Inhibition of Human Immunodeficiency Virus Type 1 Tat- trans -Activation-Responsive Region Interaction by an Antiviral Quinolone Derivative-Reference-Cited by-同舟云学术

Inhibition of Human Immunodeficiency Virus Type 1 Tat- trans -Activation-Responsive Region Interaction by an Antiviral Quinolone Derivative

Published:2004-05 Issue:5 Volume:48 Page:1895-1899
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Richter Sara¹,Parolin Cristina²,Gatto Barbara¹,Del Vecchio Claudia²,Brocca-Cofano Egidio³,Fravolini Arnaldo⁴,Palù Giorgio²,Palumbo Manlio¹

Affiliation:

1. Department of Pharmaceutical Sciences

2. Department of Histology, Microbiology and Medical Biotechnologies, Section of Microbiology and Virology, University of Padua, 35131 Padua

3. Department of Experimental and Diagnostic Medicine, Section of Microbiology, University of Ferrara, 44100 Ferrara

4. Department of Pharmaceutical Chemistry and Technology, University of Perugia, 06123 Perugia, Italy

Abstract

ABSTRACT WM5, a 6-aminoquinolone derivative, binds with high affinity to the bulge of the trans -activation-responsive region (TAR), whereas it displays low binding affinity for the loop and stem regions of TAR and for random RNA and DNA sequences. Furthermore, WM5 disrupts the natural protein-nucleic acid complex with a 50% inhibitory concentration in the low micromolar range in both in vitro and in vivo assays.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.48.5.1895-1899.2004

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