Search Results - "Hickey, Eugene"

Reversal of H3K9me2 by a Small-Molecule Inhibitor for the G9a Histone Methyltransferase by Kubicek, Stefan, O'Sullivan, Roderick J., August, E. Michael, Hickey, Eugene R., Zhang, Qiang, Teodoro, Miguel L., Rea, Stephen, Mechtler, Karl, Kowalski, Jennifer A., Homon, Carol Ann, Kelly, Terence A., Jenuwein, Thomas

“…Histone lysine methylation has important roles in the organization of chromatin domains and the regulation of gene expression. To analyze its function and…”
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The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis by Harrison, Bryce A., Dowling, James E., Bursavich, Matthew G., Troast, Dawn M., Chong, Katherine M., Hahn, Kristopher N., Zhong, Cheng, Mulvihill, Kristen M., Nguyen, Hanh, Monroy, Meghan F., Qiao, Qi, Sosa, Brian, Mostafavi, Siavash, Smukste, Inese, Lee, Dooyoung, Cappellucci, Laura, Konopka, Elizabeth H., Nowakowski, Patrycja, Stawski, Lukasz, Senices, Mayra, Nguyen, Minh Hai, Kapoor, Parmita S., Luus, Lia, Sullivan, Andrew, Bortolato, Andrea, Svensson, Mats, Hickey, Eugene R., Konze, Kyle D., Day, Tyler, Kim, Byungchan, Negri, Ana, Gerasyuto, Aleksey I., Moy, Terence I., Lu, Min, Ray, Adrian S., Wang, Liangsu, Cui, Dan, Lin, Fu-Yang, Lippa, Blaise, Rogers, Bruce N.

“…Inhibition of integrin αvβ6 is a promising approach to the treatment of fibrotic disease such as idiopathic pulmonary fibrosis. Screening a small library…”
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A GPBAR1 (TGR5) small molecule agonist shows specific inhibitory effects on myeloid cell activation in vitro and reduces experimental autoimmune encephalitis (EAE) in vivo by Lewis, Nuruddeen D, Patnaude, Lori A, Pelletier, Josephine, Souza, Donald J, Lukas, Susan M, King, F James, Hill, Jonathan D, Stefanopoulos, Dimitria E, Ryan, Kelli, Desai, Sudha, Skow, Donna, Kauschke, Stefan G, Broermann, Andre, Kuzmich, Daniel, Harcken, Christian, Hickey, Eugene R, Modis, Louise K

“…GPBAR1 is a G protein-coupled receptor that is activated by certain bile acids and plays an important role in the regulation of bile acid synthesis, lipid…”
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X‐ray crystal structure localizes the mechanism of inhibition of an IL‐36R antagonist monoclonal antibody to interaction with Ig1 and Ig2 extra cellular domains by Larson, Eric T., Brennan, Debra L., Hickey, Eugene R., Ganesan, Raj, Kroe‐Barrett, Rachel, Farrow, Neil A.

“…Cellular signaling via binding of the cytokines IL‐36α, β, and γ along with binding of the accessory protein IL‐36RAcP, to their cognate receptor IL‐36R is…”
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Structural Basis of Constitutive Activity and a Unique Nucleotide Binding Mode of Human Pim-1 Kinase by Qian, Kevin C., Wang, Lian, Hickey, Eugene R., Studts, Joey, Barringer, Kevin, Peng, Charline, Kronkaitis, Anthony, Li, Jun, White, Andre, Mische, Sheenah, Farmer, Bennett

“…Pim-1 kinase is a member of a distinct class of serine/threonine kinases consisting of Pim-1, Pim-2, and Pim-3. Pim kinases are highly homologous to one…”
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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site by Pargellis, Christopher, Tong, Liang, Churchill, Laurie, Cirillo, Pier F, Gilmore, Thomas, Graham, Anne G, Grob, Peter M, Hickey, Eugene R, Moss, Neil, Pav, Susan, Regan, John

