Julja, Strickland, Corey, Dandliker, Peter J, Smith, Graham F, Nickbarg, Elliott B

“…Recent advances in understanding the relevance of noncoding RNA (ncRNA) to disease have increased interest in drugging ncRNA with small molecules. The recent…”
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Retrospective analysis of the potential use of virtual control groups in preclinical toxicity assessment using the eTOX database by Wright, Peter S.R., Smith, Graham F., Briggs, Katharine A., Thomas, Robert, Maglennon, Gareth, Mikulskis, Paulius, Chapman, Melissa, Greene, Nigel, Phillips, Benjamin U., Bender, Andreas

“…Virtual Control Groups (VCGs) based on Historical Control Data (HCD) in preclinical toxicity testing have the potential to reduce animal usage. As a case study…”
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The 1997 event in the Crab pulsar revisited by Graham Smith, F., Lyne, A. G., Jordan, C.

“…A complex event observed in the radio pulses from the Crab pulsar in 1997 included echoes, a dispersive delay and large changes in intensity. It is shown that…”
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Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications by Lim, Jongwon, Altman, Michael D., Baker, James, Brubaker, Jason D., Chen, Hongmin, Chen, Yiping, Kleinschek, Melanie A., Li, Chaomin, Liu, Duan, Maclean, John K.F., Mulrooney, Erin F., Presland, Jeremy, Rakhilina, Larissa, Smith, Graham F., Yang, Ruojing

“…[Display omitted] IRAK4 plays a critical role in the IL-1R and TLR signalling, and selective inhibition of the kinase activity of the protein represents an…”
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Mode switching and subpulse drifting in PSR B0826-34 by Esamdin, A., Lyne, A. G., Graham-Smith, F., Kramer, M., Manchester, R. N., Wu, X.

“…We present high-quality observations of PSR B0826-34 at 1374 MHz. The emission from this pulsar exhibits strong bursts of pulses followed by long periods of…”
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RNA as a small molecule druggable target by Rizvi, Noreen F., Smith, Graham F.

“…[Display omitted] Small molecule drugs have readily been developed against many proteins in the human proteome, but RNA has remained an elusive target for drug…”
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45 years of rotation of the Crab pulsar by Lyne, A G, Jordan, C A, Graham-Smith, F, Espinoza, C M, Stappers, B W, Weltevrede, P

“…The 30-Hz rotation rate of the Crab pulsar has been monitored at Jodrell Bank Observatory since 1984 and by other observatories before then. Since 1968, the…”
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Targeting RNA with small molecules-A safety perspective by Lightfoot, Helen L, Smith, Graham F

“…RNA is a major player in cellular function, and consequently can drive a number of disease pathologies. Over the past several years, small molecule-RNA…”
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Targeting Xist with compounds that disrupt RNA structure and X inactivation by Aguilar, Rodrigo, Spencer, Kerrie B., Kesner, Barry, Rizvi, Noreen F., Badmalia, Maulik D., Mrozowich, Tyler, Mortison, Jonathan D., Rivera, Carlos, Smith, Graham F., Burchard, Julja, Dandliker, Peter J., Patel, Trushar R., Nickbarg, Elliott B., Lee, Jeannie T.

“…Although more than 98% of the human genome is non-coding 1 , nearly all of the drugs on the market target one of about 700 disease-related proteins. The…”
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Prediction of In Vivo Pharmacokinetic Parameters and Time–Exposure Curves in Rats Using Machine Learning from the Chemical Structure by Obrezanova, Olga, Martinsson, Anton, Whitehead, Tom, Mahmoud, Samar, Bender, Andreas, Miljković, Filip, Grabowski, Piotr, Irwin, Ben, Oprisiu, Ioana, Conduit, Gareth, Segall, Matthew, Smith, Graham F, Williamson, Beth, Winiwarter, Susanne, Greene, Nigel

“…Animal pharmacokinetic (PK) data as well as human and animal in vitro systems are utilized in drug discovery to define the rate and route of drug elimination…”
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Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies by Brown, Dean G, Smith, Graham F, Wobst, Heike J

