Darunavir, a Conceptually New HIV-1 Protease Inhibitor for the Treatment of Drug-resistant HIV
作者： Arun K. Ghosh , Zachary L. Dawson , Hiroaki Mitsuya
DOI: 10.1016/J.BMC.2007.09.010
关键词:
摘要: Our structure-based design strategies which specifically target the HIV-1 protease backbone, resulted in a number of exceedingly potent nonpeptidyl inhibitors. One these inhibitors, darunavir (TMC114), contains privileged, designed high-affinity P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF). Darunavir has recently been approved for treatment HIV/AIDS patients harboring multidrug-resistant variants that do not respond to previously existing HAART regimens.
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