Brought to life: targeted activation of enzyme function with small molecules.

摘要: Cell-permeable small molecules that are capable of activating particular enzymes would be invaluable tools for studying protein function in complex cell-signaling cascades. But, is it feasible to identify compounds allow chemical–biology researchers activate specific a cellular context? In this review, we describe some recent advances achieving targeted enzyme activation with molecules. addition surveying progress the identification and targeting contain natural allosteric-activation sites, focus on recently developed protein-engineering strategies render an interest “activatable” by pre-chosen compound. Three distinct engineered discussed: direct chemical “rescue” intentionally inactivated enzyme, de novo small-molecule-binding site, generation activatable via fusion target previously characterized domains.