Search Results - "SOHAL, Bindi"

Validation of a rapid equilibrium dialysis approach for the measurement of plasma protein binding by Waters, Nigel J, Jones, Rachel, Williams, Gareth, Sohal, Bindi

“…Equilibrium dialysis (ED) is one of the most frequently used approaches to investigate drug binding, where the major drawbacks are the time to reach…”
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Prediction of Drug Clearance by Glucuronidation from in Vitro Data: Use of Combined Cytochrome P450 and UDP-Glucuronosyltransferase Cofactors in Alamethicin-Activated Human Liver Microsomes by KILFORD, Peter J, STRINGER, Rowan, SOHAL, Bindi, HOUSTON, J. Brian, GALETIN, Aleksandra

“…Glucuronidation via UDP-glucuronosyltransferase (UGT) is an increasingly important clearance pathway. In this study intrinsic clearance (CL int ) values for…”
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An inhibitor of NADPH oxidase-4 attenuates established pulmonary fibrosis in a rodent disease model by Jarman, Elizabeth R, Khambata, Valerie S, Cope, Claire, Jones, Peter, Roger, Jan, Ye, Li Yun, Duggan, Nicholas, Head, Denise, Pearce, Andrew, Press, Neil J, Bellenie, Ben, Sohal, Bindi, Jarai, Gabor

“…Idiopathic pulmonary fibrosis is a chronic progressive disease of increasing prevalence for which there is no effective therapy. Increased oxidative stress…”
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Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders by Goodacre, Simon C, Street, Leslie J, Hallett, David J, Crawforth, James M, Kelly, Sarah, Owens, Andrew P, Blackaby, Wesley P, Lewis, Richard T, Stanley, Joanna, Smith, Alison J, Ferris, Pushpinder, Sohal, Bindi, Cook, Susan M, Pike, Andrew, Brown, Nicola, Wafford, Keith A, Marshall, George, Castro, José L, Atack, John R

“…A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABAAα2 and -α3 subtypes is reported…”
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Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) in rats, primates, and humans by Atack, John R, Wong, Dean F, Fryer, Tim D, Ryan, Christine, Sanabria, Sandra, Zhou, Yun, Dannals, Robert F, Eng, Wai-si, Gibson, Raymond E, Burns, H Donald, Vega, Jose M, Vessy, Laura, Scott-Stevens, Paul, Beech, John S, Baron, Jean-Claude, Sohal, Bindi, Schrag, Michael L, Aigbirhio, Franklin I, McKernan, Ruth M, Hargreaves, Richard J

“…The GABA(A) receptor alpha2/alpha3 subtype-selective compound…”
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Utility of Long-Term Cultured Human Hepatocytes as an in Vitro Model for Cytochrome P450 Induction by MENESES-LORENTE, Georgina, PATTISON, Christine, GUYOMARD, Claire, CHESNE, Christophe, HEAVENS, Robert, WATT, Alan P, SOHAL, Bindi

“…Cytochrome P450 (P450) induction may have considerable implications for drug therapy. Therefore, understanding the induction potential of a new chemical entity…”
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An Evaluation of a Low-Density DNA Microarray Using Cytochrome P450 Inducers by Meneses-Lorente, Georgina, de Longueville, Françoise, Dos Santos-Mendes, Sofia, Bonnert, Timothy P, Jack, Andrew, Evrard, Stéphanie, Bertholet, Vincent, Pike, Andrew, Scott-Stevens, Paul, Remacle, José, Sohal, Bindi

“…The aim of this study was to validate a low-density DNA microarray “Rat HepatoChip”, which contains 59 genes from a range of potential toxic markers and drug…”
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Design and Synthesis of Inhibitors of the E3 Ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 as a Treatment for Lung Remodeling in Pulmonary Arterial Hypertension by Shaw, Duncan E., Smith, Nichola, Beerli, Rene, Cotesta, Simona, D’Alessandro, Pier-Luca, Edwards, Anne-Marie, Lattmann, Rene, Lizos, Dimitrios, Pulz, Robert, Rooney, Lisa, Sohal, Bindi, Rynn, Caroline, Taylor, Jessica, Troxler, Thomas, Williams, Gareth, Guth, Sabine, Rowlands, David

“…Pulmonary arterial hypertension (PAH) is a devastating rare disease, which despite currently available treatments, still represents a high unmet medical need…”
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1-Aminobenzotriazole modulates oral drug pharmacokinetics through cytochrome P450 inhibition and delay of gastric emptying in rats by Stringer, Rowan A, Weber, Eckhard, Tigani, Bruno, Lavan, Paul, Medhurst, Stephen, Sohal, Bindi

