Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
7694178 | Current Opinion in Chemical Biology | 2016 | 9 Pages |
Abstract
In conventional chemical genetics, cell-active small-molecules directly block protein activity, altering phenotype. However these molecules may not be sufficiently selective or effective at modulating complex epigenetic pathways. By mutating the target protein, and creating a mutant-selective inhibitor, the bump-and-hole approach can provide single-target selectivity. PROTAC molecules direct their target to proteosomal degradation by recruiting an E3 ubiquitin ligase, resulting in more efficacious target downregulation.238
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Authors
Andrew C Runcie, Kwok-Ho Chan, Michael Zengerle, Alessio Ciulli,