Open AccessTherapeutic Exploitation of GPR18: Beyond the Cannabinoids?
Author(s) -
Paula Morales,
Ana Lago-Fernandez,
Dow P. Hurst,
Noori Sotudeh,
Eugen Brǎiloiu,
Patricia H. Reggio,
Mary E. Abood,
Nadine Jagerovic
Publication year - 2020
Publication title -
journal of medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.01
H-Index - 261
eISSN - 1520-4804
pISSN - 0022-2623
DOI - 10.1021/acs.jmedchem.0c00926
Subject(s) - gpr18 , cannabinoid receptor , cannabinoid , chemistry , homology modeling , cannabinoid receptor antagonist , computational biology , pharmacology , receptor , biochemistry , biology , antagonist , enzyme
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 1 R and CB 2 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 structural features of GPR18. In order to guide future drug design in this field, highlights from molecular modeling of GPR18 will be provided.