科研之友
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摘要
Non-nucleoside reverse transcriptase inhibitors (NNRT1s) represent a chemically diverse class of HIV-1 specific antiretroviral drugs. NNRTIs are non competitive inhibitors of the HIV reverse transcriptase (RT) that bind to a hydrophobic pocket in the vicinity of the active site of RT and as such inhibit polymerization via an allosteric mechanism. Three representatives are currently approved at the EU level : nevirapine and efavirenz (first generation NNRTls) and the recently approved etravirine, a next generation NNRTI. A deep understanding of first generation NNRTI resistance mechanisms as well as a particular attention to chemical structure and binding modes has driven class optimization.
- 出版日期2008-10
