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Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products

Toxicology and Pharmacology, KU Leuven, Campus Gasthuisberg, O&N 2, Herestraat 49, P.O. Box 922, 3000 Leuven, Belgium
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Int. J. Mol. Sci. 2020, 21(14), 5064; https://doi.org/10.3390/ijms21145064
Received: 12 June 2020 / Revised: 14 July 2020 / Accepted: 15 July 2020 / Published: 17 July 2020
(This article belongs to the Special Issue Cannabis: Chemical Compositions and Molecular Pharmacology)
Cannabinoid receptors (CB1 and CB2), as part of the endocannabinoid system, play a critical role in numerous human physiological and pathological conditions. Thus, considerable efforts have been made to develop ligands for CB1 and CB2, resulting in hundreds of phyto- and synthetic cannabinoids which have shown varying affinities relevant for the treatment of various diseases. However, only a few of these ligands are clinically used. Recently, more detailed structural information for cannabinoid receptors was revealed thanks to the powerfulness of cryo-electron microscopy, which now can accelerate structure-based drug discovery. At the same time, novel peptide-type cannabinoids from animal sources have arrived at the scene, with their potential in vivo therapeutic effects in relation to cannabinoid receptors. From a natural products perspective, it is expected that more novel cannabinoids will be discovered and forecasted as promising drug leads from diverse natural sources and species, such as animal venoms which constitute a true pharmacopeia of toxins modulating diverse targets, including voltage- and ligand-gated ion channels, G protein-coupled receptors such as CB1 and CB2, with astonishing affinity and selectivity. Therefore, it is believed that discovering novel cannabinoids starting from studying the biodiversity of the species living on planet earth is an uncharted territory. View Full-Text
Keywords: cannabinoid receptor type 1 (CB1) and type 2 (CB2); phytocannabinoids; synthetic cannabinoids; structural analysis; animal venoms cannabinoid receptor type 1 (CB1) and type 2 (CB2); phytocannabinoids; synthetic cannabinoids; structural analysis; animal venoms
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MDPI and ACS Style

An, D.; Peigneur, S.; Hendrickx, L.A.; Tytgat, J. Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products. Int. J. Mol. Sci. 2020, 21, 5064. https://doi.org/10.3390/ijms21145064

AMA Style

An D, Peigneur S, Hendrickx LA, Tytgat J. Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products. International Journal of Molecular Sciences. 2020; 21(14):5064. https://doi.org/10.3390/ijms21145064

Chicago/Turabian Style

An, Dongchen; Peigneur, Steve; Hendrickx, Louise A.; Tytgat, Jan. 2020. "Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products" Int. J. Mol. Sci. 21, no. 14: 5064. https://doi.org/10.3390/ijms21145064

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