Activity-based probes: discovering new biology and new drug targets.
The development and application of chemical technologies enabling direct analysis of enzyme activity in living systems has undergone explosive growth in recent years. Activity-based protein profiling (ABPP) is a key constituent of this broad field, and is among the most powerful and mature chemical proteomic technologies. This tutorial review introduces the essential features of ABPP and the design and application of activity-based probes (ABPs) from drug target elucidation and in vivo visualisation of enzyme activity to comprehensive profiling of the catalytic content of living systems, and the discovery of new biological pathways.
Heal
William P
WP
Department of Chemistry, South Kensington Campus, Imperial College, London, SW7 2AZ, UK.
Dang
T H Tam
TH
Tate
Edward W
EW
D000818:Animals; D020169:Caspases / Q000737:chemistry / Q000378:metabolism; D002384:Catalysis; D003952:Diagnostic Imaging; D005456:Fluorescent Dyes / Q000737:chemistry; D015335:Molecular Probes / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000737:chemistry; D015398:Signal Transduction; D013499:Surface Properties
D005456:Fluorescent Dyes; D015335:Molecular Probes; D010455:Peptides; D004364:Pharmaceutical Preparations; D020169:Caspases