Year: 2015
Type: conference-paper
Abstract: Endocannabinoids play an essential role in human health and disease, regulating processes such as immunomodulation, energy balance and neurotransmission. Diacylglycerollipase-α (DAGL-α) is responsible for the production of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the central nervous system. It is a potential drug target for the treatment of obesity and neurodegenerative diseases. Currently, there are no selective inhibitors and activity-based probes available for its study. The identification of selective DAGL- inhibitors is hampered by a lack of assays that make use of endogenous DAGL- activity in proteomes. Determination of the selectivity of the inhibitors in native tissues is important, because DAGL- belongs to the class of serine hydrolases, containing more than 200 members with various physiological functions. Here, I will present a chemical biology approach to identify and characterize highly selective chemical probes to study the function of this protein both in vitro and in vivo.
Author: Marcelis Van der Selt
Language: English
Subfield: Pharmacology (medical)
Field: Medicine
Domain: Health Sciences
Open Access status: green
OpenAlex ID: W2802517687