Search Results - "Broughton, Howard"

A Residue-Resolved Bayesian Approach to Quantitative Interpretation of Hydrogen–Deuterium Exchange from Mass Spectrometry: Application to Characterizing Protein–Ligand Interactions by Saltzberg, Daniel J, Broughton, Howard B, Pellarin, Riccardo, Chalmers, Michael J, Espada, Alfonso, Dodge, Jeffrey A, Pascal, Bruce D, Griffin, Patrick R, Humblet, Christine, Sali, Andrej

“…Characterization of interactions between proteins and other molecules is crucial for understanding the mechanisms of action of biological systems and, thus,…”
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Benchmarking causal reasoning algorithms for gene expression-based compound mechanism of action analysis by Hosseini-Gerami, Layla, Higgins, Ixavier Alonzo, Collier, David A, Laing, Emma, Evans, David, Broughton, Howard, Bender, Andreas

“…Elucidating compound mechanism of action (MoA) is beneficial to drug discovery, but in practice often represents a significant challenge. Causal Reasoning…”
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MAVEN: compound mechanism of action analysis and visualisation using transcriptomics and compound structure data in R/Shiny by Hosseini-Gerami, Layla, Hernansaiz Ballesteros, Rosa, Liu, Anika, Broughton, Howard, Collier, David Andrew, Bender, Andreas

“…Abstract Background Understanding the Mechanism of Action (MoA) of a compound is an often challenging but equally crucial aspect of drug discovery that can…”
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The Angiopoietin-Like Protein 3 and 8 Complex Interacts with Lipoprotein Lipase and Induces LPL Cleavage by Jin, Najia, Matter, William F, Michael, Laura F, Qian, Yuewei, Gheyi, Tarun, Cano, Leticia, Perez, Carlos, Lafuente, Celia, Broughton, Howard B, Espada, Alfonso

“…Lipoprotein lipase (LPL) is the key enzyme that hydrolyzes triglycerides from triglyceride-rich lipoproteins. Angiopoietin-like proteins (ANGPTL) 3, 4, and 8…”
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The Chemical Basis of Serine Palmitoyltransferase Inhibition by Myriocin by Wadsworth, John M, Clarke, David J, McMahon, Stephen A, Lowther, Jonathan P, Beattie, Ashley E, Langridge-Smith, Pat R. R, Broughton, Howard B, Dunn, Teresa M, Naismith, James H, Campopiano, Dominic J

“…Sphingolipids (SLs) are essential components of cellular membranes formed from the condensation of l-serine and a long-chain acyl thioester. This first step is…”
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Integration of phage and yeast display platforms: A reliable and cost effective approach for binning of peptides as displayed on-phage by Pandya, Priyanka, Sayers, Robert O, Ting, Joey P, Morshedian, Shaghayegh, Torres, Carina, Cudal, Justine S, Zhang, Kai, Fitchett, Jonathan R, Zhang, Qing, Zhang, Feiyu F, Wang, Jing, Durbin, Jim D, Carrillo, Juan J, Espada, Alfonso, Broughton, Howard, Qian, Yuewei, Afshar, Sepideh

“…Hundreds of target specific peptides are routinely discovered by peptide display platforms. However, due to the high cost of peptide synthesis only a limited…”
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Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt) by Lugar, Charles W, Clarke, Christian A, Morphy, Richard, Rudyk, Helene, Sapmaz, Selma, Stites, Ryan E, Vaught, Grant M, Furness, Kelly, Broughton, Howard B, Durst, Greg L, Clawson, David K, Stout, Stephanie L, Guo, Sherry Y, Durbin, Jim D, Stayrook, Keith R, Edmondson, Denise D, Kikly, Kristy, New, Nicole E, Bina, Holly A, Chambers, Mark G, Shetler, Pamela, Chang, William Y, Chang, Veavi Ching-Yun, Barr, Rob, Gough, Wendy H, Steele, Jimmy P, Getman, Brian, Patel, Nita, Mathes, Brian M, Richardson, Timothy I

“…The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells…”
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Utilization of peptide phage display to investigate hotspots on IL-17A and what it means for drug discovery by Ting, Joey P, Tung, Frances, Antonysamy, Stephen, Wasserman, Stephen, Jones, Spencer B, Zhang, Feiyu F, Espada, Alfonso, Broughton, Howard, Chalmers, Michael J, Woodman, Michael E, Bina, Holly A, Dodge, Jeffrey A, Benach, Jordi, Zhang, Aiping, Groshong, Christopher, Manglicmot, Danalyn, Russell, Marijane, Afshar, Sepideh

“…To date, IL-17A antibodies remain the only therapeutic approach to correct the abnormal activation of the IL-17A/IL-17R signaling complex. Why is it that…”
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Mechanism of action deconvolution of the small-molecule pathological tau aggregation inhibitor Anle138b by Hosseini-Gerami, Layla, Ficulle, Elena, Humphryes-Kirilov, Neil, Airey, David C, Scherschel, James, Kananathan, Sarubini, Eastwood, Brian J, Bose, Suchira, Collier, David A, Laing, Emma, Evans, David, Broughton, Howard, Bender, Andreas

