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Báo cáo khoa học: Crystal structures of HIV protease V82A and L90M mutants reveal changes in the indinavir-binding site

Chia sẻ: Nguyen Thang | Ngày: | Loại File: PDF | Số trang:9

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The crystal structures of the wild-type HIV-1 protease (PR) and the two resistant variants, PRV82Aand PRL90M,have been determined in complex with the antiviral drug, indi-navir, to gain insight into the molecular basis of drug resistance. V82A and L90M correspond to an active site mutation and nonactive site mutation, respectively. The inhibition (Ki)of PRV82Aand PRL90Mwas 3.3- and 0.16-fold, respectively, relative to the value for PR. They showed only a modest decrease, of 10–15%, in theirkcat /Kmvalues relative to PR. ...

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Nội dung Text: Báo cáo khoa học: Crystal structures of HIV protease V82A and L90M mutants reveal changes in the indinavir-binding site

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