“…The p38 MAP kinase plays a crucial role in regulating the production of proinflammatory cytokines, such as tumor necrosis factor and interleukin-1. Blocking…”
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Selective CB2 receptor agonists. Part 1: The identification of novel ligands through computer-aided drug design (CADD) approaches by Hickey, Eugene R., Zindell, Renee, Cirillo, Pier F., Wu, Lifen, Ermann, Monika, Berry, Angela K., Thomson, David S., Albrecht, Claudia, Gemkow, Mark J., Riether, Doris

“…[Display omitted] Computer-aided drug design scaffold hopping strategies were utilized to identify new classes of CB2 agonists when compounds of an established…”
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An in Silico Method for Predicting Ames Activities of Primary Aromatic Amines by Calculating the Stabilities of Nitrenium Ions by Bentzien, Jörg, Hickey, Eugene R, Kemper, Raymond A, Brewer, Mark L, Dyekjær, Jane D, East, Stephen P, Whittaker, Mark

“…In this paper, we describe an in silico first principal approach to predict the mutagenic potential of primary aromatic amines. This approach is based on the…”
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Pyrazole Urea-Based Inhibitors of p38 MAP Kinase:  From Lead Compound to Clinical Candidate by Regan, John, Breitfelder, Steffen, Cirillo, Pier, Gilmore, Thomas, Graham, Anne G, Hickey, Eugene, Klaus, Bernhard, Madwed, Jeffrey, Moriak, Monica, Moss, Neil, Pargellis, Chris, Pav, Sue, Proto, Alfred, Swinamer, Alan, Tong, Liang, Torcellini, Carol

“…We report on a series of N-pyrazole, N‘-aryl ureas and their mode of binding to p38 mitogen activated protein kinase. Importantly, a key binding domain that is…”
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Selective CB2 receptor agonists. Part 3: The optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model by Bartolozzi, Alessandra, Cirillo, Pier Francesco, Berry, Angela K., Hickey, Eugene R., Thomson, David S., Wu, Lifen, Zindell, Renee, Albrecht, Claudia, Ceci, Angelo, Gemkow, Mark J., Nagaraja, Nelamangala V., Romig, Helmut, Sauer, Achim, Riether, Doris

“…[Display omitted] A novel class of potent cannabinoid receptor 2 (CB2) agonists based on a (S)-piperidine scaffold was identified using ligand-based…”
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Identification of a Potent Sodium Hydrogen Exchanger Isoform 1 (NHE1) Inhibitor with a Suitable Profile for Chronic Dosing and Demonstrated Cardioprotective Effects in a Preclinical Model of Myocardial Infarction in the Rat by Huber, John D, Bentzien, Jörg, Boyer, Stephen J, Burke, Jennifer, De Lombaert, Stéphane, Eickmeier, Christian, Guo, Xin, Haist, James V, Hickey, Eugene R, Kaplita, Paul, Karmazyn, Morris, Kemper, Raymond, Kennedy, Charles A, Kirrane, Thomas, Madwed, Jeffrey B, Mainolfi, Elizabeth, Nagaraja, Nelamangara, Soleymanzadeh, Fariba, Swinamer, Alan, Eldrup, Anne B

“…Sodium–hydrogen exchanger isoform 1 (NHE1) is a ubiquitously expressed transmembrane ion channel responsible for intracellular pH regulation. During myocardial…”
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Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 3, aryl substituted pyrrolidines by Bosanac, Todd, Hickey, Eugene R., Ginn, John, Kashem, Mohammed, Kerr, Steven, Kugler, Stanley, Li, Xiang, Olague, Alan, Schlyer, Sabine, Young, Erick R.R.

