Search Results - "Cockett, Mark I"

Safety and efficacy of anti-PD-L1 therapy in the woodchuck model of HBV infection by Balsitis, Scott, Gali, Volodymyr, Mason, Pamela J, Chaniewski, Susan, Levine, Steven M, Wichroski, Michael J, Feulner, Michael, Song, Yunling, Granaldi, Karen, Loy, James K, Thompson, Chris M, Lesniak, Jacob A, Brockus, Catherine, Kishnani, Narendra, Menne, Stephan, Cockett, Mark I, Iyer, Renuka, Mason, Stephen W, Tenney, Daniel J

“…Immune clearance of Hepatitis B virus (HBV) is characterized by broad and robust antiviral T cell responses, while virus-specific T cells in chronic hepatitis…”
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A novel small molecule inhibitor of hepatitis C virus entry by Baldick, Carl J, Wichroski, Michael J, Pendri, Annapurna, Walsh, Ann W, Fang, Jie, Mazzucco, Charles E, Pokornowski, Kevin A, Rose, Ronald E, Eggers, Betsy J, Hsu, Mayla, Zhai, Weixu, Zhai, Guangzhi, Gerritz, Samuel W, Poss, Michael A, Meanwell, Nicholas A, Cockett, Mark I, Tenney, Daniel J

“…Small molecule inhibitors of hepatitis C virus (HCV) are being developed to complement or replace treatments with pegylated interferons and ribavirin, which…”
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Antiviral Properties of HIV-1 Capsid Inhibitor GSK878 by Wang, Chunfu, Huang, Haichang, Mallon, Kirsten, Valera, Lourdes, Parcella, Kyle, Cockett, Mark I, Kadow, John F, Gillis, Eric P, Krystal, Mark, Fridell, Robert A

“…GSK878 is a newly described HIV-1 inhibitor that binds to the mature capsid (CA) hexamer in a pocket originally identified as the binding site of the…”
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High-throughput screening and rapid inhibitor triage using an infectious chimeric Hepatitis C virus by Wichroski, Michael J, Fang, Jie, Eggers, Betsy J, Rose, Ronald E, Mazzucco, Charles E, Pokornowski, Kevin A, Baldick, Carl J, Anthony, Monique N, Dowling, Craig J, Barber, Lauren E, Leet, John E, Beno, Brett R, Gerritz, Samuel W, Agler, Michele L, Cockett, Mark I, Tenney, Daniel J

“…The recent development of a Hepatitis C virus (HCV) infectious virus cell culture model system has facilitated the development of whole-virus screening assays…”
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Transcriptional profiling of the dose response: a more powerful approach for characterizing drug activities by Ji, Rui-Ru, de Silva, Heshani, Jin, Yisheng, Bruccoleri, Robert E, Cao, Jian, He, Aiqing, Huang, Wenjun, Kayne, Paul S, Neuhaus, Isaac M, Ott, Karl-Heinz, Penhallow, Becky, Cockett, Mark I, Neubauer, Michael G, Siemers, Nathan O, Ross-Macdonald, Petra

“…The dose response curve is the gold standard for measuring the effect of a drug treatment, but is rarely used in genomic scale transcriptional profiling due to…”
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RGS7 Is Palmitoylated and Exists as Biochemically Distinct Forms by Rose, Jeremy J., Taylor, Jackie B., Shi, Jing, Cockett, Mark I., Jones, Philip G., Hepler, John R.

“…: Regulator of G protein signaling (RGS) proteins are GTPase‐activating proteins that modulate neurotransmitter and G protein signaling. RGS7 and its binding…”
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Discovery of BMS-955176, a Second Generation HIV‑1 Maturation Inhibitor with Broad Spectrum Antiviral Activity by Regueiro-Ren, Alicia, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Swidorski, Jacob J, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Beno, Brett R, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Hanumegowda, Umesh, Dicker, Ira B

“…HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad…”
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Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176) by Regueiro-Ren, Alicia, Swidorski, Jacob J, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R, Arora, Vinod, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B

“…GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb…”
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The activity of the tissue inhibitors of metalloproteinases is regulated by C-terminal domain interactions: A kinetic analysis of the inhibition of gelatinase A by Willenbrock, Frances, Crabbe, Thomas, Slocombe, Patrick M, Sutton, Chris W, Docherty, Andrew J. P, Cockett, Mark I, O'Shea, Mark, Brocklehurst, Keith, Phillips, Ian R, Murphy, Gillian

“…The cloning and expression of the full-length tissue inhibitor of metalloproteinase 2 (TIMP-2), delta 187-194TIMP-2, and delta 128-194TIMP-2 and the…”
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Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing by Sun, Li-Qiang, Mull, Eric, Zheng, Barbara, D’Andrea, Stanley, Zhao, Qian, Wang, Alan Xiangdong, Sin, Ny, Venables, Brian L, Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Cocuzza, Anthony, Bilder, Donna M, Mathur, Arvind, Rampulla, Richard, Chen, Bang-Chi, Palani, Theerthagiri, Ganesan, Sivakumar, Arunachalam, Pirama Nayagam, Falk, Paul, Levine, Steven, Chen, Chaoqun, Friborg, Jacques, Yu, Fei, Hernandez, Dennis, Sheaffer, Amy K, Knipe, Jay O, Han, Yong-Hae, Schartman, Richard, Donoso, Maria, Mosure, Kathy, Sinz, Michael W, Zvyaga, Tatyana, Rajamani, Ramkumar, Kish, Kevin, Tredup, Jeffrey, Klei, Herbert E, Gao, Qi, Ng, Alicia, Mueller, Luciano, Grasela, Dennis M, Adams, Stephen, Loy, James, Levesque, Paul C, Sun, Huabin, Shi, Hong, Sun, Lucy, Warner, William, Li, Danshi, Zhu, Jialong, Wang, Ying-Kai, Fang, Hua, Cockett, Mark I, Meanwell, Nicholas A, McPhee, Fiona, Scola, Paul M

