Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

In vitro Evaluation of Bis-3-chloropiperidines as RNA Modulators Targeting TAR and TAR-protein Interaction

Version 1 : Received: 12 December 2021 / Approved: 14 December 2021 / Online: 14 December 2021 (11:13:29 CET)

A peer-reviewed article of this Preprint also exists.

Sosic, A.; Olivato, G.; Carraro, C.; Göttlich, R.; Fabris, D.; Gatto, B. In Vitro Evaluation of Bis-3-Chloropiperidines as RNA Modulators Targeting TAR and TAR-Protein Interaction. Int. J. Mol. Sci. 2022, 23, 582. Sosic, A.; Olivato, G.; Carraro, C.; Göttlich, R.; Fabris, D.; Gatto, B. In Vitro Evaluation of Bis-3-Chloropiperidines as RNA Modulators Targeting TAR and TAR-Protein Interaction. Int. J. Mol. Sci. 2022, 23, 582.

Journal reference: Int. J. Mol. Sci. 2022, 23, 582
DOI: 10.3390/ijms23020582

Abstract

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.

Keywords

RNA targeting; RNA-based interactions; bis-3-chloropiperidines

Subject

CHEMISTRY, Medicinal Chemistry

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