Search Results - "Wrobel, Jay E."

Small-molecule probes targeting the viral PPxY-host Nedd4 interface block egress of a broad range of RNA viruses by Han, Ziying, Lu, Jianhong, Liu, Yuliang, Davis, Benjamin, Lee, Michael S, Olson, Mark A, Ruthel, Gordon, Freedman, Bruce D, Schnell, Matthias J, Wrobel, Jay E, Reitz, Allen B, Harty, Ronald N

“…Budding of filoviruses, arenaviruses, and rhabdoviruses is facilitated by subversion of host proteins, such as Nedd4 E3 ubiquitin ligase, by viral PPxY late…”
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Calcium Regulation of Hemorrhagic Fever Virus Budding: Mechanistic Implications for Host-Oriented Therapeutic Intervention by Han, Ziying, Madara, Jonathan J, Herbert, Andrew, Prugar, Laura I, Ruthel, Gordon, Lu, Jianhong, Liu, Yuliang, Liu, Wenbo, Liu, Xiaohong, Wrobel, Jay E, Reitz, Allen B, Dye, John M, Harty, Ronald N, Freedman, Bruce D

“…Hemorrhagic fever viruses, including the filoviruses (Ebola and Marburg) and arenaviruses (Lassa and Junín viruses), are serious human pathogens for which…”
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Design, Synthesis, and SAR of New Pyrrole-Oxindole Progesterone Receptor Modulators Leading to 5-(7-Fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348) by Fensome, Andrew, Adams, William R, Adams, Andrea L, Berrodin, Tom J, Cohen, Jeff, Huselton, Christine, Illenberger, Arthur, Kern, Jeffrey C, Hudak, Valerie A, Marella, Michael A, Melenski, Edward G, McComas, Casey C, Mugford, Cheryl A, Slayden, Ov D, Yudt, Matthew, Zhang, Zhiming, Zhang, Puwen, Zhu, Yuan, Winneker, Richard C, Wrobel, Jay E

“…We have continued to explore the 3,3-dialkyl-5-aryloxindole series of progesterone receptor (PR) modulators looking for new agents to be used in female…”
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Antiretroviral Drug Discovery Targeting the HIV-1 Nef Virulence Factor by Emert-Sedlak, Lori A, Shi, Haibin, Tice, Colin M, Chen, Li, Alvarado, John J, Shu, Sherry T, Du, Shoucheng, Thomas, Catherine E, Wrobel, Jay E, Reitz, Allen B, Smithgall, Thomas E

“…While antiretroviral drugs have transformed the lives of HIV-infected individuals, chronic treatment is required to prevent rebound from viral reservoir cells…”
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Compound FC-10696 Inhibits Egress of Marburg Virus by Han, Ziying, Ye, Hong, Liang, Jingjing, Shepley-McTaggart, Ariel, Wrobel, Jay E, Reitz, Allen B, Whigham, Alison, Kavelish, Katrina N, Saporito, Michael S, Freedman, Bruce D, Shtanko, Olena, Harty, Ronald N

“…Marburg virus (MARV) VP40 protein (mVP40) directs egress and spread of MARV, in part, by recruiting specific host WW domain-containing proteins via its…”
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Quinoxaline-based inhibitors of Ebola and Marburg VP40 egress by Loughran, H. Marie, Han, Ziying, Wrobel, Jay E., Decker, Sarah E., Ruthel, Gordon, Freedman, Bruce D., Harty, Ronald N., Reitz, Allen B.

“…[Display omitted] We prepared a series of quinoxalin-2-mercapto-acetyl-urea analogs and evaluated them for their ability to inhibit viral egress in our Marburg…”
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In vivo and in vitro characterization of a first-in-class novel azole analog that targets pregnane X receptor activation by Venkatesh, Madhukumar, Wang, Hongwei, Cayer, Julie, Leroux, Melissa, Salvail, Dany, Das, Bhaskar, Wrobel, Jay E, Mani, Sridhar

“…The pregnane X receptor (PXR) is a master regulator of xenobiotic clearance and is implicated in deleterious drug interactions (e.g., acetaminophen…”
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A method for C2 acylation of 1,3-indandiones by Larsen, Brian J., Rosano, Robert J., Ford-Hutchinson, Thomas A., Reitz, Allen B., Wrobel, Jay E.

“…The 1,3-indandione scaffold is an important structural motif used in the preparation of a large number of industrial chemical and pharmaceutical compounds…”
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Tight-Binding Hydroxypyrazole HIV‑1 Nef Inhibitors Suppress Viral Replication in Donor Mononuclear Cells and Reverse Nef-Mediated MHC‑I Downregulation by Shi, Haibin, Tice, Colin M, Emert-Sedlak, Lori, Chen, Li, Li, Wing Fai, Carlsen, Marianne, Wrobel, Jay E, Reitz, Allen B, Smithgall, Thomas E

“…The HIV-1 Nef accessory factor is critical to the viral life cycle in vivo and promotes immune escape of infected cells via downregulation of cell-surface…”
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Synthesis and evaluation of orally active small molecule HIV-1 Nef antagonists by Emert-Sedlak, Lori A., Loughran, H. Marie, Shi, Haibin, Kulp, John L., Shu, Sherry T., Zhao, Jielu, Day, Billy W., Wrobel, Jay E., Reitz, Allen B., Smithgall, Thomas E.

“…[Display omitted] The HIV-1 Nef accessory factor enhances viral replication and promotes immune system evasion of HIV-infected cells, making it an attractive…”
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Dipeptide Prodrugs of the Glutamate Modulator Riluzole by Pelletier, Jeffrey C., Chen, Suzie, Bian, Haiyan, Shah, Raj, Smith, Garry R., Wrobel, Jay E., Reitz, Allen B.

