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Viruses. 2009 Dec;1(3):1209-39. doi: 10.3390/v1031209. Epub 2009 Dec 11.

Current and Novel Inhibitors of HIV Protease.

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  • 1Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Gilead Sciences and IOCB Research Center, Flemingovo n. 2, 166 10, Prague 6, Czech Republic; E-Mails: (J.P.); (P.R.).


The design, development and clinical success of HIV protease inhibitors represent one of the most remarkable achievements of molecular medicine. This review describes all nine currently available FDA-approved protease inhibitors, discusses their pharmacokinetic properties, off-target activities, side-effects, and resistance profiles. The compounds in the various stages of clinical development are also introduced, as well as alternative approaches, aiming at other functional domains of HIV PR. The potential of these novel compounds to open new way to the rational drug design of human viruses is critically assessed.


HAART; HIV protease; alternative inhibitors; pharmacokinetic boosting; protease dimerization; protease inhibitors; resistance development

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