Search Results - "Head, Victoria"

Defective epithelial barrier function in asthma by Xiao, Chang, PhD, Puddicombe, Sarah M., PhD, Field, Sarah, PhD, Haywood, Joel, BSc, Broughton-Head, Victoria, PhD, Puxeddu, Ilaria, MD, PhD, Haitchi, Hans Michael, MD, PhD, Vernon-Wilson, Elizabeth, PhD, Sammut, David, MD, Bedke, Nicole, PhD, Cremin, Catherine, BSc, Sones, Jody, BSc, Djukanović, Ratko, MD, DM, Howarth, Peter H., MD, DM, Collins, Jane E., PhD, Holgate, Stephen T., MD, DSc, Monk, Phillip, PhD, Davies, Donna E., PhD

“…Background Asthma is a complex disease involving gene and environment interactions. Although atopy is a strong predisposing risk factor for asthma, local…”
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Discovery, Optimization, and Biological Evaluation of 5‑(2-(Trifluoromethyl)phenyl)­indazoles as a Novel Class of Transient Receptor Potential A1 (TRPA1) Antagonists by Rooney, Lisa, Vidal, Agnès, D’Souza, Anne-Marie, Devereux, Nick, Masick, Brian, Boissel, Valerie, West, Ryan, Head, Victoria, Stringer, Rowan, Lao, Jianmin, Petrus, Matt J, Patapoutian, Ardem, Nash, Mark, Stoakley, Natalie, Panesar, Moh, Verkuyl, J. Martin, Schumacher, Andrew M, Petrassi, H. Michael, Tully, David C

“…A high throughput screening campaign identified 5-(2-chlorophenyl)indazole compound 4 as an antagonist of the transient receptor potential A1 (TRPA1) ion…”
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Footprinting: A method for determining the sequence selectivity, affinity and kinetics of DNA-binding ligands by Hampshire, Andrew J., Rusling, David A., Broughton-Head, Victoria J., Fox, Keith R.

“…Footprinting is a simple method for assessing the sequence selectivity of DNA-binding ligands. The method is based on the ability of the ligand to protect DNA…”
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Unfractionated heparin reduces the elasticity of sputum from patients with cystic fibrosis by Broughton-Head, Victoria J, Shur, Jagdeep, Carroll, Mary P, Smith, James R, Shute, Janis K

“…Mucus obstruction of the airway in patients with cystic fibrosis (CF) reduces lung function, invites infection, and limits delivery of inhaled drugs including…”
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Actin limits enhancement of nanoparticle diffusion through cystic fibrosis sputum by mucolytics by Broughton-Head, Victoria J, Smith, James R, Shur, Jagdeep, Shute, Janis K

“…Abstract Background The secretions in the cystic fibrosis (CF) airways contains high concentrations of polymers, including the respiratory mucins and varying…”
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Triplex Staples:  DNA Double-Strand Cross-Linking at Internal and Terminal Sites Using Psoralen-Containing Triplex-Forming Oligonucleotides by Li, Hong, Broughton-Head, Victoria J, Peng, Guomei, Powers, Vicki E. C, Ovens, Matthew J, Fox, Keith R, Brown, Tom

“…A method has been developed to attach 4‘-(hydroxymethyl)-4,5‘,8-trimethylpsoralen to the 5 position of thymine bases during solid-phase oligonucleotide…”
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Kinetic studies on the formation of DNA triplexes containing the nucleoside analogue 2'-O-(2-aminoethyl)-5-(3-amino-1-propynyl)uridine by Rusling, David A, Broughton-Head, Victoria J, Tuck, Alex, Khairallah, Hannah, Osborne, Sadie D, Brown, Tom, Fox, Keith R

“…We have examined the kinetics of triple helix formation of oligonucleotides that contain the nucleotide analogue…”
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Combining nucleoside analogues to achieve recognition of oligopurine tracts by triplex-forming oligonucleotides at physiological pH by Rusling, David A., Le Strat, Loic, Powers, Vicki E.C., Broughton-Head, Victoria J., Booth, James, Lack, Oliver, Brown, Tom, Fox, Keith R.

