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G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology
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G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology

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

Deadline for manuscript submissions: closed (20 April 2024) | Viewed by 9024

Special Issue Editor

Dr. Anastasios Lymperopoulos

E-Mail Website
Guest Editor
Laboratory for the Study of Neurohormonal Control of the Circulation, Department of Pharmaceutical Sciences, Nova Southeastern University, Fort Lauderdale, FL 33328-2018, USA
Interests: cardiovascular G protein-coupled receptors (GPCRs); heart failure; autonomic control of the circulation; adrenal physiology and pharmacology; adrenergic receptors; angiotensin receptors; signal transduction; gene therapy; aldosterone pharmacology; GPCR-Kinases; arrestins; G protein signaling
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

G protein-coupled receptors (GPCRs), also known as heptahelical or seven transmembrane-spanning receptors, reside in the plasma membrane and enable various hormones and neurotransmitters to exert their actions on mammalian cells. These receptors are essential for the homeostasis of every mammalian multi-cellular organism because they mediate extracellular signals that are not lipophilic enough to pass through cell membranes to reach their intracellular targets. Therefore, it is not surprising that GPCRs constitute the single largest pharmaceutical target class, modulating various aspects of cellular and tissue physiology, but also playing important roles in pathological situations/human diseases that arise from perturbations in cellular physiology. The greatest testament to the significance of these receptors for human physiology and disease is the fact that more than one third of all drugs currently used in clinical practice are direct ligands (agonists, antagonists and inverse agonists) of this class of receptors.

This Special Issue of “Int. J. Mol. Sci.” is inviting articles that discuss the most recent advances in various specific topics related to the roles of GPCRs in human physiology and disease at the molecular, cellular, and/or organ/system levels.

The specific topics include (but are not limited to) the following:

  • GPCR signal transduction;
  • GPCR signaling regulation or termination;
  • GPCRs and cell nucleus (DNA transcription, cell cycle and division; DNA damage response);
  • GPCRs in adipose tissue (fat) cells;
  • GPCRs in astrocytes and microglia;
  • GPCRs in cardiac myocytes;
  • GPCRs in endocrine glands (pituitary, thyroid, parathyroid, adrenals and pancreas);
  • GPCRs in cells of the GI tract;
  • GPCRs in cells of the respiratory apparatus (bronchi; lungs);
  • GPCRs in cellular aging;
  • GPCRs in cellular energetics/mitochondrial metabolism;
  • GPCRs in cellular oxidative stress;
  • GPCRs in female reproductive organ cells (uterus; ovaries);
  • GPCRs in fibroblasts;
  • GPCRs in immune and inflammatory cells;
  • GPCRs in male reproductive organ cells (testes, prostate; urinary bladder);
  • GPCRs in malignant cells/cancer;
  • GPCRs in neurons of the autonomic nervous system;
  • GPCRs in neurons of the central nervous system (CNS)/brain;
  • GPCRs in the liver ;
  • GPCRs in renal cells;
  • GPCRs in stem cell physiology;
  • GPCRs in vascular endothelial cells;
  • GPCRs in vascular smooth muscle cells;
  • Sex differences in GPCR function/physiology.

Dr. Anastasios Lymperopoulos
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.

Keywords

  • GPCR
  • signal transduction
  • molecular physiology
  • disease
  • cellular pathophysiology

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Published Papers (4 papers)

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Research

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18 pages, 3234 KiB  
Article
Melanocortin-4 Receptor PLC Activation Is Modulated by an Interaction with the Monocarboxylate Transporter 8
by Larissa Anthofer, Philipp Gmach, Zeynep Cansu Uretmen Kagiali, Gunnar Kleinau, Jonas Rotter, Robert Opitz, Patrick Scheerer, Annette G. Beck-Sickinger, Philipp Wolf, Heike Biebermann, Ingo Bechmann, Peter Kühnen, Heiko Krude and Sarah Paisdzior
Int. J. Mol. Sci. 2024, 25(14), 7565; https://doi.org/10.3390/ijms25147565 - 10 Jul 2024
Viewed by 1102
Abstract
The melanocortin-4 receptor (MC4R) is a key player in the hypothalamic leptin–melanocortin pathway that regulates satiety and hunger. MC4R belongs to the G protein-coupled receptors (GPCRs), which are known to form heterodimers with other membrane proteins, potentially modulating receptor function or characteristics. Like [...] Read more.
The melanocortin-4 receptor (MC4R) is a key player in the hypothalamic leptin–melanocortin pathway that regulates satiety and hunger. MC4R belongs to the G protein-coupled receptors (GPCRs), which are known to form heterodimers with other membrane proteins, potentially modulating receptor function or characteristics. Like MC4R, thyroid hormones (TH) are also essential for energy homeostasis control. TH transport across membranes is facilitated by the monocarboxylate transporter 8 (MCT8), which is also known to form heterodimers with GPCRs. Based on the finding in single-cell RNA-sequencing data that both proteins are simultaneously expressed in hypothalamic neurons, we investigated a putative interplay between MC4R and MCT8. We developed a novel staining protocol utilizing a fluorophore-labeled MC4R ligand and demonstrated a co-localization of MC4R and MCT8 in human brain tissue. Using in vitro assays such as BRET, IP1, and cAMP determination, we found that MCT8 modulates MC4R-mediated phospholipase C activation but not cAMP formation via a direct interaction, an effect that does not require a functional MCT8 as it was not altered by a specific MCT8 inhibitor. This suggests an extended functional spectrum of MCT8 as a GPCR signaling modulator and argues for the investigation of further GPCR-protein interactions with hitherto underrepresented physiological functions. Full article
(This article belongs to the Special Issue G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology)
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Review

