Search Results - "RUMSEY, William L"

Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases by Cuadrado, Antonio, Rojo, Ana I., Wells, Geoffrey, Hayes, John D., Cousin, Sharon P., Rumsey, William L., Attucks, Otis C., Franklin, Stephen, Levonen, Anna-Liisa, Kensler, Thomas W., Dinkova-Kostova, Albena T.

“…The transcription factor NF-E2 p45-related factor 2 (NRF2; encoded by NFE2L2 ) and its principal negative regulator, the E3 ligase adaptor Kelch-like…”
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Small molecule-mediated allosteric activation of the base excision repair enzyme 8-oxoguanine DNA glycosylase and its impact on mitochondrial function by Tian, Gaochao, Katchur, Steven R., Jiang, Yong, Briand, Jacques, Schaber, Michael, Kreatsoulas, Constantine, Schwartz, Benjamin, Thrall, Sara, Davis, Alicia M., Duvall, Sam, Kaufman, Brett A., Rumsey, William L.

“…8-Oxoguanine DNA glycosylase (OGG1) initiates base excision repair of the oxidative DNA damage product 8-oxoguanine. OGG1 is bifunctional; catalyzing glycosyl…”
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Cell-free DNA levels associate with COPD exacerbations and mortality by Ware, Sarah A, Kliment, Corrine R, Giordano, Luca, Redding, Kevin M, Rumsey, William L, Bates, Stewart, Zhang, Yingze, Sciurba, Frank C, Nouraie, S Mehdi, Kaufman, Brett A

“…Good biological indicators capable of predicting chronic obstructive pulmonary disease (COPD) phenotypes and clinical trajectories are lacking. Because nuclear…”
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Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases by Salmon, Michael, Luttmann, Mark A, Foley, James J, Buckley, Peter T, Schmidt, Dulcie B, Burman, Miriam, Webb, Edward F, DeHaas, Christopher J, Kotzer, Charles J, Barrett, Victoria J, Slack, Robert J, Sarau, Henry M, Palovich, Michael R, Lainé, Dramane I, Hay, Douglas W P, Rumsey, William L

“…Activation of muscarinic subtype 3 (M3) muscarinic cholinergic receptors (mAChRs) increases airway tone, whereas its blockade improves lung function and…”
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Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction by Heightman, Tom D, Callahan, James F, Chiarparin, Elisabetta, Coyle, Joseph E, Griffiths-Jones, Charlotte, Lakdawala, Ami S, McMenamin, Rachel, Mortenson, Paul N, Norton, David, Peakman, Torren M, Rich, Sharna J, Richardson, Caroline, Rumsey, William L, Sanchez, Yolanda, Saxty, Gordon, Willems, Henriëtte M. G, Wolfe, Lawrence, Woolford, Alison J.-A, Wu, Zining, Yan, Hongxing, Kerns, Jeffrey K, Davies, Thomas G

“…The KEAP1–NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be…”
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Enhanced mitochondrial DNA repair of the common disease-associated variant, Ser326Cys, of hOGG1 through small molecule intervention by Baptiste, Beverly A., Katchur, Steven R., Fivenson, Elayne M., Croteau, Deborah L., Rumsey, William L., Bohr, Vilhelm A.

“…The common oxidatively generated lesion, 8-oxo-7,8-dihydroguanine (8-oxoGua), is removed from DNA by base excision repair. The glycosylase primarily charged…”
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Structural Analysis and Optimization of NK1 Receptor Antagonists through Modulation of Atropisomer Interconversion Properties by Albert, Jeffrey S, Ohnmacht, Cyrus, Bernstein, Peter R, Rumsey, William L, Aharony, David, Alelyunas, Yun, Russell, Daniel J, Potts, William, Sherwood, Scott A, Shen, Lihong, Dedinas, Robert F, Palmer, William E, Russell, Keith

“…We have previously described a series of antagonists that showed high potency and selectivity for the NK1 receptor. However, these compounds also had the…”
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Naphtho[2,1-b][1,5] and [1,2-f][1,4]oxazocines as selective NK1 antagonists by OHNMACHT, Cyrus J, ALBERT, Jeffrey S, BERNSTEIN, Peter R, RUMSEY, William L, MASEK, Brian B, DEMBOFSKY, Bruce T, KOETHER, Gerard M, ANDISIK, Donald W, AHARONY, David

“…Previously we reported on the synthesis and properties of a series of highly potent piperidinyl 2-subsituted-3-cyano-1-naphthamide NK1 antagonists that…”
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Effects of airborne toxicants on pulmonary function and mitochondrial DNA damage in rodent lungs by Rumsey, William L, Bolognese, Brian, Davis, Alicia B, Flamberg, Pearl L, Foley, Joseph P, Katchur, Steven R, Kotzer, Charles J, Osborn, Ruth R, Podolin, Patricia L

