Search Results - "Stewart, Eugene"

Emergence of Resistance in HIV-1 Integrase with Dolutegravir Treatment in a Pediatric Population from the IMPAACT P1093 Study by Vavro, Cindy, Ruel, Theodore, Wiznia, Andrew, Montañez, Nicole, Nangle, Keith, Horton, Joseph, Buchanan, Ann M, Stewart, Eugene L, Palumbo, Paul

“…P1093 is a multicenter, open-label, phase I/II study of pharmacokinetics, safety, and tolerability of dolutegravir plus an optimized background regimen in…”
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Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study by Underwood, Mark, Horton, Joe, Nangle, Keith, Hopking, Judy, Smith, Kimberly, Aboud, Michael, Wynne, Brian, Sievers, Jörg, Stewart, Eugene L, Wang, Ruolan

“…At week 48 in the phase IIIb DAWNING study, the integrase strand transfer inhibitor (INSTI) dolutegravir plus 2 nucleoside reverse transcriptase inhibitors…”
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Correction for Underwood et al., "Integrase Inhibitor Resistance Mechanisms and Structural Characteristics in Antiretroviral Therapy-Experienced, Integrase Inhibitor-Naive Adults with HIV-1 Infection Treated with Dolutegravir plus Two Nucleoside Reverse Transcriptase Inhibitors in the DAWNING Study" by Underwood, Mark, Horton, Joe, Nangle, Keith, Hopking, Judy, Smith, Kimberly, Aboud, Michael, Wynne, Brian, Sievers, Jörg, Stewart, Eugene L, Wang, Ruolan

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Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors by Haffner, Curt D, Becherer, J. David, Boros, Eric E, Cadilla, Rodolfo, Carpenter, Tiffany, Cowan, David, Deaton, David N, Guo, Yu, Harrington, Wallace, Henke, Brad R, Jeune, Michael R, Kaldor, Istvan, Milliken, Naphtali, Petrov, Kim G, Preugschat, Frank, Schulte, Christie, Shearer, Barry G, Shearer, Todd, Smalley, Terrence L, Stewart, Eugene L, Stuart, J. Darren, Ulrich, John C

“…A series of thiazoloquin­(az)­olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown…”
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Rational Design of Potent Non-Nucleoside Inhibitors of HIV‑1 Reverse Transcriptase by Chong, Pek, Sebahar, Paul, Youngman, Michael, Garrido, Dulce, Zhang, Huichang, Stewart, Eugene L., Nolte, Robert T., Wang, Liping, Ferris, Robert G., Edelstein, Mark, Weaver, Kurt, Mathis, Amanda, Peat, Andrew

“…A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess…”
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A pre-steady state and steady state kinetic analysis of the N-ribosyl hydrolase activity of hCD157 by Preugschat, Frank, Carter, Luke H., Boros, Eric E., Porter, David J.T., Stewart, Eugene L., Shewchuk, Lisa M.

“…•Nicotinamide riboside (NR) and nicotinic acid riboside (NAR) are hydrolyzed by hCD157.•The enzyme hydrolyzes NR with a kcat/KM of 17μM−1s−1. NR is the…”
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Complementary NAD + replacement strategies fail to functionally protect dystrophin-deficient muscle by Frederick, David W, McDougal, Alan V, Semenas, Melisa, Vappiani, Johanna, Nuzzo, Andrea, Ulrich, John C, Becherer, J David, Preugschat, Frank, Stewart, Eugene L, Sévin, Daniel C, Kramer, H Fritz

“…Duchenne muscular dystrophy (DMD) is a progressive muscle wasting disorder stemming from a loss of functional dystrophin. Current therapeutic options for DMD…”
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Discovery of 4‑Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38 by Becherer, J. David, Boros, Eric E., Carpenter, Tiffany Y., Cowan, David J., Deaton, David N., Haffner, Curt D., Jeune, Michael R., Kaldor, Istvan W., Poole, J. Chuck, Preugschat, Frank, Rheault, Tara R., Schulte, Christie A., Shearer, Barry G., Shearer, Todd W., Shewchuk, Lisa M., Smalley, Terrence L., Stewart, Eugene L., Stuart, J. Darren, Ulrich, John C.

“…Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure–activity relationships (SAR)…”
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Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition by Bledsoe, Randy K., Montana, Valerie G., Stanley, Thomas B., Delves, Chris J., Apolito, Christopher J., McKee, David D., Consler, Thomas G., Parks, Derek J., Stewart, Eugene L., Willson, Timothy M., Lambert, Millard H., Moore, John T., Pearce, Kenneth H., Xu, H.Eric

“…Transcriptional regulation by the glucocorticoid receptor (GR) is mediated by hormone binding, receptor dimerization, and coactivator recruitment. Here, we…”
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Structural Basis for Androgen Receptor Interdomain and Coactivator Interactions Suggests a Transition in Nuclear Receptor Activation Function Dominance by He, Bin, Gampe, Robert T., Kole, Adam J., Hnat, Andrew T., Stanley, Thomas B., An, Gang, Stewart, Eugene L., Kalman, Rebecca I., Minges, John T., Wilson, Elizabeth M.

“…The androgen receptor (AR) is required for male sex development and contributes to prostate cancer cell survival. In contrast to other nuclear receptors that…”
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2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships by Deaton, David N., Haffner, Curt D., Henke, Brad R., Jeune, Michael R., Shearer, Barry G., Stewart, Eugene L., Stuart, J. Darren, Ulrich, John C.

