Search Results - "Cywin, Charles L"

National Institutes of Health Blueprint Neurotherapeutics Network: Results to Date and Path Forward by Cywin, Charles L., Tamiz, Amir P.

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Design, Synthesis, and Evaluation of Nonretinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease by Cioffi, Christopher L, Dobri, Nicoleta, Freeman, Emily E, Conlon, Michael P, Chen, Ping, Stafford, Douglas G, Schwarz, Daniel M. C, Golden, Kathy C, Zhu, Lei, Kitchen, Douglas B, Barnes, Keith D, Racz, Boglarka, Qin, Qiong, Michelotti, Enrique, Cywin, Charles L, Martin, William H, Pearson, Paul G, Johnson, Graham, Petrukhin, Konstantin

“…Accumulation of lipofuscin in the retina is associated with pathogenesis of atrophic age-related macular degeneration and Stargardt disease. Lipofuscin…”
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Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease by Cioffi, Christopher L, Racz, Boglarka, Freeman, Emily E, Conlon, Michael P, Chen, Ping, Stafford, Douglas G, Schwarz, Daniel M. C, Zhu, Lei, Kitchen, Douglas B, Barnes, Keith D, Dobri, Nicoleta, Michelotti, Enrique, Cywin, Charles L, Martin, William H, Pearson, Paul G, Johnson, Graham, Petrukhin, Konstantin

“…Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic bisretinoid…”
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A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket by Tong, Liang, Pav, Susan, White, Della M, Rogers, Sheri, Crane, Kathy M, Cywin, Charles L, Brown, Maryanne L, Pargellis, Christopher A

“…The crystal structure of human p38 mitogen-activated protein (MAP) kinase in complex with a potent and highly specific pyridinyl-imidazole inhibitor has been…”
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Hit to Lead Account of the Discovery of a New Class of Inhibitors of Pim Kinases and Crystallographic Studies Revealing an Unusual Kinase Binding Mode by Qian, Kevin, Wang, Lian, Cywin, Charles L, Farmer, Bennett T, Hickey, Eugene, Homon, Carol, Jakes, Scott, Kashem, Mohammed A, Lee, George, Leonard, Scott, Li, Jun, Magboo, Ronald, Mao, Wang, Pack, Edward, Peng, Charlene, Prokopowicz, Anthony, Welzel, Morgan, Wolak, John, Morwick, Tina

“…A series of inhibitors of Pim-2 kinase identified by high-throughput screening is described. Details of the hit validation and lead generation process and…”
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Effect of Structural Modification of Enol−Carboxamide-Type Nonsteroidal Antiinflammatory Drugs on COX-2/COX-1 Selectivity by Lazer, Edward S, Miao, Clara K, Cywin, Charles L, Sorcek, Ronald, Wong, Hin-Chor, Meng, Zhaoxing, Potocki, Ian, Hoermann, MaryAnn, Snow, Roger J, Tschantz, Matt A, Kelly, Terence A, McNeil, Daniel W, Coutts, Simon J, Churchill, Laurie, Graham, Anne G, David, Eva, Grob, Peter M, Engel, Wolfhard, Meier, Hans, Trummlitz, Günter

“…Meloxicam (5), an NSAID in the enol−carboxamide class, was developed on the basis of its antiinflammatory activity and relative safety in animal models. In…”
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Evolution of the Thienopyridine Class of Inhibitors of IκB Kinase-β:  Part I:  Hit-to-Lead Strategies by Morwick, Tina, Berry, Angela, Brickwood, Janice, Cardozo, Mario, Catron, Katrina, DeTuri, Molly, Emeigh, Jonathan, Homon, Carol, Hrapchak, Matt, Jacober, Stephen, Jakes, Scott, Kaplita, Paul, Kelly, Terence A, Ksiazek, John, Liuzzi, Michel, Magolda, Ronald, Mao, Can, Marshall, Daniel, McNeil, Daniel, Prokopowicz, Anthony, Sarko, Christopher, Scouten, Erika, Sledziona, Cynthia, Sun, Sanxing, Watrous, Jane, Wu, Jiang Ping, Cywin, Charles L

