In Vitro Evaluation of Bis-3-Chloropiperidines as RNA Modulators Targeting TAR and TAR-Protein Interaction |
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| Authors: | Alice Sosic Giulia Olivato Caterina Carraro Richard Gttlich Dan Fabris Barbara Gatto |
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| Affiliation: | 1.Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Francesco Marzolo 5, 35131 Padova, Italy; (A.S.); (G.O.); (C.C.);2.Institute of Organic Chemistry, Justus Liebig University Giessen, Heinrich-Buff-Ring 17, 35392 Giessen, Germany;3.Department of Chemistry, University of Connecticut, 55 North Eagleville Rd., Storrs, CT 06269, USA; |
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| Abstract: | After a long limbo, RNA has gained its credibility as a druggable target, fully earning its deserved role in the next generation of pharmaceutical R&D. We have recently probed the trans-activation response (TAR) element, an RNA stem–bulge–loop domain of the HIV-1 genome with bis-3-chloropiperidines (B-CePs), and revealed the compounds unique behavior in stabilizing 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 analytical approaches for the study of multicomponent RNA-based interactions. |
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| Keywords: | RNA targeting RNA-based interactions bis-3-chloropiperidines |
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