“…[Display omitted] Starting from 4-amino-8-quinoline carboxamide lead 1a and scaffold hopping to the chemically more tractable quinazoline, a systematic…”
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X-ray Crystal Structure of the Novel Enhanced-Affinity Glucocorticoid Agonist Fluticasone Furoate in the Glucocorticoid Receptor−Ligand Binding Domain by Biggadike, Keith, Bledsoe, Randy K, Hassell, Anne M, Kirk, Barrie E, McLay, Iain M, Shewchuk, Lisa M, Stewart, Eugene L

“…An X-ray crystal structure is reported for the novel enhanced-affinity glucocorticoid agonist fluticasone furoate (FF) in the ligand binding domain of the…”
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A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator by Madauss, Kevin P, Grygielko, Eugene T, Deng, Su-Jun, Sulpizio, Anthony C, Stanley, Thomas B, Wu, Charlene, Short, Steve A, Thompson, Scott K, Stewart, Eugene L, Laping, Nicholas J, Williams, Shawn P, Bray, Jeffrey D

“…Selective progesterone receptor modulators (SPRMs) have been suggested as therapeutic agents for treatment of gynecological disorders. One such SPRM,…”
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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists by Zuercher, William J, Buckholz, Richard G, Campobasso, Nino, Collins, Jon L, Galardi, Cristin M, Gampe, Robert T, Hyatt, Stephen M, Merrihew, Susan L, Moore, John T, Oplinger, Jeffrey A, Reid, Paul R, Spearing, Paul K, Stanley, Thomas B, Stewart, Eugene L, Willson, Timothy M

“…Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased…”
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A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors by Schulte, Christie A., Deaton, David N., Diaz, Elsie, Do, Young, Gampe, Robert T., Guss, Jeffrey H., Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Holt, Jason, Jeune, Michael R., Kahler, Kirsten M., Kramer, H. Fritz, Le, Joelle, Mortenson, Paul N., Musetti, Caterina, Nolte, Robert T., Orband-Miller, Lisa A., Peckham, Gregory E., Petrov, Kim G., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Saxty, Gordon, Shillings, Anthony, Smalley, Terrence L., Somers, Don O., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A.

“…Through an internal virtual screen performed at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were…”
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The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors by Deaton, David N., Do, Young, Holt, Jason, Jeune, Michael R., Kramer, H. Fritz, Larkin, Andrew L., Orband-Miller, Lisa A., Peckham, Gregory E., Poole, Chuck, Price, Daniel J., Schaller, Lee T., Shen, Ying, Shewchuk, Lisa M., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A., Ward, Paris, Wilson, Joseph W., Xu, Tianshun, Guss, Jeffrey H., Musetti, Caterina, Rendina, Alan R., Affleck, Karen, Anders, David, Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Hutchinson, Jonathan, Leveridge, Melanie V., Nicholls, Harry, Smith, Ian E.D., Somers, Don O., Sneddon, Helen F., Uddin, Sorif, Cleasby, Anne, Mortenson, Paul N., Richardson, Caroline, Saxty, Gordon

“…[Display omitted] With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a…”
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Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase by Maynard, Andrew, Crosby, Renae M., Ellis, Byron, Hamatake, Robert, Hong, Zhi, Johns, Brian A., Kahler, Kirsten M., Koble, Cecilia, Leivers, Anna, Leivers, Martin R., Mathis, Amanda, Peat, Andrew J., Pouliot, Jeffrey J., Roberts, Christopher D., Samano, Vicente, Schmidt, Rachel M., Smith, Gary K., Spaltenstein, Andrew, Stewart, Eugene L., Thommes, Pia, Turner, Elizabeth M., Voitenleitner, Christian, Walker, Jill T., Waitt, Greg, Weatherhead, Jason, Weaver, Kurt, Williams, Shawn, Wright, Lois, Xiong, Zhiping Z., Haigh, David, Shotwell, J. Brad

“…A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical…”
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The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure by Cadilla, Rodolfo, Deaton, David N., Do, Young, Elkins, Patricia A., Ennulat, Daniela, Guss, Jeffrey H., Holt, Jason, Jeune, Michael R., King, Andrew G., Klapwijk, Jan C., Kramer, H. Fritz, Kramer, Nicholas J., Laffan, Susan B., Masuria, Paresh I., McDougal, Alan V., Mortenson, Paul N., Musetti, Caterina, Peckham, Gregory E., Pietrak, Beth L., Poole, Chuck, Price, Daniel J., Rendina, Alan R., Sati, Girish, Saxty, Gordon, Shearer, Barry G., Shewchuk, Lisa M., Sneddon, Helen F., Stewart, Eugene L., Stuart, J. Darren, Thomas, Dean N., Thomson, Stephen A., Ward, Paris, Wilson, Joseph W., Xu, Tiahshun, Youngman, Mark A.

“…[Display omitted] GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC50 = 9.9 nM) as…”
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The evolution of progesterone receptor ligands by Madauss, Kevin P., Stewart, Eugene L., Williams, Shawn P.

“…Progesterone is one of the first nuclear receptor hormones to be described functionally and subsequently approached as a drug target. Because progesterone (1)…”
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The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist by MADAUSS, Kevin P, BLEDSOE, Randy K, MCLAY, Iain, STEWART, Eugene L, UINGS, Iain J, WEINGARTEN, Gordon, WILLIAMS, Shawn P

“…The amino-pyrazole 2,6-dichloro-N-ethyl benzamide 1 is a selective GR agonist with dexamethasone-like in vitro potency. Its X-ray crystal structure in the GR…”
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