Brought to life: targeted activation of enzyme function with small molecules View Full Text


Ontology type: schema:ScholarlyArticle      Open Access: True


Article Info

DATE

2009-03

AUTHORS

Anthony C. Bishop, Vincent L. Chen

ABSTRACT

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 that allow chemical-biology researchers to activate specific enzymes in a cellular context? In this review, we describe some recent advances in achieving targeted enzyme activation with small molecules. In addition to surveying progress in the identification and targeting of enzymes that contain natural allosteric-activation sites, we focus on recently developed protein-engineering strategies that allow researchers to render an enzyme of interest "activatable" by a pre-chosen compound. Three distinct strategies for targeting an engineered enzyme are discussed: direct chemical "rescue" of an intentionally inactivated enzyme, activation of an enzyme by targeting a de novo small-molecule-binding site, and the generation of activatable enzymes via fusion of target enzymes to previously characterized small-molecule-binding domains. More... »

PAGES

1-9

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s12154-008-0012-4

DOI

http://dx.doi.org/10.1007/s12154-008-0012-4

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1049682002

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/19568788


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