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Erratum: Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis (Chemical Biology and Drug Design (2007) 69, (298-313)
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Orientador(es)
Resumo(s)
There is a clinical need for HIV protease inhibitors
that can evade resistance mutations. One possible
approach to designing such inhibitors relies upon
the crystallographic observation that the sub strates of HIV protease occupy a rather constant
region within the binding site. In particular, it has
been hypothesized that inhibitors which lie within
this region will tend to resist clinically relevant
mutations. The present study offers the first pros pective evaluation of this hypothesis, via compu tational design of inhibitors predicted to conform
to the substrate envelope, followed by synthesis
and evaluation against wild-type and mutant pro teases, as well as structural studies of complexes
of the designed inhibitors with HIV protease. The
results support the utility of the substrate envel ope hypothesis as a guide to the design of robust
protease inhibitors.
Descrição
Palavras-chave
AIDS Crystal Drug design Inhibitor Protease Erratum . Faculdade de Ciências Exatas e da Engenharia
Contexto Educativo
Citação
Editora
Wiley