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Current and Novel Inhibitors of HIV Protease
Institute 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
AIDS Center, Department of Infectious Diseases, University Hospital Bulovka, Budínova 2, 120 00, Prague 8, Czech Republic
Department of Infectious Diseases, Third Faculty of Medicine, Charles University in Prague, Prague, Czech Republic
Institute of Molecular Genetics, Academy of Sciences of the Czech Republic, Flemingovo n. 2, 166 10, Prague 6, Czech Republic
Department of Biochemistry, Faculty of Science, Charles University in Prague, Hlavova 8, 128 43, Prague 2, Czech Republic
* Author to whom correspondence should be addressed.
Received: 8 October 2009; in revised form: 7 December 2009 / Accepted: 7 December 2009 / Published: 11 December 2009
Abstract: 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.
Keywords: HIV protease; protease inhibitors; HAART; resistance development; pharmacokinetic boosting; protease dimerization; alternative inhibitors
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MDPI and ACS Style
Pokorná, J.; Machala, L.; Řezáčová, P.; Konvalinka, J. Current and Novel Inhibitors of HIV Protease. Viruses 2009, 1, 1209-1239.
Pokorná J, Machala L, Řezáčová P, Konvalinka J. Current and Novel Inhibitors of HIV Protease. Viruses. 2009; 1(3):1209-1239.
Pokorná, Jana; Machala, Ladislav; Řezáčová, Pavlína; Konvalinka, Jan. 2009. "Current and Novel Inhibitors of HIV Protease." Viruses 1, no. 3: 1209-1239.