Search Results - "Ledeboer, Mark W."

Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit by Byrn, Randal A, Jones, Steven M, Bennett, Hamilton B, Bral, Chris, Clark, Michael P, Jacobs, Marc D, Kwong, Ann D, Ledeboer, Mark W, Leeman, Joshua R, McNeil, Colleen F, Murcko, Mark A, Nezami, Azin, Perola, Emanuele, Rijnbrand, Rene, Saxena, Kumkum, Tsai, Alice W, Zhou, Yi, Charifson, Paul S

“…VX-787 is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. Viral genetics…”
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Structural basis of TRPC4 regulation by calmodulin and pharmacological agents by Vinayagam, Deivanayagabarathy, Quentin, Dennis, Yu-Strzelczyk, Jing, Sitsel, Oleg, Merino, Felipe, Stabrin, Markus, Hofnagel, Oliver, Yu, Maolin, Ledeboer, Mark W, Nagel, Georg, Malojcic, Goran, Raunser, Stefan

“…Canonical transient receptor potential channels (TRPC) are involved in receptor-operated and/or store-operated Ca signaling. Inhibition of TRPCs by small…”
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Dual p38/JNK mitogen activated protein kinase inhibitors prevent ozone-induced airway hyperreactivity in guinea pigs by Verhein, Kirsten C, Salituro, Francesco G, Ledeboer, Mark W, Fryer, Allison D, Jacoby, David B

“…Ozone exposure causes airway hyperreactivity and increases hospitalizations resulting from pulmonary complications. Ozone reacts with the epithelial lining…”
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Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model by Yu, Maolin, Ledeboer, Mark W, Daniels, Matthew, Malojcic, Goran, Tibbitts, Thomas T, Coeffet-Le Gal, Marie, Pan-Zhou, Xin-Ru, Westerling-Bui, Amy, Beconi, Maria, Reilly, John F, Mundel, Peter, Harmange, Jean-Christophe

“…The nonselective Ca2+-permeable transient receptor potential (TRP) channels play important roles in diverse cellular processes, including actin remodeling and…”
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Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3‑Kinase γ by Collier, Philip N., Messersmith, David, Le Tiran, Arnaud, Bandarage, Upul K., Boucher, Christina, Come, Jon, Cottrell, Kevin M., Damagnez, Veronique, Doran, John D., Griffith, James P., Khare-Pandit, Suvarna, Krueger, Elaine B., Ledeboer, Mark W., Ledford, Brian, Liao, Yusheng, Mahajan, Sudipta, Moody, Cameron S., Roday, Setu, Wang, Tiansheng, Xu, Jinwang, Aronov, Alex M.

“…A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase…”
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Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors by Boyd, Michael J, Bandarage, Upul K, Bennett, Hamilton, Byrn, Randal R, Davies, Ioana, Gu, Wenxin, Jacobs, Marc, Ledeboer, Mark W, Ledford, Brian, Leeman, Joshua R, Perola, Emanuele, Wang, Tiansheng, Bennani, Youssef, Clark, Michael P, Charifson, Paul S

“…VX-787 is a first in class, orally bioavailable compound that offers unparalleled potential for the treatment of pandemic and seasonal influenza. As a part of…”
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Novel 2‑Substituted 7‑Azaindole and 7‑Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza by Bandarage, Upul K., Clark, Michael P., Perola, Emanuele, Gao, Huai, Jacobs, Marc D., Tsai, Alice, Gillespie, Jeffery, Kennedy, Joseph M., Maltais, François, Ledeboer, Mark W., Davies, Ioana, Gu, Wenxin, Byrn, Randal A., Nti Addae, Kwame, Bennett, Hamilton, Leeman, Joshua R., Jones, Steven M., O’Brien, Colleen, Memmott, Christine, Bennani, Youssef, Charifson, Paul S.

“…JNJ-63623872 (2) is a first-in-class, orally bioavailable compound that offers significant potential for the treatment of pandemic and seasonal influenza…”
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Transplanted organoids empower human preclinical assessment of drug candidate for the clinic by Westerling-Bui, Amy D., Fast, Eva Maria, Soare, Thomas W., Venkatachalan, Srinivasan, DeRan, Michael, Fanelli, Alyssa B., Kyrychenko, Sergii, Hoang, Hien, Corriea, Grinal M., Zhang, Wei, Yu, Maolin, Daniels, Matthew, Malojcic, Goran, Pan-Zhou, Xin-Ru, Ledeboer, Mark W., Harmange, Jean-Christophe, Emani, Maheswarareddy, Tibbitts, Thomas T., Reilly, John F., Mundel, Peter

“…Pharmacodynamic (PD) studies are an essential component of preclinical drug discovery. Current approaches for PD studies, including the analysis of novel…”
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Total Synthesis and Comparative Evaluation of Luzopeptin A−C and Quinoxapeptin A−C by Boger, Dale L, Ledeboer, Mark W, Kume, Masaharu, Searcey, Mark, Jin, Qing

“…Full details of the total syntheses of luzopeptin A−C and quinoxapeptin A−C, C 2-symmetric cyclic depsidecapeptides bearing two pendant heterocyclic…”
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Total Synthesis of Quinoxapeptin A-C: Establishment of Absolute Stereochemistry by Boger, Dale L., Ledeboer, Mark W., Kume, Masaharu, Jin, Qing

“…The relative and absolute stereochemistry of the naturally occurring potent HIV reverse transcriptase (RT) inhibitors 1 and 2, quinoxapeptin A and B, were…”
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Discovery of Novel, Orally Bioavailable β‑Amino Acid Azaindole Inhibitors of Influenza PB2 by Farmer, Luc J., Clark, Michael P., Boyd, Michael J., Perola, Emanuele, Jones, Steven M., Tsai, Alice, Jacobs, Marc D., Bandarage, Upul K., Ledeboer, Mark W., Wang, Tiansheng, Deng, Hongbo, Ledford, Brian, Gu, Wenxin, Duffy, John P., Bethiel, Randy S., Shannon, Dean, Byrn, Randal A., Leeman, Joshua R., Rijnbrand, Rene, Bennett, Hamilton B., O’Brien, Colleen, Memmott, Christine, Nti-Addae, Kwame, Bennani, Youssef L., Charifson, Paul S.

