There is an unmet need for new drugs treating metabolic syndrome (MetS) and its underlying causes. Many signaling pathways are implicated in chronic conditions leading to MetS and its sequelae. The role of the endocannabinoid (EC) system in modulating the pathophysiology of such conditions is well-documented. The selective antagonism of central cannabinoid receptors acting via CB1 receptor has shown to reduce food intake, ameliorating insulin resistance and alleviating fibrosis. With the withdrawal of first-in-class, brain-penetrant, CB1 blocker rimonabant due to psychiatric side-effects, novel approaches are needed to harness the potential of CB1R blockade for therapeutic benefits without CNS effects. The laboratory’s efforts in developing new medicinal chemistry design approaches and generation of novel pharmacological tools leading to peripherally restricted CB1R antagonist clinical candidate will be highlighted. The lab has also developed a new, green protocol to expand the toolbox of new chemistry motifs available for drug discovery. Utilization of this methodology in relation to tailored polypharmacological approaches targeting peripheral CB1 receptor blockade will be discussed in detail.

Novel drug discovery approaches targeting the endocannabinoid system

Fall 2022 abstracts, posters, and presentations will launch in mid-September.

ACS Fall 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.