Trapping moving targets with small molecules.
Ontology highlight
ABSTRACT:
SUBMITTER: Lee GM
PROVIDER: S-EPMC2981433 | biostudies-literature | 2009 Apr
REPOSITORIES: biostudies-literature
Publications
Trapping moving targets with small molecules.
Lee Gregory M GM Craik Charles S CS
Science (New York, N.Y.) 20090401 5924
Structure-based drug design traditionally uses static protein models as inspirations for focusing on "active" site targets. Allosteric regulation of biological macromolecules, however, is affected by both conformational and dynamic properties of the protein or protein complex and can potentially lead to more avenues for therapeutic development. We discuss the advantages of searching for molecules that conformationally trap a macromolecule in its inactive state. Although multiple methodologies ex ...[more]
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