Design, synthesis, and in vitro activity of peptidomimetic inhibitors of myeloid differentiation factor 88
| Autor: | Marica Sassano, Davide Vignola, Vito Ruggiero, M.G. Quaglia, Giancarlo Basile, M. Pia Zibella, Rita De Santis, Mauro Semproni, Domenico Mastroianni, Andrea Ciacci, Paolo Carminati, Nicola Fanto, Valentina Bombardi, Grazia Gallo |
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| Rok vydání: | 2008 |
| Předmět: |
Models
Molecular Peptidomimetic Saccharomyces cerevisiae Cell Line Structure-Activity Relationship Two-Hybrid System Techniques Drug Discovery Humans Receptor Transcription factor Toll-like receptor Effector Chemistry Molecular Mimicry Toll-Like Receptors NF-kappa B Signal transducing adaptor protein Receptors Interleukin-1 Stereoisomerism Protein Structure Tertiary Biochemistry Myeloid Differentiation Factor 88 Molecular Medicine Signal transduction Oligopeptides Signal Transduction |
| Zdroj: | Journal of medicinal chemistry. 51(5) |
| ISSN: | 0022-2623 |
| Popis: | We describe the design and synthesis of a peptidomimetic library derived from the heptapeptide Ac-RDVLPGT-NH 2, belonging to the Toll/IL-1 receptor (TIR) domain of the adaptor protein MyD88 and effective in inhibiting its homodimerization. The ability of the peptidomimetics to inhibit protein-protein interaction was assessed by yeast 2-hybrid assay and further validated in a mammalian cell system by evaluating the inhibition of NF-kappaB activation, a transcription factor downstream of MyD88 signaling pathway that allows production of essential effector molecules for immune and inflammatory responses. |
| Databáze: | OpenAIRE |
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