Current and Novel Inhibitors of HIV Protease
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, sid...
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MDPI AG
2009-12-01
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| Series: | Viruses |
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| Online Access: | http://www.mdpi.com/1999-4915/1/3/1209/ |
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doaj-70031e2c4d9a450186517972e0a002e92020-11-24T23:16:57ZengMDPI AGViruses1999-49152009-12-01131209123910.3390/v1031209Current and Novel Inhibitors of HIV ProteaseJan KonvalinkaLadislav MachalaPavlína ŘezáčováJana PokornáThe 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. http://www.mdpi.com/1999-4915/1/3/1209/HIV proteaseprotease inhibitorsHAARTresistance developmentpharmacokinetic boostingprotease dimerizationalternative inhibitors |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Jan Konvalinka Ladislav Machala Pavlína Řezáčová Jana Pokorná |
| spellingShingle |
Jan Konvalinka Ladislav Machala Pavlína Řezáčová Jana Pokorná Current and Novel Inhibitors of HIV Protease Viruses HIV protease protease inhibitors HAART resistance development pharmacokinetic boosting protease dimerization alternative inhibitors |
| author_facet |
Jan Konvalinka Ladislav Machala Pavlína Řezáčová Jana Pokorná |
| author_sort |
Jan Konvalinka |
| title |
Current and Novel Inhibitors of HIV Protease |
| title_short |
Current and Novel Inhibitors of HIV Protease |
| title_full |
Current and Novel Inhibitors of HIV Protease |
| title_fullStr |
Current and Novel Inhibitors of HIV Protease |
| title_full_unstemmed |
Current and Novel Inhibitors of HIV Protease |
| title_sort |
current and novel inhibitors of hiv protease |
| publisher |
MDPI AG |
| series |
Viruses |
| issn |
1999-4915 |
| publishDate |
2009-12-01 |
| description |
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. |
| topic |
HIV protease protease inhibitors HAART resistance development pharmacokinetic boosting protease dimerization alternative inhibitors |
| url |
http://www.mdpi.com/1999-4915/1/3/1209/ |
| work_keys_str_mv |
AT jankonvalinka currentandnovelinhibitorsofhivprotease AT ladislavmachala currentandnovelinhibitorsofhivprotease AT pavlinarezacova currentandnovelinhibitorsofhivprotease AT janapokorna currentandnovelinhibitorsofhivprotease |
| _version_ |
1725585605261262848 |