“…High-throughput screening is routinely employed as a method for the identification of novel hit structures. Large numbers of active compounds are typically…”
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Hit-to-lead studies on benzimidazole inhibitors of ITK: Discovery of a novel class of kinase inhibitors by Snow, Roger J., Abeywardane, Asitha, Campbell, Scot, Lord, John, Kashem, Mohammed A., Khine, Hnin Hnin, King, Josephine, Kowalski, Jennifer A., Pullen, Steven S., Roma, Teresa, Roth, Gregory P., Sarko, Christopher R., Wilson, Noel S., Winters, Michael P., Wolak, John P., Cywin, Charles L.

“…Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents…”
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Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method by Kowalski, Jennifer A., Swinamer, Alan D., Muegge, Ingo, Eldrup, Anne B., Kukulka, Alison, Cywin, Charles L., De Lombaert, Stéphane

“…Rapid exploration of multi-dimensional SAR around a series of trisubstituted urea inhibitors of sEH was accomplished using a focused library approach. A…”
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Discovery of potent and selective PKC-θ inhibitors by Cywin, Charles L., Dahmann, Georg, Prokopowicz, Anthony S., Young, Erick R.R., Magolda, Ronald L., Cardozo, Mario G., Cogan, Derek A., DiSalvo, Darren, Ginn, John D., Kashem, Mohammed A., Wolak, John P., Homon, Carol A., Farrell, Thomas M., Grbic, Heather, Hu, Hanbo, Kaplita, Paul V., Liu, Lisa H., Spero, Denice M., Jeanfavre, Deborah D., O’Shea, Kathy M., White, Della M., Woska, Joseph R., Brown, Maryanne L.

“…An uHTS campaign was performed to identify selective inhibitors of PKC-θ. Initial triaging of the hit set based on selectivity and historical analysis led to…”
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Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account by Wu, Frank, Büttner, Frank H., Chen, Rhonda, Hickey, Eugene, Jakes, Scott, Kaplita, Paul, Kashem, Mohammed A., Kerr, Steven, Kugler, Stanley, Paw, Zofia, Prokopowicz, Anthony, Shih, Cheng-Kon, Snow, Roger, Young, Erick, Cywin, Charles L.

“…Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here,…”
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Hit to Lead Account of the Discovery of Bisbenzamide and Related Ureidobenzamide Inhibitors of Rho Kinase by Morwick, Tina, Büttner, Frank H, Cywin, Charles L, Dahmann, Georg, Hickey, Eugene, Jakes, Scott, Kaplita, Paul, Kashem, Mohammed A, Kerr, Steven, Kugler, Stanley, Mao, Wang, Marshall, Daniel, Paw, Zofia, Shih, Cheng-Kon, Wu, Frank, Young, Erick

“…A highly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidobenzamide series, both…”
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5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk) by Winters, Michael P, Robinson, Darius J, Khine, Hnin Hnin, Pullen, Steven S, Woska, Jr, Joseph R, Raymond, Ernest L, Sellati, Rosemarie, Cywin, Charles L, Snow, Roger J, Kashem, Mohammed A, Wolak, John P, King, Josephine, Kaplita, Paul V, Liu, Lisa H, Farrell, Thomas M, DesJarlais, Renee, Roth, Gregory P, Takahashi, Hidenori, Moriarty, Kevin J

“…A series of novel 5-aminomethyl-1H-benzimidazole based inhibitors of Itk were prepared. Structure-activity relationships, selectivity and cell activity are…”
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Design and Synthesis of Dipeptide Nitriles as Reversible and Potent Cathepsin S Inhibitors by Ward, Yancey D, Thomson, David S, Frye, Leah L, Cywin, Charles L, Morwick, Tina, Emmanuel, Michel J, Zindell, Renée, McNeil, Daniel, Bekkali, Younes, Hrapchak, Matt, DeTuri, Molly, Crane, Kathy, White, Della, Pav, Susan, Wang, Yong, Hao, Ming-Hong, Grygon, Christine A, Labadia, Mark E, Freeman, Dorothy M, Davidson, Walter, Hopkins, Jerry L, Brown, Maryanne L, Spero, Denice M

