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Therapeutic Exploitation of GPR18: Beyond the Cannabinoids?


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.

SUBMITTER: Morales P 

PROVIDER: S-EPMC7949482 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Therapeutic Exploitation of GPR18: Beyond the Cannabinoids?

Morales Paula P   Lago-Fernandez Ana A   Hurst Dow P DP   Sotudeh Noori N   Brailoiu Eugen E   Reggio Patricia H PH   Abood Mary E ME   Jagerovic Nadine N  

Journal of medicinal chemistry 20200923 23


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 CB<sub>1</sub>R and CB<sub>2</sub>R, 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 s  ...[more]

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