A novel class of potent NF-κB signaling inhibitors
| Autor: | Kristina Wolf, Jan Mies, Johann Leban, Markus H.J. Seifert, Sandra Rath, Viola Trentinaglia, Marcel Baierl, Astrid Gotschlich, Kerstin Kronthaler |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Reporter gene
Virtual screening Quantitative structure–activity relationship medicine.drug_class Chemistry Organic Chemistry Clinical Biochemistry NF-kappa B Quantitative Structure-Activity Relationship Pharmaceutical Science NF-κB Biochemistry Anti-inflammatory In vitro Pathway signaling Nf κb signaling chemistry.chemical_compound Drug Discovery medicine Molecular Medicine Molecular Biology Cell Proliferation Signal Transduction |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:5858-5862 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.08.022 |
| Popis: | A novel class of NF-kappaB pathway signaling inhibitors was discovered by virtual screening, medicinal chemistry, and QSAR analysis. An initial set of compounds inhibited NF-kappaB signaling in a whole cell reporter gene assay in the micro-molar range. Activity was improved step by step by medicinal chemistry to yield nano-molar signaling inhibitors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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