“…The specificity of the immune response relies on processing of foreign proteins and presentation of antigenic peptides at the cell surface. Inhibition of…”
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Discovery and SAR of novel [1,6]Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK) by Cywin, Charles L, Zhao, Bao-Ping, McNeil, Daniel W, Hrapchak, Matt, Prokopowicz, Anthony S, Goldberg, Daniel R, Morwick, Tina M, Gao, Amy, Jakes, Scott, Kashem, Mohammed, Magolda, Ronald L, Soll, Richard M, Player, Mark R, Bobko, Mark A, Rinker, James, DesJarlais, Renee L, Winters, Michael P

“…The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity…”
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An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity by Desai, Sudha N., White, Della M., O'Shea, Kathryn M., Brown, Maryanne L., Cywin, Charles L., Spero, Denice M., Panzenbeck, Maret J.

“…Cathepsin S is a major histocompatibility complex (MHC) class II associated invariant chain (Ii) degrading enzyme expressed in antigen presenting cells such as…”
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The design of potent hydrazones and disulfides as cathepsin S inhibitors by Cywin, Charles L, Firestone, Raymond A, McNeil, Daniel W, Grygon, Christine A, Crane, Kathryn M, White, Della M, Kinkade, Peter R, Hopkins, Jerry L, Davidson, Walter, Labadia, Mark E, Wildeson, Jessi, Morelock, Maurice M, Peterson, Jeffrey D, Raymond, Ernest L, Brown, Maryanne L, Spero, Denice M

“…The design and synthesis of dipeptidyl disulfides and dipeptidyl benzoylhydrazones as selective inhibitors of the cysteine protease Cathepsin S are described…”
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Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 7. 8-Arylethyldipyridodiazepinones as Potent Broad-Spectrum Inhibitors of Wild-Type and Mutant Enzymes by Klunder, Janice M, Hoermann, MaryAnn, Cywin, Charles L, David, Eva, Brickwood, Janice R, Schwartz, Racheline, Barringer, Kevin J, Pauletti, Daniel, Shih, Cheng-Kon, Erickson, David A, Sorge, Christopher L, Joseph, David P, Hattox, Susan E, Adams, Julian, Grob, Peter M

“…Like other nonnucleoside inhibitors of HIV-1 reverse transcriptase, the dipyridodiazepinone nevirapine (Viramune, 1) selects for drug resistant variants of…”
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Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones by Cywin, Charles L, Klunder, Janice M, Hoermann, MaryAnn, Brickwood, Janice R, David, Eva, Grob, Peter M, Schwartz, Racheline, Pauletti, Daniel, Barringer, Kevin J, Shih, Cheng-Kon, Sorge, Christopher L, Erickson, David A, Joseph, David P, Hattox, Susan E

“…Nevirapine (I) is the first human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitor to reach regulatory approval. As a…”
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Design and Synthesis of Dipeptide Nitriles as Reversible and Potent Cathepsin S Inhibitors by Ward, Yancey D, Thomson, David S, Frye, Leah L, Cywin, Charles L, Morwick, Tina, Emmanuel, Michel J, Zindell, Renée, McNeil, Daniel, Bekkali, Younes, Girardot, Marc, Hrapchak, Matt, DeTuri, Molly, Crane, Kathy, White, Della, Pav, Susan, Wang, Yong, Hao, Ming-Hong, Grygon, Christine A, Labadia, Mark E, Freeman, Dorothy M, Davidson, Walter, Hopkins, Jerry L, Brown, Maryanne L, Spero, Denice M

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