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Therapeutic Exploitation of GPR18: Beyond the Cannabinoids?

Paula Morales, Ana Lago-Fernandez, Dow P. Hurst, Noori Sotudeh, Eugen Brailoiu, Patricia H. Reggio, Mary E. Abood, Nadine Jagerovic

2020Journal of Medicinal Chemistry57 citationsDOIOpen Access PDF

Abstract

GPR18 is a G-protein-coupled receptor that belongs to the orphan class A family. Even though it shares low sequence homology with the cannabinoid receptors CB1R and CB2R, a growing body of research suggests its relationship with the endocannabinoid system, not only because it is able to recognize cannabinoid ligands but also because of its expression and ability to heteromerize with CBRs. In this review, we aim to analyze the biological relevance, reported modulators, and structural features of GPR18. In order to guide future drug design in this field, highlights from molecular modeling of GPR18 will be provided.

Topics & Concepts

GPR18Cannabinoid receptorCannabinoidChemistryCannabinoid receptor antagonistHomology modelingComputational biologyPharmacologyReceptorBiochemistryBiologyAgonistEnzymeCannabis and Cannabinoid ResearchReceptor Mechanisms and SignalingPancreatic function and diabetes
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