“…A key histopathological hallmark of Alzheimer's disease (AD) is the presence of neurofibrillary tangles of aggregated microtubule-associated protein tau in…”
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Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy by Gharbi, Severine Isabelle, Pelletier, Laura A., Espada, Alfonso, Gutiérrez, Jesus, Sanfeliciano, Sonia Maria Gutiérrez, Rauch, Charles T., Ganado, Maria Patricia, Baquero, Carmen, Zapatero, Elisabet, Zhang, Aiping, Benach, Jordi, Russell, Anna-Maria, Cano, Leticia, Gomez, Sandra, Broughton, Howard, Pulliam, Nicholas, Perez, Carmen Maria, Torres, Raquel, Debets, Marjoke F., de Dios, Alfonso, Puig, Oscar, Hilgers, Mark T., Lallena, Maria Jose

“…Despite the biological and therapeutic relevance of CDK4/6 for the treatment of HR+, HER2- advanced breast cancer, the detailed mode of action of CDK4/6…”
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Identification of a Novel, Selective GABAA α5 Receptor Inverse Agonist Which Enhances Cognition by Chambers, Mark S, Atack, John R, Broughton, Howard B, Collinson, Neil, Cook, Susan, Dawson, Gerard R, Hobbs, Sarah C, Marshall, George, Maubach, Karen A, Pillai, Goplan V, Reeve, Austin J, MacLeod, Angus M

“…In pursuit of a GABAA α5-subtype-selective inverse agonist to enhance cognition, a series of 6,7-dihydro-2-benzothiophen-4(5H)-ones has been identified as a…”
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Author Correction: Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy by Gharbi, Severine Isabelle, Pelletier, Laura A., Espada, Alfonso, Gutiérrez, Jesus, Sanfeliciano, Sonia Maria Gutiérrez, Rauch, Charles T., Ganado, Maria Patricia, Baquero, Carmen, Zapatero, Elisabet, Zhang, Aiping, Benach, Jordi, Russell, Anna-Maria, Cano, Leticia, Gomez, Sandra, Broughton, Howard, Pulliam, Nicholas, Perez, Carmen Maria, Torres, Raquel, Debets, Marjoke F., de Dios, Alfonso, Puig, Oscar, Hilgers, Mark T., Lallena, Maria Jose

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Selection of heterocycles for drug design by Broughton, Howard B., Watson, Ian A.

“…A method has been devised to obtain heterocyclic ring systems suitable for use in drug design and library design, with an emphasis on the selection of systems…”
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N-Arylsulfonylindole Derivatives as Serotonin 5-HT6 Receptor Ligands by Russell, Michael G. N, Baker, Robert J, Barden, Laura, Beer, Margaret S, Bristow, Linda, Broughton, Howard B, Knowles, Michael, McAllister, George, Patel, Smita, Castro, José L

“…A series of N 1-arylsulfonyltryptamines were found to be potent ligands of the human serotonin 5-HT6 receptor with the 5-methoxy-1-benzenesulfonyl analogue…”
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3-[[4-(4-Chlorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine:  An Antagonist with High Affinity and Selectivity for the Human Dopamine D4 Receptor by Kulagowski, Janusz J, Broughton, Howard B, Curtis, Neil R, Mawer, Ian M, Ridgill, Mark P, Baker, Raymond, Emms, Frances, Freedman, Stephen B, Marwood, Rosemarie, Patel, Shil, Patel, Smita, Ragan, C. Ian, Leeson, Paul D

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Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles by van Niel, Monique B, Collins, Ian, Beer, Margaret S, Broughton, Howard B, Cheng, Susan K. F, Goodacre, Simon C, Heald, Anne, Locker, Karen L, MacLeod, Angus M, Morrison, Denise, Moyes, Christopher R, O'Connor, Desmond, Pike, Andrew, Rowley, Michael, Russell, Michael G. N, Sohal, Balbinder, Stanton, Josephine A, Thomas, Steven, Verrier, Hugh, Watt, Alan P, Castro, José L

“…It has previously been reported that a 3-(3-(piperazin-1-yl)propyl)indole series of 5-HT1D receptor ligands have pharmacokinetic advantages over the…”
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5-(4-Chlorophenyl)-4-methyl-3-(1-(2- phenylethyl)piperidin-4-yl)isoxazole:  A Potent, Selective Antagonist at Human Cloned Dopamine D4 Receptors by Rowley, Michael, Broughton, Howard B, Collins, Ian, Baker, Raymond, Emms, Frances, Marwood, Rosemarie, Patel, Shil, Patel, Smita, Ragan, C. Ian, Freedman, Stephen B, Leeson, Paul D

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Stereocontrolled Synthesis of Cyclopropanol Amino Acids from Allylic Sulfones:  Conformationally Restricted Building Blocks by Díez, David, Garcia, P, Marcos, Isidro S, Garrido, N. M, Basabe, P, Broughton, Howard B, Urones, Julio G

“…A new amino acid methyl ester with a cyclopropanol has been synthesized starting from the allyl sulfone 10. The starting material, 10, could be obtained in…”
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6,7-Dihydro-2-benzothiophen-4(5H)-ones:  A Novel Class of GABA-A α5 Receptor Inverse Agonists by Chambers, Mark S, Atack, John R, Bromidge, Frances A, Broughton, Howard B, Cook, Susan, Dawson, Gerard R, Hobbs, Sarah C, Maubach, Karen A, Reeve, Austin J, Seabrook, Guy R, Wafford, Keith, MacLeod, Angus M

“…Nonselective inverse agonists at the benzodiazepine binding site on the GABA-A chloride ion channel enhance cognitive performance in animals but cannot be used…”
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A method for including protein flexibility in protein-ligand docking: improving tools for database mining and virtual screening by Broughton, Howard B.

“…Second-generation methods for docking ligands into their biological receptors, such as FLOG, provide for flexibility of the ligand but not of the receptor…”
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