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Nature 453, 861-862 (12 June 2008) | doi:10.1038/453861a; Published online 11 June 2008

Biochemistry: Molecular cloaking devices

Thomas Kodadek1

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Protease enzymes cut other proteins into pieces, but some can be blocked by inhibitors. One such inhibitor binds to the substrate rather than the enzyme, suggesting a new tactic for drug discovery.

Most drug developers try to identify small molecules that bind to a target enzyme with high affinity and specificity. Binding usually occurs at the enzyme's active site; by nestling into this molecular pocket, the drug blocks binding of the enzyme's natural substrate.

  1. Thomas Kodadek is in the Departments of Internal Medicine and Molecular Biology, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA.
    e-mail: Email: thomas.kodadek@utsouthwestern.edu

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