Abstract
HIV protease (PR) is a key target for antiviral drugs, and HIV protease inhibitors (PIs) are a prime example of successful structure-based drug design. PIs show clear therapeutic benefits, but their efficacy can be compromised by poor bioavailabilitity, unwanted side effects, and most importantly, development of antiviral drug resistance. Therefore, the quest for novel, highly active compounds with improved resistance profiles, better pharmacokinetic properties, and fewer adverse effects continues. In particular, the problem of cross-resistance could be circumvented by identifying novel compounds that show different binding modes to HIV PR than the current clinical inhibitors.
Keywords: Proteinase, proteolytic processing, virostatic, rational drug design, resistance development.
Current Pharmaceutical Design
Title:Unorthodox Inhibitors of HIV Protease: Looking Beyond Active-site-directed Peptidomimetics
Volume: 20 Issue: 21
Author(s): Jiri Schimer and Jan Konvalinka
Affiliation:
Keywords: Proteinase, proteolytic processing, virostatic, rational drug design, resistance development.
Abstract: HIV protease (PR) is a key target for antiviral drugs, and HIV protease inhibitors (PIs) are a prime example of successful structure-based drug design. PIs show clear therapeutic benefits, but their efficacy can be compromised by poor bioavailabilitity, unwanted side effects, and most importantly, development of antiviral drug resistance. Therefore, the quest for novel, highly active compounds with improved resistance profiles, better pharmacokinetic properties, and fewer adverse effects continues. In particular, the problem of cross-resistance could be circumvented by identifying novel compounds that show different binding modes to HIV PR than the current clinical inhibitors.
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Cite this article as:
Schimer Jiri and Konvalinka Jan, Unorthodox Inhibitors of HIV Protease: Looking Beyond Active-site-directed Peptidomimetics, Current Pharmaceutical Design 2014; 20 (21) . https://dx.doi.org/10.2174/13816128113199990634
DOI https://dx.doi.org/10.2174/13816128113199990634 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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