“…We conducted an analysis on screening data generated from 1445 compounds against a panel of 130 enzymes, ion channels, and receptors to assess secondary…”
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Designing drugs to avoid toxicity by Smith, Graham F

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Prediction of inotropic effect based on calcium transients in human iPSC-derived cardiomyocytes and machine learning by Yang, Hongbin, Obrezanova, Olga, Pointon, Amy, Stebbeds, Will, Francis, Jo, Beattie, Kylie A., Clements, Peter, Harvey, James S., Smith, Graham F., Bender, Andreas

“…Functional changes to cardiomyocytes are undesirable during drug discovery and identifying the inotropic effects of compounds is hence necessary to decrease…”
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Mechanisms of Nitrosamine Mutagenicity and Their Relationship to Rodent Carcinogenic Potency by Snodin, David J., Trejo-Martin, Alejandra, Ponting, David J., Smith, Graham F., Czich, Andreas, Cross, Kevin, Custer, Laura, Elloway, Joanne, Greene, Nigel, Kalgutkar, Amit S., Stalford, Susanne A., Tennant, Rachael E., Vock, Esther, Zalewski, Adam, Ziegler, Verena, Dobo, Krista L.

“…A thorough literature review was undertaken to understand how the pathways of N-nitrosamine transformation relate to mutagenic potential and carcinogenic…”
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Synthesis of Cyclic Peptidomimetics via a Pd-Catalyzed Macroamination Reaction by Hopkins, Brett A, Smith, Graham F, Sciammetta, Nunzio

“…A new method to access cyclic peptidomimetics via a Pd-catalyzed macroamination reaction is presented. Natural amino acid amines are revealed as proficient…”
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Statistical analysis of preclinical inter-species concordance of histopathological findings in the eTOX database by Wright, Peter S.R., Briggs, Katharine A., Thomas, Robert, Smith, Graham F., Maglennon, Gareth, Mikulskis, Paulius, Chapman, Melissa, Greene, Nigel, Phillips, Benjamin U., Bender, Andreas

“…Preclinical inter-species concordance can increase the predictivity of observations to the clinic, potentially reducing drug attrition caused by unforeseen…”
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Optimization of an Imidazo[1,2‑a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy by McCoull, William, Boyd, Scott, Brown, Martin R, Coen, Muireann, Collingwood, Olga, Davies, Nichola L, Doherty, Ann, Fairley, Gary, Goldberg, Kristin, Hardaker, Elizabeth, He, Guang, Hennessy, Edward J, Hopcroft, Philip, Hodgson, George, Jackson, Anne, Jiang, Xiefeng, Karmokar, Ankur, Lainé, Anne-Laure, Lindsay, Nicola, Mao, Yumeng, Markandu, Roshini, McMurray, Lindsay, McLean, Neville, Mooney, Lorraine, Musgrove, Helen, Nissink, J. Willem M, Pflug, Alexander, Reddy, Venkatesh Pilla, Rawlins, Philip B, Rivers, Emma, Schimpl, Marianne, Smith, Graham F, Tentarelli, Sharon, Travers, Jon, Troup, Robert I, Walton, Josephine, Wang, Cheng, Wilkinson, Stephen, Williamson, Beth, Winter-Holt, Jon, Yang, Dejian, Zheng, Yuting, Zhu, Qianxiu, Smith, Paul D

“…Inhibition of Mer and Axl kinases has been implicated as a potential way to improve the efficacy of current immuno-oncology therapeutics by restoring the…”
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Deriving waveform parameters from calcium transients in human iPSC-derived cardiomyocytes to predict cardiac activity with machine learning by Yang, Hongbin, Stebbeds, Will, Francis, Jo, Pointon, Amy, Obrezanova, Olga, Beattie, Kylie A., Clements, Peter, Harvey, James S., Smith, Graham F., Bender, Andreas

“…Human induced pluripotent stem cell-derived cardiomyocytes have been established to detect dynamic calcium transients by fast kinetic fluorescence assays that…”
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Pulsar reflections within the Crab Nebula by Lyne, A. G., Pritchard, R. S., Graham-Smith, F.

“…Between 1997 August and October, the radio pulses from the Crab pulsar were followed by discrete moving echoes, which appear to be reflections from part of an…”
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