Medicinal chemistry campaign to synthesize synaptamide analogs (GPR110)

National Center For Advancing Translational Sciences

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Abstract

During this period, the team has continued to pursue cell-based assays to measure G-protein coupled receptor 110 (GPR110) activation and drive structure-activity-relationship (SAR) of a set of novel synaptamide analogs. Additionally, a cell-based high-throughput screen to identify novel small molecule modulators of GPR110 is being developed. SAR studies have identified a potent, selective and metabolically stable GPR110 agonist that has demonstrated promising activity in several models of neuronal damage, such traumatic brain injury and optic nerve damage. Evaluation of this compound in mouse models of multiple sclerosis is underway.