“…We have used DNase I footprinting to examine DNA triple helix formation at a 12 base pair oligopurine · oligopyrimidine sequence, using oligonucleotides that…”
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Photoinduced Crosslinking of Double-helical DNA by Psoralen Covalently Linked to a Triple Helix-forming Oligonucleotide under Near-physiological Conditions by Li, Hong, Broughton-Head, Victoria J., Fox, Keith R., Brown, Tom

“…Stable triplexes have been generated under near-physiological conditions by the introduction of the C and T base analogues 3-methyl-2-aminopyridine-2…”
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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C by Weiss, Andreas, Lorthiois, Edwige, Barys, Louise, Beyer, Kim S, Bomio-Confaglia, Claudio, Burks, Heather, Chen, Xueying, Cui, Xiaoming, de Kanter, Ruben, Dharmarajan, Lekshmi, Fedele, Carmine, Gerspacher, Marc, Guthy, Daniel Alexander, Head, Victoria, Jaeger, Ashley, Núñez, Eloísa Jiménez, Kearns, Jeffrey D, Leblanc, Catherine, Maira, Sauveur-Michel, Murphy, Jason, Oakman, Helen, Ostermann, Nils, Ottl, Johannes, Rigollier, Pascal, Roman, Danielle, Schnell, Christian, Sedrani, Richard, Shimizu, Toshio, Stringer, Rowan, Vaupel, Andrea, Voshol, Hans, Wessels, Peter, Widmer, Toni, Wilcken, Rainer, Xu, Kun, Zecri, Frederic, Farago, Anna F, Cotesta, Simona, Brachmann, Saskia M

“…Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional…”
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Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva by Ullrich, Thomas, Arista, Luca, Weiler, Sven, Teixeira-Fouchard, Sylvie, Broennimann, Valérie, Stiefl, Nikolaus, Head, Victoria, Kramer, Ina, Guth, Sabine

“…[Display omitted] Inhibition of mutant activin A type-1 receptor ACVR1 (ALK2) signaling by small-molecule drugs is a promising therapeutic approach to treat…”
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Selective inhibition of histamine-evoked Ca2+ signals by compartmentalized cAMP in human bronchial airway smooth muscle cells by Dale, Philippa, Head, Victoria, Dowling, Mark R., Taylor, Colin W.

“…[Display omitted] •β2-adrenoceptors, via cAMP and PKA, inhibit histamine-evoked Ca2+ signals in human bronchial airway smooth muscle cells.•Responses to other…”
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Development of autotaxin inhibitors: A series of tetrazole cinnamides by Thomson, Christopher G., Le Grand, Darren, Dowling, Mark, Beattie, David, Elphick, Lucy, Faller, Michael, Freeman, Mark, Hardaker, Elizabeth, Head, Victoria, Hemmig, Rene, Hill, Johan, Lister, Andrew, Pascoe, David, Rieffel, Sebastien, Shrestha, Binesh, Steward, Oliver, Zink, Florence

“…A series of inhibitors of Autotaxin (ATX) have been developed from a high throughput screening hit, 1a, which shows an alternative binding mode to known…”
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Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models by Brachmann, Saskia M., Weiss, Andreas, Guthy, Daniel A., Beyer, Kim, Voshol, Johannes, Maira, Michel, Prahallad, Anirudh, Porta, Diana Graus, Schnell, Christian, Ostermann, Nils, Vaupel, Andrea, Gerspacher, Marc, Leblanc, Catherine, Erdmann, Dirk, Sterker, Dario, Kerr, Grainne, Jerome, Giovannoni, Head, Victoria, Stringer, Rowan, De Kanter, Ruben, Jeff, Kearns, Roman, Danielle, Widmer, Toni, Wessels, Peter, Nunez, Eloisa Jimenez, Sedrani, Richard, Zecri, Frederic, Hofmann, Francesco, Engleman, Jeff, Lorthiois, Edwige, Cotesta, Simona

“…RAS is the most frequently mutated oncogene in cancer. KRAS G12C mutations are most prevalent in lung adenocarcinoma (~13%) and colorectal adenocarcinoma…”
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Development of autotaxin inhibitors: A series of zinc binding triazoles by Thomson, Christopher G., Le Grand, Darren, Dowling, Mark, Brocklehurst, Cara E., Chinn, Colin, Elphick, Lucy, Faller, Michael, Freeman, Mark, Furminger, Vikki, Gasser, Cornelia, Hamadi, Ahmed, Hardaker, Elizabeth, Head, Victoria, Hill, Johan C., Janus, Diana I., Pearce, David, Poulaud, Anne-Sophie, Stanley, Emily, Sviridenko, Lilya

“…[Display omitted] •PF-8380 has been used as a template to design a new series of ATX inhibitors.•Reduction of crystallinity was key to improving solubility of…”
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Selective inhibition of histamine-evoked Ca 2+ signals by compartmentalized cAMP in human bronchial airway smooth muscle cells by Dale, Philippa, Head, Victoria, Dowling, Mark R, Taylor, Colin W

“…Intracellular Ca and cAMP typically cause opposing effects on airway smooth muscle contraction. Receptors that stimulate these pathways are therapeutic targets…”
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T1386 Effect of Small and Intermediate Conductance Potassium Channel Modulators On Visceral Hypersensitivity and Function by McHugh, Damian, Head, Victoria, Panesar, Moh S, Tigani, Bruno, Fox, Alyson, Lilley, Elliot

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