The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor.

ABSTRACT: G protein-coupled receptors (GPCRs) play a predominant role in the drug discovery effort. These cell surface receptors are activated by a variety of specific ligands that bind to the orthosteric binding pocket located in the extracellular part of the receptor. In addition, the potential binding sites located on the surface of the receptor enable their allosteric modulation with critical consequences for their function and pharmacology. For decades, drug discovery focused on targeting the GPCR orthosteric binding sites. However, finding that GPCRs can be modulated allosterically opened a new venue for developing novel pharmacological modulators with higher specificity. Alternatively, focus on discovering of non-retinoid small molecules beneficial in retinopathies associated with mutations i

SUBMITTER: Ortega JT 

PROVIDER: S-EPMC6941084 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature