This Article Full Text Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Reprints and Permissions Copyright Information Books from ASM Press MicrobeWorld Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Richter, S. Articles by Palumbo, M. Search for Related Content PubMed PubMed Citation Articles by Richter, S. Articles by Palumbo, M.

 Previous Article  |  Next Article 

Antimicrobial Agents and Chemotherapy, May 2004, p. 1895-1899, Vol. 48, No. 5
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.5.1895-1899.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

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

Department of Pharmaceutical Sciences,¹ Department of Histology, Microbiology and Medical Biotechnologies, Section of Microbiology and Virology, University of Padua, 35131 Padua,² Department of Experimental and Diagnostic Medicine, Section of Microbiology, University of Ferrara, 44100 Ferrara,³ Department of Pharmaceutical Chemistry and Technology, University of Perugia, 06123 Perugia, Italy⁴

Received 4 September 2003/ Returned for modification 6 November 2003/ Accepted 8 January 2004

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.

This article has been cited by other articles:

• Stevens, M., Pollicita, M., Pannecouque, C., Verbeken, E., Tabarrini, O., Cecchetti, V., Aquaro, S., Perno, C. F., Fravolini, A., De Clercq, E., Schols, D., Balzarini, J. (2007). Novel In Vivo Model for the Study of Human Immunodeficiency Virus Type 1 Transcription Inhibitors: Evaluation of New 6-Desfluoroquinolone Derivatives. Antimicrob. Agents Chemother. 51: 1407-1413 [Abstract] [Full Text]  
• Stevens, M., Balzarini, J., Tabarrini, O., Andrei, G., Snoeck, R., Cecchetti, V., Fravolini, A., De Clercq, E., Pannecouque, C. (2005). Cell-dependent interference of a series of new 6-aminoquinolone derivatives with viral (HIV/CMV) transactivation. J Antimicrob Chemother 56: 847-855 [Abstract] [Full Text]  
• Nguyen, T., Hamby, A., Massa, S. M. (2005). Clioquinol down-regulates mutant huntingtin expression in vitro and mitigates pathology in a Huntington's disease mouse model. Proc. Natl. Acad. Sci. USA 102: 11840-11845 [Abstract] [Full Text]  
• Daelemans, D., Pannecouque, C., Pavlakis, G. N., Tabarrini, O., De Clercq, E. (2005). A Novel and Efficient Approach to Discriminate between Pre- and Post-Transcription HIV Inhibitors. Mol. Pharmacol. 67: 1574-1580 [Abstract] [Full Text]