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Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules
[Image: see text] A unique series of biologically active chemical probes that selectively inhibit NF-κB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical too...
| Autores principales: | , , , , , , , , , , |
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| Formato: | Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2010
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2887059/ https://www.ncbi.nlm.nih.gov/pubmed/20481485 http://dx.doi.org/10.1021/jm1000248 |
| _version_ | 1782182500985995264 |
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| author | Peddibhotla, Satyamaheshwar Shi, Ranxin Khan, Pasha Smith, Layton H. Mangravita-Novo, Arianna Vicchiarelli, Michael Su, Ying Okolotowicz, Karl J. Cashman, John R. Reed, John C. Roth, Gregory P. |
| author_facet | Peddibhotla, Satyamaheshwar Shi, Ranxin Khan, Pasha Smith, Layton H. Mangravita-Novo, Arianna Vicchiarelli, Michael Su, Ying Okolotowicz, Karl J. Cashman, John R. Reed, John C. Roth, Gregory P. |
| author_sort | Peddibhotla, Satyamaheshwar |
| collection | PubMed |
| description | [Image: see text] A unique series of biologically active chemical probes that selectively inhibit NF-κB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical tools to be used in gaining further understanding on the cellular mechanisms driven by B and T cell antigen receptors. Starting from the founding member of this chemical series 1a (notated in PubChem as CID-2858522), we report the chemical synthesis, SAR studies, and pharmacological profiling of this pathway-selective inhibitor of NF-κB activation. |
| format | Text |
| id | pubmed-2887059 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2010 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-28870592010-06-17 Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules Peddibhotla, Satyamaheshwar Shi, Ranxin Khan, Pasha Smith, Layton H. Mangravita-Novo, Arianna Vicchiarelli, Michael Su, Ying Okolotowicz, Karl J. Cashman, John R. Reed, John C. Roth, Gregory P. J Med Chem [Image: see text] A unique series of biologically active chemical probes that selectively inhibit NF-κB activation induced by protein kinase C (PKC) pathway activators have been identified through a cell-based phenotypic reporter gene assay. These 2-aminobenzimidazoles represent initial chemical tools to be used in gaining further understanding on the cellular mechanisms driven by B and T cell antigen receptors. Starting from the founding member of this chemical series 1a (notated in PubChem as CID-2858522), we report the chemical synthesis, SAR studies, and pharmacological profiling of this pathway-selective inhibitor of NF-κB activation. American Chemical Society 2010-05-18 2010-06-24 /pmc/articles/PMC2887059/ /pubmed/20481485 http://dx.doi.org/10.1021/jm1000248 Text en Copyright © 2010 American Chemical Society http://pubs.acs.org This is an open-access article distributed under the ACS AuthorChoice Terms & Conditions. Any use of this article, must conform to the terms of that license which are available at http://pubs.acs.org. |
| spellingShingle | Peddibhotla, Satyamaheshwar Shi, Ranxin Khan, Pasha Smith, Layton H. Mangravita-Novo, Arianna Vicchiarelli, Michael Su, Ying Okolotowicz, Karl J. Cashman, John R. Reed, John C. Roth, Gregory P. Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title | Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title_full | Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title_fullStr | Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title_full_unstemmed | Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title_short | Inhibition of Protein Kinase C-Driven Nuclear Factor-κB Activation: Synthesis, Structure−Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules |
| title_sort | inhibition of protein kinase c-driven nuclear factor-κb activation: synthesis, structure−activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2887059/ https://www.ncbi.nlm.nih.gov/pubmed/20481485 http://dx.doi.org/10.1021/jm1000248 |
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