In vitro Evaluation of Bis-3-chloropiperidines as RNA Modulators Targeting TAR and TAR-protein Interaction
| Autor: | Alice Sosic, Giulia Olivato, Caterina Carraro, Richard Göttlich, Dan Fabris, Barbara Gatto |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
QH301-705.5
medicinal_chemistry Organic Chemistry RNA targeting RNA-based interactions bis-3-chloropiperidines General Medicine Nucleocapsid Proteins Article Catalysis Computer Science Applications Inorganic Chemistry Chemistry Piperidines HIV-1 Nucleic Acid Conformation RNA Viral Biology (General) Physical and Theoretical Chemistry QD1-999 Molecular Biology Bis-3-chloropiperidines Spectroscopy |
| Zdroj: | International Journal of Molecular Sciences; Volume 23; Issue 2; Pages: 582 International Journal of Molecular Sciences, Vol 23, Iss 582, p 582 (2022) International Journal of Molecular Sciences |
| Popis: | After a long limbo, RNA has gained its credibility as a druggable target, fully earning its de-served role in the next-generation area of pharmaceutical R&D. We have recently probed the Trans-Activation Response element (TAR), a RNA stem–bulge–loop domain of the HIV-1 genome with bis-3-chloropiperidines (B-CePs), and revealed the compounds unique behavior in stabiliz-ing TAR structure, thus impairing in vitro the chaperone activity of the HIV-1 nucleocapsid (NC) protein. Seeking to elucidate the determinants of B-CePs inhibition, we have further characterized here their effects on the target TAR and its NC recognition, while developing quantitative analyti-cal approaches for the study of multicomponent RNA-based interactions. |
| Databáze: | OpenAIRE |
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