“…In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the…”
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A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors by Wang, Tiansheng, Ledeboer, Mark W., Duffy, John P., Pierce, Albert C., Zuccola, Harmon J., Block, Eric, Shlyakter, Dina, Hogan, James K., Bennani, Youssef L.

“…Pictet–Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole ( 11) or deazapurine ( 12) gave high yields of the…”
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Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole by Wang, Tiansheng, Duffy, John P, Wang, Jian, Halas, Summer, Salituro, Francesco G, Pierce, Albert C, Zuccola, Harmon J, Black, James R, Hogan, James K, Jepson, Scott, Shlyakter, Dina, Mahajan, Sudipta, Gu, Yong, Hoock, Thomas, Wood, Mark, Furey, Brinley F, Frantz, J. Daniel, Dauffenbach, Lisa M, Germann, Ursula A, Fan, Bin, Namchuk, Mark, Bennani, Youssef L, Ledeboer, Mark W

“…The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further…”
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2-Aminopyrazolo[1,5- a]pyrimidines as potent and selective inhibitors of JAK2 by Ledeboer, Mark W., Pierce, Albert C., Duffy, John P., Gao, Huai, Messersmith, David, Salituro, Francesco G., Nanthakumar, Suganthini, Come, Jon, Zuccola, Harmon J., Swenson, Lora, Shlyakter, Dina, Mahajan, Sudipta, Hoock, Thomas, Fan, Bin, Tsai, Wan-Jung, Kolaczkowski, Elaine, Carrier, Scott, Hogan, James K., Zessis, Richard, Pazhanisamy, S., Bennani, Youssef L.

“…The discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5- a]pyrimidines of potent and selective inhibitors of JAK2 is…”
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Asymmetric Reduction. A Convenient Method for the Reduction of Alkynyl Ketones by Parker, Kathlyn A, Ledeboer, Mark W

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Total Synthesis of Luzopeptins A−C by Boger, Dale L, Ledeboer, Mark W, Kume, Masaharu

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Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2 by Clark, Michael P, Ledeboer, Mark W, Davies, Ioana, Byrn, Randal A, Jones, Steven M, Perola, Emanuele, Tsai, Alice, Jacobs, Marc, Nti-Addae, Kwame, Bandarage, Upul K, Boyd, Michael J, Bethiel, Randy S, Court, John J, Deng, Hongbo, Duffy, John P, Dorsch, Warren A, Farmer, Luc J, Gao, Huai, Gu, Wenxin, Jackson, Katrina, Jacobs, Dylan H, Kennedy, Joseph M, Ledford, Brian, Liang, Jianglin, Maltais, François, Murcko, Mark, Wang, Tiansheng, Wannamaker, M. Woods, Bennett, Hamilton B, Leeman, Joshua R, McNeil, Colleen, Taylor, William P, Memmott, Christine, Jiang, Min, Rijnbrand, Rene, Bral, Christopher, Germann, Ursula, Nezami, Azin, Zhang, Yuegang, Salituro, Francesco G, Bennani, Youssef L, Charifson, Paul S

“…In our effort to develop agents for the treatment of influenza, a phenotypic screening approach utilizing a cell protection assay identified a series of…”
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Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases by Farmer, Luc J, Ledeboer, Mark W, Hoock, Thomas, Arnost, Michael J, Bethiel, Randy S, Bennani, Youssef L, Black, James J, Brummel, Christopher L, Chakilam, Ananthsrinivas, Dorsch, Warren A, Fan, Bin, Cochran, John E, Halas, Summer, Harrington, Edmund M, Hogan, James K, Howe, David, Huang, Hui, Jacobs, Dylan H, Laitinen, Leena M, Liao, Shengkai, Mahajan, Sudipta, Marone, Valerie, Martinez-Botella, Gabriel, McCarthy, Pamela, Messersmith, David, Namchuk, Mark, Oh, Luke, Penney, Marina S, Pierce, Albert C, Raybuck, Scott A, Rugg, Arthur, Salituro, Francesco G, Saxena, Kumkum, Shannon, Dean, Shlyakter, Dina, Swenson, Lora, Tian, Shi-Kai, Town, Christopher, Wang, Jian, Wang, Tiansheng, Wannamaker, M. Woods, Winquist, Raymond J, Zuccola, Harmon J

“…While several therapeutic options exist, the need for more effective, safe, and convenient treatment for a variety of autoimmune diseases persists. Targeting…”
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Corrigendum to “Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors” [Bioorg. Med. Chem. Lett. 25 (2015) 1990–1994] by Boyd, Michael J., Bandarage, Upul K., Bennett, Hamilton, Byrn, Randal R., Davies, Ioana, Gu, Wenxin, Jacobs, Marc, Ledeboer, Mark W., Ledford, Brian, Leeman, Joshua R., Perola, Emanuele, Wang, Tiansheng, Bennani, Youssef, Clark, Michael P., Charifson, Paul S.

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Corrigendum to “A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors” [Bioorg. Med. Chem. Lett. 20 (2010) 153] by Wang, Tiansheng, Ledeboer, Mark W., Duffy, John P., Salituro, Francesco G., Pierce, Albert C., Zuccola, Harmon J., Block, Eric, Shlyakter, Dina, Hogan, James K., Bennani, Youssef L.

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