Chemical Biology Lecture
- Prof. Benjamin Cravatt (The Scripps Research Institute)
- Thursday 23 June 2016
2333 CC Leiden
- Havinga Lecture Hall
Prof. Cravatt is heading the department of Chemical Physiology at the Scripps Research Institute (La Jolla, USA). He is one of the world-leading experts in chemical biology and founding father of activity-based proteomics and its application to drug discovery. He has used this technology to develop chemical tools to study the endocannabinoid system. Another prime example of his work on target-lead discovery using covalent fragments was published in Nature this week.
Activity-based proteomics - applications for enzyme and inhibitor discovery
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, the Chemical Physiology group of Prof. Cravatt has 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, Prof. Cravatt will describe the application of ABPP and complementary proteomic methods to discover and functionally annotate enzyme activities in mammalian physiology and disease, with a special emphasis on enzymes involved in metabolic disorders. Prof. Cravatt will also present competitive ABPP platforms for developing selective inhibitors for these enzymes and discuss ongoing challenges that face researchers interested in assigning protein function using chemoproteomic methods.