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Allosteric Modulation of Cannabinoid Receptor 1—Current Challenges and Future Opportunities

1
Institute of Human Genetics, Polish Academy of Sciences, Strzeszyńska 32, 60-479 Poznań, Poland
2
Department of Structure and Function of Retrotransposons, Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704 Poznań, Poland
3
Department of Integrative Genomics, Institute of Anthropology, Adam Mickiewicz University, Uniwersytetu Poznańskiego 6, 61-614 Poznań, Poland
4
Department of Biochemistry and Biotechnology, University of Life Sciences, Dojazd 11, 60-632 Poznań, Poland
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(23), 5874; https://doi.org/10.3390/ijms20235874
Received: 1 November 2019 / Revised: 19 November 2019 / Accepted: 20 November 2019 / Published: 22 November 2019
(This article belongs to the Section Molecular Pharmacology)
The cannabinoid receptor type 1 (CB1R), a G protein-coupled receptor (GPCR), plays an essential role in the control of many physiological processes such as hunger, memory loss, gastrointestinal activity, catalepsy, fear, depression, and chronic pain. Therefore, it is an attractive target for drug discovery to manage pain, neurodegenerative disorders, obesity, and substance abuse. However, the psychoactive adverse effects, generated by CB1R activation in the brain, limit the use of the orthosteric CB1R ligands as drugs. The discovery of CB1R allosteric modulators during the last decade provided new tools to target the CB1R. Moreover, application of the site-directed mutagenesis in combination with advanced physical methods, especially X-ray crystallography and computational modeling, has opened new horizons for understanding the complexity of the structure, function, and activity of cannabinoid receptors. In this paper, we present the latest advances in research on the CB1R, its allosteric modulation and allosteric ligands, and their translational potential. We focused on structural essentials of the cannabinoid 1 receptor- ligand (drug) interactions, as well as modes of CB1R signaling regulation. View Full-Text
Keywords: cannabinoid receptor type 1; CB1R; CB 1 receptor; GPCR; allosteric modulation; functional selectivity; biased signaling; drug development cannabinoid receptor type 1; CB1R; CB 1 receptor; GPCR; allosteric modulation; functional selectivity; biased signaling; drug development
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Hryhorowicz, S.; Kaczmarek-Ryś, M.; Andrzejewska, A.; Staszak, K.; Hryhorowicz, M.; Korcz, A.; Słomski, R. Allosteric Modulation of Cannabinoid Receptor 1—Current Challenges and Future Opportunities. Int. J. Mol. Sci. 2019, 20, 5874.

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