期刊
VIRUSES-BASEL
卷 1, 期 3, 页码 1209-1239出版社
MDPI
DOI: 10.3390/v1031209
关键词
HIV protease; protease inhibitors; HAART; resistance development; pharmacokinetic boosting; protease dimerization; alternative inhibitors
类别
资金
- Ministry of Education of the Czech Republic [1M0508]
- Grant Agency of the Academy of Science of the Czech Republic [IAAX00320901]
- European Union [03769]
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.
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