Abstract
Here we report the X-ray structures of chemically synthesized HIV-1 protease and the inactive [D25N]HIV-1 protease complexed with the ketomethylene isostere inhibitor Ac–Thr–Ile–Nle ψ[CO–CH 2]Nle–Gln–Arg.amide at 1.4 and 1.8 Å resolution, respectively. In complex with the active enzyme, the keto-group was found to be converted into the hydrated gem-diol, while the structure of the complex with the inactive D25N enzyme revealed an intact keto-group. These data support the general acid–general base mechanism for HIV-1 protease catalysis.
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