The Interplay of G-Protein-Coupled Receptor Signaling between Humans and Diseases

A special issue of Cells (ISSN 2073-4409).

Deadline for manuscript submissions: 10 October 2025 | Viewed by 1934

Special Issue Editor


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Guest Editor
Department of Pharmacology, New York Medical College, Valhalla, NY, USA
Interests: G-protein-coupled receptor biology; obesity; cardiometabolic disease; eicosanoids

Special Issue Information

Dear Colleagues,

G-protein-coupled receptors (GPCRs) represent a pivotal class of signaling molecules exclusive to eukaryotic organisms, serving as the largest cohort of cell-surface proteins encoded within the human genome. GPCRs intricately orchestrate a myriad of physiological processes with their pervasive involvement spanning across virtually every facet of human biology. Moreover, their significance as druggable targets cannot be overstated. In recognition of the paramount importance of GPCRs in disease pathogenesis and therapeutic intervention, we are pleased to announce a Special Issue of Cells dedicated to the latest advancements in GPCR research. We invite submissions encompassing original research articles or comprehensive reviews, delving into the recent strides made in understanding GPCRs across a spectrum of diseases. Contributions addressing cellular signaling dynamics, the elucidation of molecular mechanisms, and the role of GPCRs in the pathophysiology of conditions such as diabetes, obesity, cardiovascular diseases, neurological disorders, and cancers are particularly encouraged. Through this endeavor, we aim to foster a deeper comprehension of GPCR biology and its translational implications, ultimately paving the way for innovative therapeutic strategies and improved patient outcomes. Join us in shaping the discourse on GPCR research and its transformative potential in elucidating disease mechanisms and advancing therapeutic modalities. Together, let us unravel the complexities of GPCR signaling and its profound implications for human health.

Dr. Victor Garcia
Guest Editor

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Keywords

  • G-proteins
  • G-protein-coupled receptors
  • G-protein-independent signaling
  • cAMP signals

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Published Papers (1 paper)

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Review

27 pages, 841 KiB  
Review
Regulation of β-Adrenergic Receptors in the Heart: A Review on Emerging Therapeutic Strategies for Heart Failure
by Warisara Parichatikanond, Ratchanee Duangrat, Hitoshi Kurose and Supachoke Mangmool
Cells 2024, 13(20), 1674; https://doi.org/10.3390/cells13201674 - 10 Oct 2024
Viewed by 1649
Abstract
The prolonged overstimulation of β-adrenergic receptors (β-ARs), a member of the G protein-coupled receptor (GPCR) family, causes abnormalities in the density and functionality of the receptor and contributes to cardiac dysfunctions, leading to the development and progression of heart diseases, especially heart failure [...] Read more.
The prolonged overstimulation of β-adrenergic receptors (β-ARs), a member of the G protein-coupled receptor (GPCR) family, causes abnormalities in the density and functionality of the receptor and contributes to cardiac dysfunctions, leading to the development and progression of heart diseases, especially heart failure (HF). Despite recent advancements in HF therapy, mortality and morbidity rates continue to be high. Treatment with β-AR antagonists (β-blockers) has improved clinical outcomes and reduced overall hospitalization and mortality rates. However, several barriers in the management of HF remain, providing opportunities to develop new strategies that focus on the functions and signal transduction of β-ARs involved in the pathogenesis of HF. As β-AR can signal through multiple pathways influenced by different receptor subtypes, expression levels, and signaling components such as G proteins, G protein-coupled receptor kinases (GRKs), β-arrestins, and downstream effectors, it presents a complex mechanism that could be targeted in HF management. In this narrative review, we focus on the regulation of β-ARs at the receptor, G protein, and effector loci, as well as their signal transductions in the physiology and pathophysiology of the heart. The discovery of potential ligands for β-AR that activate cardioprotective pathways while limiting off-target signaling is promising for the treatment of HF. However, applying findings from preclinical animal models to human patients faces several challenges, including species differences, the genetic variability of β-ARs, and the complexity and heterogeneity of humans. In this review, we also summarize recent updates and future research on the regulation of β-ARs in the molecular basis of HF and highlight potential therapeutic strategies for HF. Full article
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