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Current Research on G Protein-Coupled Receptors
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Current Research on G Protein-Coupled Receptors

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 30 July 2024 | Viewed by 1898

Special Issue Editor

Prof. Dr. Francis Galibert

E-Mail Website
Guest Editor
Institut Génétique et Développement (UMR 6061) CNRS, Université de Rennes, Rennes, France
Interests: olfactory receptor

Special Issue Information

Dear Colleagues,

G protein coupled receptors or GPCR in short is a very large group of proteins that represent a significative portion of a mammalian genome. Since their discovery, some 20 years ago, up to seven Nobel prizes were awarded in recognition of the importance of this field. This diverse group of proteins, the number of which is not known but well over a thousand is present in all eukaryotic cells. They all share a number of characteristics.

By sequence analogy analysis, they are divided into 6 classes, which despite the lack of sequence homology between them have a common structure and mechanism of signal transduction: as cell surface receptors they are activated by a variety of ligands, the binding of which induces a conformational change that activates an associated G protein inducing an exchange GDP into GTP with an increase of the intracellular Ca2+.

The ligands correspond to an extremely large set of molecules either small lipids like most odorant molecules or large neuropeptides, allowing GPCR to be involved in a variety of physiological roles among which there are the visual, gustatory and smell senses, but also regulation of immune system activity, inflammation or hormonal homeostasis to cite a few.

Given this, GPCR are the target of a number of drugs. Up to 30 to 50 percent of marketed drugs are estimated to exert their clinical effect through a GPCR.

The special issue we have in mind should tackle most if not all of the facet of GPCR from structure to function and therapeutic and We warmly welcome submissions, including original papers and reviews.   

Prof. Dr. Francis Galibert
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Published Papers (2 papers)

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Research

17 pages, 2304 KiB  
Article
Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRABeCB2.0 Sensor
by Samay Shivshankar, Josephine Nimely, Henry Puhl III and Malliga R. Iyer
Int. J. Mol. Sci. 2024, 25(9), 5012; https://doi.org/10.3390/ijms25095012 - 3 May 2024
Viewed by 466
Abstract
Cannabinoid receptors CB1R and CB2R are G-protein coupled receptors acted upon by endocannabinoids (eCBs), namely 2-arachidonoylglycerol (2-AG) and N-arachidonoyl ethanolamine (AEA), with unique pharmacology and modulate disparate physiological processes. A genetically encoded GPCR activation-based sensor that was developed [...] Read more.
Cannabinoid receptors CB1R and CB2R are G-protein coupled receptors acted upon by endocannabinoids (eCBs), namely 2-arachidonoylglycerol (2-AG) and N-arachidonoyl ethanolamine (AEA), with unique pharmacology and modulate disparate physiological processes. A genetically encoded GPCR activation-based sensor that was developed recently—GRABeCB2.0—has been shown to be capable of monitoring real-time changes in eCB levels in cultured cells and preclinical models. However, its responsiveness to exogenous synthetic cannabinoid agents, particularly antagonists and allosteric modulators, has not been extensively characterized. This current study expands upon the pharmacological characteristics of GRABeCB2.0 to enhance the understanding of fluorescent signal alterations in response to various functionally indiscriminate cannabinoid ligands. The results from this study could enhance the utility of the GRABeCB2.0 sensor for in vitro as well as in vivo studies of cannabinoid action and may aid in the development of novel ligands. Full article
(This article belongs to the Special Issue Current Research on G Protein-Coupled Receptors)
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8 pages, 430 KiB  
Communication
Are the Olfactory Receptors Present at the Sperm Membrane Involved in Reproduction?
by Francis Galibert and Naoual Azzouzi
Int. J. Mol. Sci. 2023, 24(14), 11277; https://doi.org/10.3390/ijms241411277 - 10 Jul 2023
Viewed by 939
Abstract
Olfactory receptors (ORs), key components in ensuring the detection of myriad odorants, are expressed not only on the surface of olfactory neurons but also in many other tissues. In the case of ORs expressed at the sperm membrane, in vitro experiments with human [...] Read more.
Olfactory receptors (ORs), key components in ensuring the detection of myriad odorants, are expressed not only on the surface of olfactory neurons but also in many other tissues. In the case of ORs expressed at the sperm membrane, in vitro experiments with human and mouse spermatozoids have shown that they move toward the regions with the highest concentration of bourgeonal and lyral, respectively. However, to date, no in vivo experiment has shown any biological function of these ORs. To demonstrate a possible role in vivo of ORs in sperm chemotaxis, we overloaded the vaginal space of female mice from the prolific Swiss CD1 strain with lyral to induce competition with the supposed natural ligand and to prevent its detection. As shown, the mice that received lyral had much fewer newborns than the control mice treated with PBS, showing that lyral has a strong negative impact on procreation. This indicates that the ORs at the sperm surface are biologically active and make an important contribution to reproduction. Control experiments performed with hexanal, which does not alter sperm movement in vitro, indicate that the inhibition of reproduction observed was specific to lyral. In addition, we show that males are attracted to the smell of lyral, which acts as a pheromone, and prefer to copulate with mice marked on their back with lyral rather than with those that have not been marked. These results suggest an explanation for some cases of human infertility, which could result from an absence of recognition between the natural ligand and the ORs, either due to a mutation or a lack of expression from one of the two partners, allowing for the development of a diagnostic tests. These results might also lead to the development of a novel contraception strategy based on the use of vaginal tablets delivering an odorant or a drug that competes with the natural ligand. Full article
(This article belongs to the Special Issue Current Research on G Protein-Coupled Receptors)
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