“…The discovery and SAR of a series of β-aryl substituted pyrrolidine 2H-isoquinolin-1-one inhibitors of Rho-kinase (ROCK) derived from 2 is herein described…”
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Selective CB2 receptor agonists. Part 2: Structure–activity relationship studies and optimization of proline-based compounds by Riether, Doris, Zindell, Renee, Wu, Lifen, Betageri, Raj, Jenkins, James E., Khor, Someina, Berry, Angela K., Hickey, Eugene R., Ermann, Monika, Albrecht, Claudia, Ceci, Angelo, Gemkow, Mark J., Nagaraja, Nelamangala V., Romig, Helmut, Sauer, Achim, Thomson, David S.

“…[Display omitted] Through a ligand-based pharmacophore model (S)-proline based compounds were identified as potent cannabinoid receptor 2 (CB2) agonists with…”
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Exploration of cathepsin S inhibitors characterized by a triazole P1–P2 amide replacement by Moss, Neil, Xiong, Zhaoming, Burke, Mike, Cogan, Derek, Gao, Donghong A., Haverty, Kathleen, Heim-Riether, Alexander, Hickey, Eugene R., Nagaraja, Raj, Netherton, Matthew, O’Shea, Kathy, Ramsden, Philip, Schwartz, Racheline, Shih, Daw-Tsun, Ward, Yancey, Young, Erick, Zhang, Qing

“…This paper details exploration of a class of triazole-based cathepsin S inhibitors examplified by compound 6 originally reported by Ellman and coworkers. SAR…”
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Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats by GINN, John D, BOSANAC, Todd, SCHLYER, Sabine, SMITH, James D, TURNER, Michael R, WU, Frank, YOUNG, Erick R. R, CHEN, Rhonda, CYWIN, Charles, HICKEY, Eugene, KASHEM, Mohammed, KERR, Steven, KUGLER, Stanley, XIANG LI, PROKOPOWICZ, Anthony

“…Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this…”
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New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site by Moss, Neil, Breitfelder, Steffen, Betageri, Raj, Cirillo, Pier F., Fadra, Tazmeen, Hickey, Eugene R., Kirrane, Thomas, Kroe, Rachel R., Madwed, Jeffrey, Nelson, Richard M., Pargellis, Christopher A., Qian, Kevin C., Regan, John, Swinamer, Alan, Torcellini, Carol

“…Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of…”
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Discovery and characterization of the N-phenyl- N′-naphthylurea class of p38 kinase inhibitors by Cirillo, Pier F., Hickey, Eugene R., Moss, Neil, Breitfelder, Steffen, Betageri, Raj, Fadra, Tazmeen, Gaenzler, Faith, Gilmore, Thomas, Goldberg, Daniel R., Kamhi, Victor, Kirrane, Thomas, Kroe, Rachel R., Madwed, Jeffrey, Moriak, Monica, Netherton, Matthew, Pargellis, Christopher A., Patel, Usha R., Qian, Kevin C., Sharma, Rajiv, Sun, Sanxing, Swinamer, Alan, Torcellini, Carol, Takahashi, Hidenori, Tsang, Michele, Xiong, Zhaoming

“…An effort aimed at exploring structural diversity in the N-pyrazole- N′-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization…”
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A Belted Monofacial Ionophore Featuring High Selectivity for Lithium Ion Complexation by Paquette, Leo A., Tae, Jinsung, Hickey, Eugene R., Rogers, Robin D.

“…Despite its preferred equatorial conformation in the solid state and in solution, the cis,cis‐trispiro ether 1 binds readily and strongly to lithium ions. The…”
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A catalogue of Locus Algorithm pointings for optimal differential photometry for 23 779 quasars by Creaner, Oisín, Nolan, Kevin, Smith, Niall, Grennan, David, Hickey, Eugene

“…ABSTRACT This paper presents a catalogue of optimized pointings for differential photometry of 23 779 quasars extracted from the Sloan Digital Sky Survey…”
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Using machine learning to predict the correlation of spectra using SDSS magnitudes as an improvement to the Locus Algorithm by Hickey, Eugene, Creaner, Oisín, Nolan, Kevin, O’Flynn, Tom

“…The Locus Algorithm is a new technique to improve the quality of differential photometry by optimising the choices of reference stars. At the heart of this…”
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