Journal
CURRENT OPINION IN CHEMICAL BIOLOGY
Volume 4, Issue 1, Pages 40-46Publisher
CURRENT BIOLOGY LTD
DOI: 10.1016/S1367-5931(99)00049-6
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It is generally difficult to block protein-protein interactions with small-molecule drugs. A novel pharmaceutical development strategy to block protein interactions is emerging: targeted covalent modification to sterically block interactions. By this approach, compounds first interact non-covalently with a specific target protein. This interaction juxtaposes a weakly reactive group of the drug with a target amino acid sidechain, which then react by virtue of their high local concentration.
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