“…Inhalation of airborne toxicants such as cigarette smoke and ozone is a shared health risk among the world's populations. The use of toxic herbicides like…”
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3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent by Kerns, Jeffrey K, Busch-Petersen, Jakob, Fu, Wei, Boehm, Jeffrey C, Nie, Hong, Muratore, Michael, Bullion, Ann, Lin, Guoliang, Li, Huijie, Davis, Roderick, Lin, Xichen, Lakdawala, Ami S, Cousins, Rick, Field, Rita, Payne, Jeremy, Miller, David D, Bamborough, Paul, Christopher, John A, Baldwin, Ian, Osborn, Ruth R, Yonchuk, John, Webb, Edward, Rumsey, William L

“…IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the…”
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Discovery of novel, orally active dual NK1/NK2 antagonists by BERNSTEIN, Peter R, AHARONY, David, KOSMIDER, Benedict J, KIRKLAND, Karin, OHNMACHT, Cyrus J, POTTS, William, RUMSEY, William L, LIHONG SHEN, SHENVI, Ashok, SHERWOOD, Scott, STOLLMAN, David, RUSSELL, Keith, ALBERT, Jeffrey S, ANDISIK, Donald, BARTHLOW, Herbert G, BIALECKI, Russell, DAVENPORT, Timothy, DEDINAS, Robert F, DEMBOFSKY, Bruce T, KOETHER, Gerard

“…Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2…”
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4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy by Liddle, John, Bamborough, Paul, Barker, Michael D., Campos, Sebastien, Chung, Chun-Wa, Cousins, Rick P.C., Faulder, Paul, Heathcote, Michelle L., Hobbs, Heather, Holmes, Duncan S., Ioannou, Chris, Ramirez-Molina, Cesar, Morse, Mary A., Osborn, Ruth, Payne, Jeremy J., Pritchard, John M., Rumsey, William L., Tape, Daniel T., Vicentini, Giorgia, Whitworth, Caroline, Williamson, Rick A.

“…The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in…”
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The Role of IκB Kinase 2, but Not Activation of NF-κB, in the Release of CXCR3 Ligands from IFN-γ-Stimulated Human Bronchial Epithelial Cells by Tudhope, Susan J., Catley, Matthew C., Fenwick, Peter S., Russell, Richard E. K., Rumsey, William L., Newton, Robert, Barnes, Peter J., Donnelly, Louise E.

“…The severity of chronic obstructive pulmonary disease correlates with increased numbers of cytotoxic CD8+ T lymphocytes in the lung parenchyma. CD8+ T…”
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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β by Miller, David D., Bamborough, Paul, Christopher, John A., Baldwin, Ian R., Champigny, Aurelie C., Cutler, Geoffrey J., Kerns, Jeffrey K., Longstaff, Timothy, Mellor, Geoffrey W., Morey, James V., Morse, Mary A., Nie, Hong, Rumsey, William L., Taggart, John J.

“…The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by…”
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Design and optimization of cyclized NK1 antagonists with controlled atropisomeric properties by Albert, Jeffrey S, Ohnmacht, Cyrus, Bernstein, Peter R, Rumsey, William L, Aharony, David, Masek, Brian B, Dembofsky, Bruce T, Koether, Gerard M, Potts, William, Evenden, John L

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Imaging of Phosphorescence: A Novel Method for Measuring Oxygen Distribution in Perfused Tissue by Rumsey, William L., Vanderkooi, Jane M., Wilson, David F.

“…The imaging of phosphorescence provides a method for monitoring oxygen distribution within the vascular system of intact tissues. Isolated rat livers were…”
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Adaptation to hypoxia alters energy metabolism in rat heart by Rumsey, W L, Abbott, B, Bertelsen, D, Mallamaci, M, Hagan, K, Nelson, D, Erecinska, M

“…The present study characterized metabolic changes in the heart associated with long-term exposure to hypoxia, a potent stimulus for pulmonary hypertension and…”
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Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors by Rumsey, W L, Aharony, D, Bialecki, R A, Abbott, B M, Barthlow, H G, Caccese, R, Ghanekar, S, Lengel, D, McCarthy, M, Wenrich, B, Undem, B, Ohnmacht, C, Shenvi, A, Albert, J S, Brown, F, Bernstein, P R, Russell, K

“…The tachykinins, substance P, neurokinin A, and neurokinin B, have been implicated in many diseases. The present study evaluated the pharmacological properties…”
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3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IIK-β by MILLER, David D, BAMBOROUGH, Paul, MORSE, Mary A, HONG NIE, RUMSEY, William L, TAGGART, John J, CHRISTOPHER, John A, BALDWIN, Ian R, CHAMPIGNY, Aurelie C, CUTLER, Geoffrey J, KERNS, Jeffrey K, LONGSTAFF, Timothy, MELLOR, Geoffrey W, MOREY, James V

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The role of IkappaB kinase 2, but not activation of NF-kappaB, in the release of CXCR3 ligands from IFN-gamma-stimulated human bronchial epithelial cells by Tudhope, Susan J, Catley, Matthew C, Fenwick, Peter S, Russell, Richard E K, Rumsey, William L, Newton, Robert, Barnes, Peter J, Donnelly, Louise E

“…The severity of chronic obstructive pulmonary disease correlates with increased numbers of cytotoxic CD8(+) T lymphocytes in the lung parenchyma. CD8(+) T…”
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