Review
Cardiac & Cardiovascular Systems
Alyssa Grogan, Emilio Y. Lucero, Haoran Jiang, Howard A. Rockman
Summary: G protein-coupled receptors (GPCRs) play key roles in cardiac health and disease, and are targeted for the treatment of cardiovascular diseases. Recent advancements in understanding GPCR signaling, regulation, and pharmacological properties have provided valuable insights.
CARDIOVASCULAR RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Bui San Thai, Ling Yeong Chia, Anh T. N. Nguyen, Chengxue Qin, Rebecca H. Ritchie, Dana S. Hutchinson, Andrew Kompa, Paul J. White, Lauren T. May
Summary: Heart failure remains a significant cause of morbidity and mortality worldwide. Current treatment options have limitations, leading to many patients progressing to advanced stages. Exploration of novel therapeutics targeting G protein-coupled receptors (GPCRs) has shown promise, but efficacy and unwanted effects remain as challenges.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Review
Cardiac & Cardiovascular Systems
Yuanqiang Li, Boyu Li, Wei-Dong Chen, Yan-Dong Wang
Summary: Cardiovascular diseases (CVDs) are the leading cause of death globally, accounting for nearly 30% of deaths worldwide annually. G-protein-coupled receptors (GPCRs) are vital in regulating cellular physiology and pathology, and play a crucial role in CVDs. Targeting GPCRs has become an important approach for the treatment of CVDs, with some GPCR antagonists serving as standard therapy.
FRONTIERS IN CARDIOVASCULAR MEDICINE
(2023)
Article
Pharmacology & Pharmacy
Sam Groom, Nina K. Blum, Alexandra E. Conibear, Alexander Disney, Rob Hill, Stephen M. Husbands, Yangmei Li, Lawrence Toll, Andrea Kliewer, Stefan Schulz, Graeme Henderson, Eamonn Kelly, Chris P. Bailey
Summary: This study confirmed that Compound 1 is a G protein-biased mu agonist that can induce substantial rapid receptor desensitisation in mammalian neurons. However, contrary to previous assumptions, the desensitisation effect of Compound 1 is dependent on G protein-coupled receptor kinase (GRK).
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Sandra Berndt, Ines Liebscher
Summary: SFKs are crucial regulators of cell proliferation, differentiation, and survival, with their expression strongly linked to cancer development and tumor progression. The regulation of SFKs through GPCR-mediated pathways is complex and may involve direct protein interactions or allosteric regulation by arrestins and G proteins. The potential direct interaction between GPCRs and SFKs could lead to a novel mechanism of SFK signaling and identification of new GPCR-SFK interactions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Medicine, General & Internal
Helma Freitag, Marvin Szklarski, Sebastian Lorenz, Franziska Sotzny, Sandra Bauer, Aurelie Philippe, Claudia Kedor, Patricia Grabowski, Tanja Lange, Gabriela Riemekasten, Harald Heidecke, Carmen Scheibenbogen
Summary: The study found that levels of specific AAB were significantly correlated with fatigue and muscle pain symptoms in patients with infection-triggered ME/CFS, while patients with non-infection-triggered ME/CFS showed fewer correlations. This suggests a potential role of AAB or respective receptor pathways in the pathomechanism of the disease.
JOURNAL OF CLINICAL MEDICINE
(2021)
Article
Biology
Ramon Cierco Jimenez, Nil Casajuana-Martin, Adrian Garcia-Recio, Lidia Alcantara, Leonardo Pardo, Mercedes Campillo, Angel Gonzalez
Summary: The study analyzed 119,069 natural variants in human olfactory receptors, revealing a significant diversity of natural variations in the olfactory gene repertoire between individuals and populations, with a considerable number of changes occurring at the structurally conserved regions. Mutations in positions linked to the conserved GPCR activation mechanism were highlighted, which could imply phenotypic variation in olfactory perception.
Review
Cell Biology
Marion Laudette, Karina Formoso, Frank Lezoualc'h
Summary: This article summarizes the pathophysiological roles of GRK2, GRK5, and Epac1 in the heart, focusing on how they interact under pathological conditions and contribute to the formation of scaffolded signaling systems.
Article
Medicine, General & Internal
Gerd Wallukat, Stephan Mattecka, Katrin Wenzel, Wieland Schroedl, Birgit Vogt, Patrizia Brunner, Ahmed Sheriff, Rudolf Kunze
Summary: This study found that C-reactive protein (CRP) affects intracellular calcium signaling and blood pressure. When CRP is combined with GPCR agonists in cardiomyocytes, it can interfere with the desensitization of GPCRs, regardless of the type of GPCR, but dependent on the concentration of CRP.
JOURNAL OF CLINICAL MEDICINE
(2022)
Review
Cell Biology
Marta Lagana, Geraldine Schlecht-Louf, Francoise Bachelerie
Summary: GRKs not only regulate GPCR desensitization, but also act as scaffolds and signaling adapters in complex signaling networks that affect immune cell migration. The coordinated docking of multiple GRKs on an active chemokine receptor determines a specific receptor phosphorylation barcode that translates into different signaling and migration outcomes.
Review
Cardiac & Cardiovascular Systems
Jordana Borges, Krysten E. Ferraino, Natalie Cora, Deepika Nagliya, Malka S. Suster, Alexandra M. Carbone, Anastasios Lymperopoulos
Summary: Systolic heart failure is a global disease with the highest mortality rate, characterized by reduced cardiac function. Neurohormonal imbalances play a crucial role in chronic heart failure, and the adrenal glands are important in modulating cardiac neurohormonal stress. Adrenergic receptors and AngII receptors are the two most extensively studied types of adrenal GPCRs in this context.
JOURNAL OF CARDIOVASCULAR PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Nicole Ahrens, Dana Elbers, Helena Greb, Ulrike Janssen-Bienhold, Karl-Wilhelm Koch
Summary: The study revealed diverse properties of recoverin and opsin kinase in zebrafish retina due to differential expression and interaction profiles, indicating distinct roles of different recoverin paralogs in rod and cone cells.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Xuesong Wang, Gerard J. P. van Westen, Laura H. Heitman, Adriaan P. IJzerman
Summary: G protein-coupled receptors (GPCRs) are the largest class of membrane proteins in the human genome, regulating various biological processes and serving as targets for a significant percentage of drugs on the market. Yeast serves as a useful model for studying GPCRs and offers opportunities for novel drug discovery.
BIOCHEMICAL PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Krzysztof Jozwiak, Anita Plazinska
Summary: Studies on different receptors belonging to class A of GPCRs reveal specific molecular mechanisms behind ligand directed signaling, including the role of important residues, the impact of ligand structural features on signaling, and the key interactions between ligands and receptors.
Review
Biology
Terry W. Moody, Irene Ramos-Alvarez, Robert T. Jensen
Summary: Cancer growth is regulated by receptor tyrosine kinases (RTKs) and G-protein-coupled receptors (GPCRs). Different mutations in EGFR and NTSR1 can lead to abnormal cancer proliferation. The use of tyrosine kinase inhibitors and SR48692 as antagonists can impair the transactivation process and inhibit cancer growth.