(P2) Activity-Based Proteomics–Applications for Enzyme and Inhibitor Discovery
Year: 2013
Type: article
Abstract: Genome sequencing projects have revealed that eukaryotic and prokaryotic organisms universally possess a huge number of uncharacterized enzymes. The functional annotation of enzymatic pathways thus represents a grand challenge for researchers in the genome era. To address this problem, we have introduced chemical proteomic and metabolomic technologies that globally profile enzyme activities in complex biological systems. These methods include activity-based protein profiling (ABPP), which utilizes active site-directed chemical probes to determine the functional state of large numbers of enzymes in native proteomes. In this lecture, I will describe the integrated application of ABPP and complementary metabolomic methods to discover and functionally annotate enzyme activities in mammalian systems, including cancer and the nervous system. I will also present competitive ABPP platforms for developing selective inhibitors for poorly characterized enzymes and discuss ongoing challenges that face researchers interested in assigning protein function using chemoproteomic methods.
Source: Europe PMC (PubMed Central)
Author: Benjamin F. Cravatt
Language: English
Subfield: Spectroscopy
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W970149221