Covalent modification as a strategy to block protein-protein interactions with small-molecule drugs |
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Authors: | Way J C |
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Affiliation: | The Molecular Sciences Institute, Lexigen Pharmaceuticals, Berkeley, Lexington, CA 94704, MA 02173, USA. jway@lexigenpharm.com. |
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Abstract: | 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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