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.
Article
Endocrinology & Metabolism
Valentine Suteau, Valerie Seegers, Mathilde Munier, Rym Ben Boubaker, Cecile Reyes, David Gentien, Meline Wery, Anne Croue, Frederic Illouz, Antoine Hamy, Patrice Rodien, Claire Briet
Summary: This study analyzed the GPCR expression in progressive and refractory thyroid cancers, identifying potential targets for drug repositioning. Several downregulated or deregulated GPCRs were found in thyroid tumors, providing opportunities for precision medicine in radioiodine-refractory thyroid cancer.
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
(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
Immunology
Nan Li, Shan Shan, Xiu-Qin Li, Ting-Ting Chen, Meng Qi, Sheng-Nan Zhang, Zi-Ying Wang, Ling-Ling Zhang, Wei Wei, Wu-Yi Sun
Summary: G protein-coupled receptor kinase 2 (GRK2) plays important roles in regulating signaling pathways associated with fibrotic diseases. Recent research suggests that GRK2 could be a potential therapeutic target for fibrotic diseases.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Alfredo Ulloa-Aguirre, Teresa Zarinan, Eduardo Jardon-Valadez
Summary: This review discusses the mechanisms by which mutations in GPCRs involved in endocrine function in humans lead to misfolding, decreased plasma membrane expression of the receptor protein, and loss-of-function diseases. Special attention is given to misfolded GPCRs that regulate reproductive function, and promising therapeutic interventions targeting trafficking of these defective proteins to rescue their normal function are also described.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(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
Endocrinology & Metabolism
Fanhua Wang, Mingyao Liu, Ning Wang, Jian Luo
Summary: This review discusses the role of G-protein coupled receptors (GPCRs) in osteoarthritis (OA), including the pathophysiological processes involved, preclinical and clinical trial data, and the challenges in developing therapies targeting GPCRs for OA.
FRONTIERS IN ENDOCRINOLOGY
(2022)
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.
Review
Medicine, Research & Experimental
Juan Carlos Martinez-Morales, K. Helivier Solis, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
Summary: G protein-coupled receptors (GPCRs) are membrane proteins that function as sensors and play significant roles in various physiological and pathological processes. This review provides an overview of the current understanding of the structure, signaling, internalization, and recycling of GPCRs.
ARCHIVES OF MEDICAL RESEARCH
(2022)
Article
Multidisciplinary Sciences
Xin Xu, Zhe Wei, Guangyu Wu
Summary: This study reveals the importance of multiple motifs in the trafficking of G protein-coupled receptors (GPCRs), with a specific leucine residue being involved in synaptic targeting and a dileucine (LL) motif being required for dendritic and post-synaptic traffic of all GPCRs studied.
Article
Biochemistry & Molecular Biology
Melissa Girard, Steve Dagenais Bellefeuille, Emilie Eiselt, Guillaume Arguin, Jean-Michel Longpre, Philippe Sarret, Fernand-Pierre Gendron
Summary: This study found that endosomal trafficking plays an important role in G protein-coupled receptor (GPCR) signaling. UDP selectively activates GPCR P2Y6 as a signaling molecule. The study found that MRS2693 and UDP have different effects on the internalization of the P2Y6 receptor, with MRS2693 inducing P2Y6 internalization through an independent caveolin-dependent mechanism. This study provides insights for the development of bias ligands that can influence P2Y6 signaling.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Kate F. Byrne, Ajay Pal, James F. Curtin, John C. Stephens, Gemma K. Kinsella
Summary: The focus of the review is on G-protein-coupled receptor (GPCR) targets, with chemokine, cannabinoid, and dopamine receptors showing promise. Further research is needed on potential targets such as MC4R, adhesion receptors, LPA, and Smo receptors to develop new drug-screening strategies for safe and effective GBM therapies.
DRUG DISCOVERY TODAY
(2021)
Review
Biochemistry & Molecular Biology
Dekel David, Ziv Bentulila, Merav Tauber, Yair Ben-Chaim
Summary: GPCRs are involved in signal transduction processes, and although they span the cell membrane, they have not been considered to be regulated by membrane potential. Recent studies, however, have shown that several GPCRs are voltage regulated. This review discusses the advances in understanding the voltage dependence of GPCRs, the suggested molecular mechanisms, and the possible physiological roles.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Endocrinology & Metabolism
Livia Lenzini, Brasilina Caroccia, Teresa Maria Seccia, Gian Paolo Rossi
Summary: Understanding the regulation of adrenal function and the interactions between adrenal cortex and medulla is crucial for studying the mechanisms of various diseases. The modulation of adrenal hormone biosynthesis is a complex process involving multiple factors working together. Tight vascular and neural connections between the adrenal cortex and medulla play a role in physiological autocrine/paracrine interactions involving several peptides.
Review
Pharmacology & Pharmacy
Sergi Ferre, Francisco Ciruela, Carmen W. Dessauer, Javier Gonzalez-Maeso, Terence E. Hebert, Ralf Jockers, Diomedes E. Logothetis, Leonardo Pardo
Summary: The study proposes the concept of GPCR-effect assemblies (GEMMAs), which are pre-assembled before receptor activation and allow more efficient interactions between specific signaling components. This offers an alternative model to the conventional collision coupling model and explains the differential properties of GPCRs in different cellular environments.
PHARMACOLOGY & THERAPEUTICS
(2022)