“…We have previously reported a prodrug strategy based on the marketed drug riluzole (2-amino-6-trifluoromethoxybenzothiazole), associated with the benefits of…”
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Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1 by Hu, Baihua, Jetter, James W., Wrobel, Jay E., Antrilli, Thomas M., Bauer, Jean S., Di, Li, Polakowski, Sergiusz, Jain, Uday, Crandall, David L.

“…[Display omitted] We synthesized and evaluated a novel series of 2-carboxylic acid indole-based inhibitors of plasminogen activator inhibitor-1 (PAI-1)…”
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Intramolecular rearrangement of α-amino acid amide derivatives of 2-aminobenzothiazoles by Pelletier, Jeffrey C., Velvadapu, Venkata, McDonnell, Mark E., Wrobel, Jay E., Reitz, Allen B.

“…We have found that α-amino acid amide derivatives of 2-aminobenzothiazoles undergo a time-dependent, thermal rearrangement in which the amine group attacks the…”
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Acinetobacter baumannii OxPhos inhibitors as selective anti-infective agents by Rubin, Harvey, Selwood, Trevor, Yano, Takahiro, Weaver, Damian G, Loughran, H Marie, Costanzo, Michael J, Scott, Richard W, Wrobel, Jay E, Freeman, Katie B, Reitz, Allen B

“…The Gram-negative bacterium Acinetobacter baumannii is an opportunistic pathogen in humans and infections are poorly treated by current therapy. Recent…”
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Improvement of Physiochemical Properties of the Tetrahydroazepinoindole Series of Farnesoid X Receptor (FXR) Agonists: Beneficial Modulation of Lipids in Primates by Lundquist, Joseph T, Harnish, Douglas C, Kim, Callain Y, Mehlmann, John F, Unwalla, Rayomand J, Phipps, Kristin M, Crawley, Matthew L, Commons, Thomas, Green, Daniel M, Xu, Weixin, Hum, Wah-Tung, Eta, Julius E, Feingold, Irene, Patel, Vikram, Evans, Mark J, Lai, KehDih, Borges-Marcucci, Lisa, Mahaney, Paige E, Wrobel, Jay E

“…In an effort to develop orally active farnesoid X receptor (FXR) agonists, a series of tetrahydroazepinoindoles with appended solubilizing amine…”
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Identification of Phenylsulfone-Substituted Quinoxaline (WYE-672) as a Tissue Selective Liver X-receptor (LXR) Agonist by Hu, Baihua, Unwalla, Rayomand J, Goljer, Igor, Jetter, James W, Quinet, Elaine M, Berrodin, Thomas J, Basso, Michael D, Feingold, Irene B, Nilsson, Annika Goos, Wilhelmsson, Anna, Evans, Mark J, Wrobel, Jay E

“…A series of phenyl sulfone substituted quinoxaline were prepared and the lead compound 13 (WYE-672) was shown to be a tissue selective LXR Agonist. Compound 13…”
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(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A Wingless β-Catenin Agonist That Increases Bone Formation Rate by Pelletier, Jeffrey C, Lundquist, Joseph T, Gilbert, Adam M, Alon, Nipa, Bex, Frederick J, Bhat, Bheem M, Bursavich, Mattew G, Coleburn, Valerie E, Felix, Luciana A, Green, Daniel M, Green, Paula, Hauze, Diane B, Kharode, Yogendra P, Lam, Ho-Sun, Lockhead, Susan R, Magolda, Ronald L, Matteo, Jeanne J, Mehlmann, John F, Milligan, Colleen, Murrills, Richard J, Pirrello, Jennifer, Selim, Sally, Sharp, Michael C, Unwalla, Ray J, Vera, Matthew D, Wrobel, Jay E, Yaworsky, Paul, Bodine, Peter V. N

“…A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a…”
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Discovery of 6-({4-[2-(4-tert-Butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): An Orally Active Antagonist of the Gonadotropin Releasing Hormone Receptor (GnRH-R) by Pelletier, Jeffrey C, Chengalvala, Murty V, Cottom, Joshua E, Feingold, Irene B, Green, Daniel M, Hauze, Diane B, Huselton, Christine A, Jetter, James W, Kopf, Gregory S, Lundquist, Joseph T, Magolda, Ronald L, Mann, Charles W, Mehlmann, John F, Rogers, John F, Shanno, Linda K, Adams, William R, Tio, Cesario O, Wrobel, Jay E

“…A potent, highly insoluble, GnRH antagonist with a 2-phenyl-4-piperazinylbenzimidazole template and a quinoxaline-2,3-dione pharmacophore was modified to…”
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Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor by Vera, Matthew D., Lundquist, Joseph T., Chengalvala, Murty V., Cottom, Joshua E., Feingold, Irene B., Garrick, Lloyd M., Green, Daniel M., Hauze, Diane B., Mann, Charles W., Mehlmann, John F., Rogers, John F., Shanno, Linda, Wrobel, Jay E., Pelletier, Jeffrey C.

“…A series of bicycloheterocyclic replacements for the previously described benzimidazole template were prepared and tested for GnRH activity. Antagonism of the…”
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Pyrrole[2,3- d]azepino compounds as agonists of the farnesoid X receptor (FXR) by Mehlmann, John F., Crawley, Matthew L., Lundquist, Joseph T., Unwalla, Ray J., Harnish, Douglas C., Evans, Mark J., Kim, Callain Y., Wrobel, Jay E., Mahaney, Paige E.

“…The rational design and discovery of a new series of pyrrole[2,3- d]azepino FXR agonists with aqueous solubility and improved pharmaceutical properties is…”
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