Article
Biology
Alexander S. Hauser, Charlotte Avet, Claire Normand, Arturo Mancini, Asuka Inoue, Michel Bouvier, David E. Gloriam
Summary: Two-thirds of human hormones and one-third of clinical drugs act on membrane receptors coupled to G proteins, but there are differences in the reported G protein couplings among recent large-scale datasets. This study presents a common coupling map that uncovers novel couplings, GPCR-G protein selectivity, and the comparison of co-coupling and co-expression of G proteins with phylogenetic relationships. These findings will advance receptor research and cellular signaling, and contribute to the development of safer drugs.
Review
Pharmacology & Pharmacy
Nathalie Fuentes, Morgan McCullough, Reynold A. Panettieri, Kirk M. Druey
Summary: Asthma is a prevalent disorder characterized by chronic lung inflammation and reversible airways obstruction, with features including increased airway narrowing, excessive mucus secretion, airway remodeling, and airways hyperresponsiveness. Environmental factors such as allergens, viruses, and air pollution can promote asthma, leading to symptoms like cough, wheezing, and shortness of breath. G-protein-coupled receptors play a central role in asthma, with various treatments targeting these receptors to regulate airway smooth muscle tone and lung inflammation.
PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Biochemistry & Molecular Biology
Argha Mitra, Arijit Sarkar, Marton Richard Szabo, Attila Borics
Summary: Recent advancements in experimental structural biology have provided high-resolution structures of G protein-coupled receptors, shedding light on the mechanisms of transition between active and inactive states. Molecular dynamics simulations demonstrate that external stimulus transmission to the intracellular surface of the receptor involves subtle movements of polar amino acid side chains.
Article
Multidisciplinary Sciences
Rong-Chang Li, Laurie L. Molday, Chih-Chun Lin, Xiaozhi Ren, Alexander Fleischmann, Robert S. Molday, King-Wai Yau
Summary: This study provides evidence that the ligand-triggered GPCR pathway in mammalian olfactory transduction produces less than one downstream effector when an odorant-receptor molecule is complexed with its most effective odorants. This finding suggests a potential paradigm shift in our understanding of GPCR signaling.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Review
Physiology
Tiantian Su, Qiuyun Guan, Huijuan Cheng, Zhenduo Zhu, Chunru Jiang, Paipai Guo, Yu Tai, Hanfei Sun, Manman Wang, Wei Wei, Qingtong Wang
Summary: GPR56 is a human G protein-coupled receptor that plays important roles in various physiological and pathological processes, including the development of the central nervous system, the development and differentiation of hematopoietic stem cells, and tumor metastasis. Its long N-terminal extracellular region makes it an attractive therapeutic target for neurological and hematopoietic diseases.
Review
Biochemistry & Molecular Biology
Navjyoti Chakraborty, Nandula Raghuram
Summary: This review provides a comprehensive overview of plant GPCRs, cataloging all known plant GPCRs and discussing the evidence and controversies surrounding their role in plant G-protein signaling. The article argues against dismissing GPCRs and highlights the need for further investigation to establish definitive conclusions.
PLANT MOLECULAR BIOLOGY
(2023)
Article
Cell Biology
Jakob Mitgau, Julius Franke, Camilla Schinner, Gabriele Stephan, Sandra Berndt, Dimitris G. Placantonakis, Hermann Kalwa, Volker Spindler, Caroline Wilde, Ines Liebscher
Summary: This study provides information on the structural requirements and forces needed for ECM-mediated activation of the GPR126 receptor. The N terminus of GPR126 acts as an allosteric module that can fine-tune receptor activation in a context-specific manner.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Review
Cell Biology
Preeti Kumari Chaudhary, Soochong Kim
Summary: GPCRs play a crucial role in cancer progression, but the specific mechanisms of their involvement are still unclear. Studies have revealed the multifaceted impact of GPCRs on cancer development and the signaling pathways involved.
Review
Cell Biology
Haoran Jiang, Daniella Galtes, Jialu Wang, Howard A. Rockman
Summary: This review explores the signaling pathways, dynamic structures, and physiological relevance of the three most important GPCR signaling effectors in the cardiovascular system: heterotrimeric G proteins, GPCR kinases (GRKs), and 8-arrestins. It summarizes their prominent roles in GPCR pharmacology before transitioning into less well-explored areas. The application of new technologies has contributed to an increasing understanding of GPCR structure and downstream effectors.
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
(2022)
Review
Biochemistry & Molecular Biology
Ying Liu, Xiaoyun Wang, Danhui Dong, Luqin Guo, Xiaonan Dong, Jing Leng, Bing Zhao, Yang-Dong Guo, Na Zhang
Summary: G-proteins and GPCRs, as crucial signal transducers in signal transduction, have attracted increasing attention in both animal and plant research. The mode of action of G-proteins differs significantly between animals and plants, with plants possessing self-activated G alpha subunits and unique GPCR functions. More research is needed to understand the regulatory mechanisms and roles of uncanonical GPCRs in plant stress resistance and agricultural production.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Eleonore W. E. Verweij, Reggie Bosma, Meichun Gao, Jelle van den Bor, Betty Al Araaj, Sabrina M. de Munnik, Xiaoyuan Ma, Rob Leurs, Henry F. Vischer
Summary: This study used bioluminescence resonance energy transfer (BRET)-based biosensors to measure the effects of different agonists on the H1R signaling pathway, and found that one of the agonists exhibited biased agonism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Hao Chen, Suli Zhang, Ruiqi Hou, Huirong Liu
Summary: This review summarizes the discovery of the beta(1)-AR-Gi pathway and its significance in the treatment of heart diseases.
ACTA BIOCHIMICA ET BIOPHYSICA SINICA
(2022)
Review
Plant Sciences
Yijie Wang, Jose Ramon Botella
Summary: As sessile organisms, plants have evolved mechanisms to adapt to environmental fluctuations. Heterotrimeric G proteins play essential roles in the response to stress in plants, regulating multiple signaling pathways. Understanding the functions of G proteins in stress reactions can contribute to the development of resilient crops and global food security.
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)
Article
Biochemistry & Molecular Biology
Argha Mitra, Arijit Sarkar, Attila Borics
Summary: Research has revealed both structural similarities and receptor-specific differences between G protein-coupled receptors, which could be associated with different signaling pathways.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)