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Open AccessReview

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

Department of Pharmacology and Cleveland Center for Membrane and Structural Biology, School of Medicine, Case Western Reserve University, Cleveland, OH 44106, USA
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(24), 6218;
Received: 18 November 2019 / Revised: 27 November 2019 / Accepted: 6 December 2019 / Published: 10 December 2019
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 in rhodopsin is currently a fast-growing pharmacological field. In this review, we summarize the accumulated knowledge on retinoid ligands and non-retinoid modulators of the light-sensing GPCR, rhodopsin and their potential in combating the specific vision-related pathologies. Also, recent findings reporting the potential of biologically active compounds derived from natural products as potent rod opsin modulators with beneficial effects against degenerative diseases related to this receptor are highlighted here. View Full-Text
Keywords: G protein-coupled receptor; flavonoids; opsin; retinoids; rhodopsin; small molecules G protein-coupled receptor; flavonoids; opsin; retinoids; rhodopsin; small molecules
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MDPI and ACS Style

Ortega, J.T.; Jastrzebska, B. The Retinoid and Non-Retinoid Ligands of the Rod Visual G Protein-Coupled Receptor. Int. J. Mol. Sci. 2019, 20, 6218.

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