“…The simultaneous effects of the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT) on inhibition of in vivo metabolism and gastric emptying were evaluated…”
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NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo by Namoto, Kenji, Baader, Clara, Orsini, Vanessa, Landshammer, Alexandro, Breuer, Eva, Dinh, Kieu Trinh, Ungricht, Rosemarie, Pikiolek, Monika, Laurent, Stephane, Lu, Bo, Aebi, Alexandra, Schönberger, Katharina, Vangrevelinghe, Eric, Evrova, Olivera, Sun, Tianliang, Annunziato, Stefano, Lachal, Julie, Redmond, Emily, Wang, Louis, Wetzel, Kristie, Capodieci, Paola, Turner, Jonathan, Schutzius, Gabi, Unterreiner, Vincent, Trunzer, Markus, Buschmann, Nicole, Behnke, Dirk, Machauer, Rainer, Scheufler, Clemens, Parker, Christian N, Ferro, Magali, Grevot, Armelle, Beyerbach, Armin, Lu, Wei-Yu, Forbes, Stuart J, Wagner, Jürgen, Bouwmeester, Tewis, Liu, Jun, Sohal, Bindi, Sahambi, Sukhdeep, Greenbaum, Linda E, Lohmann, Felix, Hoppe, Philipp, Cong, Feng, Sailer, Andreas W, Ruffner, Heinz, Glatthar, Ralf, Humar, Bostjan, Clavien, Pierre-Alain, Dill, Michael T, George, Elizabeth, Maibaum, Jürgen, Liberali, Prisca, Tchorz, Jan S

“…The YAP/Hippo pathway is an organ growth and size regulation rheostat safeguarding multiple tissue stem cell compartments. LATS kinases phosphorylate and…”
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GS07 - Nidufexor, a non-bile acid FXR agonist, decreases ALT and hepatic fat fraction in patients with NASH after 12 weeks dosing by Aspinall, Richard, Shennak, Mustafa, Stocia, George, Quinn, Dean, Javashvili, Lali, Molteni, Valentina, Ukomadu, Chinweike, Sohal, Bindi, Zhang, Yiming, Martic, Miljen, Avrameas, Alexandre, Kao, Sheena, Herve, Jacques, Soon, Rachel, Badman, Michael

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Nidufexor, a non-bile acid FXR agonist, decreases ALT and hepatic fat fraction in patients with NASH after 12 weeks dosing by Aspinall, Richard, Shennak, Mustafa, Stocia, George, Quinn, Dean, Javashvili, Lali, Molteni, Valentina, Ukomadu, Chinweike, Sohal, Bindi, Zhang, Yiming, Martic, Miljen, Avrameas, Alexandre, Kao, Sheena, Herve, Jacques, Soon, Rachel, Badman, Michael

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Do We Need to Study Metabolism and Distribution in the Eye: Why, When, and Are We There Yet? by Argikar, Upendra A, Dumouchel, Jennifer L, Kramlinger, Valerie M, Cirello, Amanda L, Gunduz, Mithat, Dunne, Christine E, Sohal, Bindi

“…The liver is known to be the principal site of drug metabolism. Depending on the route of administration, especially in cases of topical and local delivery,…”
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Application of a deuterium replacement strategy to modulate the pharmacokinetics of 7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b]oxazole, a novel CRF1 antagonist by Stringer, Rowan A, Williams, Gareth, Picard, Franck, Sohal, Bindi, Kretz, Olivier, McKenna, Jeff, Krauser, Joel A

“…Deuterium isotope effects were evaluated as a strategy to optimize the pharmacokinetics of…”
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Application of a Deuterium Replacement Strategy to Modulate the Pharmacokinetics of 7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b]oxazole, a Novel CRF 1 Antagonist by Stringer, Rowan A., Williams, Gareth, Picard, Franck, Sohal, Bindi, Kretz, Olivier, McKenna, Jeff, Krauser, Joel A.

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Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma by Sandham, David A, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven J, Chatterjee, Devnandan, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Maas, Janet, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Catherine, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David A, Thomas, Matthew, Turner, Katharine L, Watson, Simon J, West, Ryan, Willard, Elisabeth, Williams, Gareth, Willis, Jennifer

“…Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule…”
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Preclinical metabolism and pharmacokinetics of NVS-CRF38, a potent and orally bioavailable corticotropin-releasing factor receptor 1 antagonist by Stringer, Rowan A., Weber, Eckhard, Culshaw, Andrew, McKenna, Jeff, Williams, Gareth, Rose, Jonathan, Sohal, Bindi

“…Abstract 1. The pharmacokinetic properties and metabolism of NVS-CRF38…”
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Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases by Sandham, David A., Arnold, Nicola, Aschauer, Heinrich, Bala, Kamlesh, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Cox, Brian, Docx, Cerys, Dubois, Gerald, Duggan, Nicholas, England, Karen, Everatt, Brian, Furegati, Marcus, Hall, Edward, Kalthoff, Frank, King, Anna, Leblanc, Catherine J., Manini, Jodie, Meingassner, Josef, Profit, Rachael, Schmidt, Alfred, Simmons, Jennifer, Sohal, Bindi, Stringer, Rowan, Thomas, Matthew, Turner, Katharine L., Walker, Christoph, Watson, Simon J., Westwick, John, Willis, Jennifer, Williams, Gareth, Wilson, Caroline

“…Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound…”
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Correction to "Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP 2 Receptor Antagonist for Treatment of Asthma" by Sandham, David A, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven J, Chatterjee, Devnandan, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Leblanc, Catherine, Maas, Janet, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Catherine, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David A, Thomas, Matthew, Turner, Katharine L, Watson, Simon J, West, Ryan, Willard, Elisabeth, Williams, Gareth, Willis, Jennifer

“…[This corrects the article DOI: 10.1021/acsmedchemlett.7b00157.]…”
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Correction to “Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma” by Sandham, David A, Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven J, Chatterjee, Devnandan, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Maas, Janet, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Catherine, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David A, Thomas, Matthew, Turner, Katharine L, Watson, Simon J, West, Ryan, Willard, Elisabeth, Williams, Gareth, Willis, Jennifer

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