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Your search keyword '"Delaet, Nancy G.J."' showing total 3 results
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3 results on '"Delaet, Nancy G.J."'

1. Optimization of α-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site

Author

Montalban, Antonio Garrido, Boman, Erik, Chang, Chau-Dung, Ceide, Susana Conde, Dahl, Russell, Dalesandro, David, Delaet, Nancy G.J., Erb, Eric, Ernst, Justin T., Gibbs, Andrew, Kahl, Jeffrey, Kessler, Linda, Kucharski, Jeff, Lum, Christopher, Lundström, Jan, Miller, Stephen, Nakanishi, Hiroshi, Roberts, Edward, Saiah, Eddine, and Sullivan, Robert

Subjects
*ENZYME inhibitors, *MITOGEN-activated protein kinases, *ALLOSTERIC regulation, *ANTI-inflammatory agents, *CYTOKINES, *AMIDES, *DRUG development, *ALPHA-Ketoamides
Abstract

Abstract: We have optimized a novel series of potent p38 MAP kinase inhibitors based on an α-ketoamide scaffold through structure based design that due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME, in vivo PK and efficacy studies show these compounds to have drug-like characteristics and have resulted in the nomination of a development candidate which is currently in phase II clinical trials for the oral treatment of inflammatory conditions. [ABSTRACT FROM AUTHOR]

Published
2010
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2. ‘Reverse’ α-ketoamide-based p38 MAP kinase inhibitors

Author

Montalban, Antonio Garrido, Boman, Erik, Chang, Chau-Dung, Ceide, Susana Conde, Dahl, Russell, Dalesandro, David, Delaet, Nancy G.J., Erb, Eric, Gibbs, Andrew, Kahl, Jeff, Kessler, Linda, Lundström, Jan, Miller, Stephen, Nakanishi, Hiroshi, Roberts, Ed, Saiah, Eddine, Sullivan, Robert, Wang, Zhijun, and Larson, Christopher J.

Subjects
*ENZYME inhibitors, *MITOGEN-activated protein kinases, *CYTOKINES, *ANTI-inflammatory agents, *AMIDES, *PHARMACOLOGY, *ALPHA-Ketoamides
Abstract

Abstract: We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an α-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addition results in improve potencies against p38. [Copyright &y& Elsevier]

Published
2008
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3. The design and synthesis of novel α-ketoamide-based p38 MAP kinase inhibitors

Author

Montalban, Antonio Garrido, Boman, Erik, Chang, Chau-Dung, Ceide, Susana Conde, Dahl, Russell, Dalesandro, David, Delaet, Nancy G.J., Erb, Eric, Ernst, Justin T., Gibbs, Andrew, Kahl, Jeffrey, Kessler, Linda, Lundström, Jan, Miller, Stephen, Nakanishi, Hiroshi, Roberts, Edward, Saiah, Eddine, Sullivan, Robert, Wang, Zhijun, and Larson, Christopher J.

Subjects
*CELLULAR immunity, *CYTOKINES, *IMMUNOREGULATION, *CLONAL selection theory
Abstract

Abstract: We have identified a novel series of potent p38 MAP kinase inhibitors through structure-based design which due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME and in vivo PK studies show these compounds to have drug-like characteristics which could result in the development of an oral treatment for inflammatory conditions. [Copyright &y& Elsevier]

Published
2008
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