Identification of GPR120 Beta-arrestin-2 Biased Agonists for the Treatment of Insulin resistance

National Center For Advancing Translational Sciences

Investigators

Abstract

Primary high-throughput screening was previously completed by the project team utilizing the optimized HTS-amenable assays. During this period, the project team has worked to build on the previous screening work by validating hit molecules, and assessing their effectiveness in downstream pathway regulation assays to confirm that observed activity is on-target with respect to GPR120. Downstream markers included inhibition of LPS-induced phosphorylation of JNK and IKKb, IkB degradation in mouse monocytes, and inhibition of cytokine secretion (TNF-a and IL-6) in response to LPS-induced inflammation in mouse monocytes.