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TMC114 (darunavir) is a promising clinical inhibitor of HIV-1 protease (PR) for treatment of drug resistant HIV/AIDS. We report the ultra-high 0.84 Å resolution crystal structure of the TMC114 complex with PR containing the drug-resistant mutation V32I (PR V32I ), and the 1.22 Å resolution structure of a complex with PR M46L . These structures show TMC114 bound at two distinct sites,...
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