“…The discovery of a back-up to the hepatitis C virus NS3 protease inhibitor asunaprevir (2) is described. The objective of this work was the identification of a…”
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The N-terminal domain of tissue inhibitor of metalloproteinases retains metalloproteinase inhibitory activity by Murphy, Gillian, Houbrechts, Annick, Cockett, Mark I, Williamson, Richard A, O'Shea, Mark, Docherty, Andrew J. P

“…Recombinant tissue inhibitor of metalloproteinases (TIMP-1) and a truncated version containing only the three N-terminal loops, delta 127-184TIMP, have been…”
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Functionalized triazines as potent HCV entry inhibitors by Mull, Eric S., Sun, Li-Qiang, Zhao, Qian, Eggers, Betsy, Pokornowski, Kevin, Zhai, Guangzhi, Rajamani, Ramkumar, Jenkins, Susan, Kramer, Melissa, Wang, Ying-Kai, Fang, Hua, Tenney, Daniel, Baldick, Carl J., Cockett, Mark I., Meanwell, Nicholas A., Scola, Paul M.

“…[Display omitted] A series of potent and novel acylsulfonamide-bearing triazines were synthesized and the structure-activity relationships (SARs) as HCV entry…”
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Regional distribution of regulators of G-protein signaling (RGS) 1, 2, 13, 14, 16, and GAIP messenger ribonucleic acids by in situ hybridization in rat brain by Grafstein-Dunn, Ellen, Young, Kathleen H., Cockett, Mark I., Khawaja, Xavier Z.

“…Regulators of G-protein signaling (RGS) proteins are a novel family of GTPase-activating proteins that interact with Gα subunits of the Gi/o, Gz, Gq and G…”
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Different Domain Interactions Are Involved in the Binding of Tissue Inhibitors of Metalloproteinases to Stromelysin-1 and Gelatinase A by Nguyen, Quang, Willenbrock, Frances, Cockett, Mark I, O'Shea, Mark, Docherty, Andrew J. P, Murphy, Gillian

“…The matrix metalloproteinases gelatinase A and stromelysin-1 have definable N-terminal (catalytic) and C-terminal domains. In order to analyze their…”
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NMR Structure of Free RGS4 Reveals an Induced Conformational Change upon Binding Gα by Moy, Franklin J, Chanda, Pranab K, Cockett, Mark I, Edris, Wade, Jones, Philip G, Mason, Kim, Semus, Simon, Powers, Robert

“…Heterotrimeric guanine nucleotide-binding proteins (G-proteins) are transducers in many cellular transmembrane signaling systems where regulators of G-protein…”
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Cloning and tissue distribution of the human G protein β5 cDNA by Jones, Philip G, Lombardi, Stephen J, Cockett, Mark I

“…Heterotrimeric G proteins integrate signals between receptors and effector proteins. We have cloned the human β5 subunit from a human brain cDNA library. The…”
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New Generation Dopaminergic Agents. 1. Discovery of a Novel Scaffold Which Embraces the D2 Agonist Pharmacophore. Structure−Activity Relationships of a Series of 2-(Aminomethyl)chromans by Mewshaw, Richard E, Kavanagh, Joseph, Stack, Gary, Marquis, Karen L, Shi, Xiaojie, Kagan, Michael Z, Webb, Michael B, Katz, Alan H, Park, Anna, Kang, Young H, Abou-Gharbia, Magid, Scerni, Rosemary, Wasik, Theodore, Cortes-Burgos, Luz, Spangler, Taylor, Brennan, Julie A, Piesla, Michael, Mazandarani, Hossein, Cockett, Mark I, Ochalski, Rafal, Coupet, Joseph, Andree, Terrance H

“…A series of 2-(aminomethyl)chromans (2-AMCs) was synthesized and evaluated for their affinity and selectivity for both the high- and low-affinity agonist…”
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Mutation of the Active Site Glutamic Acid of Human Gelatinase A: Effects on Latency, Catalysis, and the Binding of Tissue Inhibitor of Metalloproteinases-1 by Crabbe, Thomas, Zucker, Stanley, Cockett, Mark I, Willenbrock, Frances, Tickle, Simon, O'Connell, James P, Scothern, Janeen M, Murphy, Gillian, Docherty, Andrew J. P

“…Human gelatinase A, a member of the matrix metalloproteinase family, is secreted from cells as the M(r) 72,000 latent precursor, progelatinase A. The autolytic…”
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Design, Synthesis, and SAR of C‑3 Benzoic Acid, C‑17 Triterpenoid Derivatives. Identification of the HIV‑1 Maturation Inhibitor 4‑((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)‑3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro‑1H‑cyclopenta[a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176) by Regueiro-Ren, Alicia, Swidorski, Jacob J., Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L., Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R., Arora, Vinod, Huang, Xiaohua S., Rahematpura, Sandhya, Parker, Dawn D., Haskell, Roy, Santone, Kenneth S., Cockett, Mark I., Krystal, Mark, Meanwell, Nicholas A., Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B.

“…GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb…”
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Enhanced neuronal differentiation of NTera-2 cells expressing neuronally restricted β2 adrenergic receptor by Fennell, Myles, Khawaja, Xavier Z, Cockett, Mark I, Wood, Andrew

“…NTera-2/D1 (NT2) is a human teratocarcinoma cell line which can be cultured as a dividing population of precursor cells that can be manipulated with retinoic…”
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