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23 pages, 3649 KiB  
Review
Exploiting Cell-Based Assays to Accelerate Drug Development for G Protein-Coupled Receptors
by Yuxin Wu, Niels Jensen, Moritz J. Rossner and Michael C. Wehr
Int. J. Mol. Sci. 2024, 25(10), 5474; https://doi.org/10.3390/ijms25105474 - 17 May 2024
Cited by 1 | Viewed by 2345
Abstract
G protein-coupled receptors (GPCRs) are relevant targets for health and disease as they regulate various aspects of metabolism, proliferation, differentiation, and immune pathways. They are implicated in several disease areas, including cancer, diabetes, cardiovascular diseases, and mental disorders. It is worth noting that [...] Read more.
G protein-coupled receptors (GPCRs) are relevant targets for health and disease as they regulate various aspects of metabolism, proliferation, differentiation, and immune pathways. They are implicated in several disease areas, including cancer, diabetes, cardiovascular diseases, and mental disorders. It is worth noting that about a third of all marketed drugs target GPCRs, making them prime pharmacological targets for drug discovery. Numerous functional assays have been developed to assess GPCR activity and GPCR signaling in living cells. Here, we review the current literature of genetically encoded cell-based assays to measure GPCR activation and downstream signaling at different hierarchical levels of signaling, from the receptor to transcription, via transducers, effectors, and second messengers. Singleplex assay formats provide one data point per experimental condition. Typical examples are bioluminescence resonance energy transfer (BRET) assays and protease cleavage assays (e.g., Tango or split TEV). By contrast, multiplex assay formats allow for the parallel measurement of multiple receptors and pathways and typically use molecular barcodes as transcriptional reporters in barcoded assays. This enables the efficient identification of desired on-target and on-pathway effects as well as detrimental off-target and off-pathway effects. Multiplex assays are anticipated to accelerate drug discovery for GPCRs as they provide a comprehensive and broad identification of compound effects. Full article
(This article belongs to the Special Issue G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology)
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17 pages, 747 KiB  
Review
G Protein-Coupled Receptor Dimerization—What Next?
by Marta Dziedzicka-Wasylewska, Agnieszka Polit, Ewa Błasiak and Agata Faron-Górecka
Int. J. Mol. Sci. 2024, 25(6), 3089; https://doi.org/10.3390/ijms25063089 - 7 Mar 2024
Cited by 2 | Viewed by 2512
Abstract
Numerous studies highlight the therapeutic potential of G protein-coupled receptor (GPCR) heterodimers, emphasizing their significance in various pathological contexts. Despite extensive basic research and promising outcomes in animal models, the translation of GPCR heterodimer-targeting drugs into clinical use remains limited. The complexities of [...] Read more.
Numerous studies highlight the therapeutic potential of G protein-coupled receptor (GPCR) heterodimers, emphasizing their significance in various pathological contexts. Despite extensive basic research and promising outcomes in animal models, the translation of GPCR heterodimer-targeting drugs into clinical use remains limited. The complexities of in vivo conditions, particularly within thecomplex central nervous system, pose challenges in fully replicating physiological environments, hindering clinical success. This review discusses examples of the most studied heterodimers, their involvement in nervous system pathology, and the available data on their potential ligands. In addition, this review highlights the intricate interplay between lipids and GPCRs as a potential key factor in understanding the complexity of cell signaling. The multifaceted role of lipids in modulating the dynamics of GPCR dimerization is explored, shedding light on the elaborate molecular mechanisms governing these interactions. Full article
(This article belongs to the Special Issue G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology)
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16 pages, 2856 KiB  
Review
Information Transmission in G Protein-Coupled Receptors
by Roger D. Jones
Int. J. Mol. Sci. 2024, 25(3), 1621; https://doi.org/10.3390/ijms25031621 - 28 Jan 2024
Viewed by 2358
Abstract
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human genome and constitute about 30% of all drug targets. In this article, intended for a non-mathematical audience, both experimental observations and new theoretical results are compared in the context of [...] Read more.
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human genome and constitute about 30% of all drug targets. In this article, intended for a non-mathematical audience, both experimental observations and new theoretical results are compared in the context of information transmission across the cell membrane. The amount of information actually currently used or projected to be used in clinical settings is a small fraction of the information transmission capacity of the GPCR. This indicates that the number of yet undiscovered drug targets within GPCRs is much larger than what is currently known. Theoretical studies with some experimental validation indicate that localized heat deposition and dissipation are key to the identification of sites and mechanisms for drug action. Full article
(This article belongs to the Special Issue G Protein-Coupled Receptor Signaling in Molecular and Cellular Physiology)
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