Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine.
نویسندگان
چکیده
Designing selective inhibitors of proteases has proven problematic, in part because pharmacophores that confer potency exploit the conserved catalytic apparatus. We developed a fundamentally different approach by designing irreversible inhibitors that target noncatalytic cysteines that are structurally unique to a target in a protein family. We have successfully applied this approach to the important therapeutic target HCV protease, which has broad implications for the design of other selective protease inhibitors.
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ورودعنوان ژورنال:
- Nature chemical biology
دوره 7 1 شماره
صفحات -
تاریخ انتشار 2011