Article
Multidisciplinary Sciences
Li-Hua Zhao, Jingyu Lin, Su-Yu Ji, X. Edward Zhou, Chunyou Mao, Dan-Dan Shen, Xinheng He, Peng Xiao, Jinpeng Sun, Karsten Melcher, Yan Zhang, Xiao Yu, H. Eric Xu
Summary: This study presents the structures of CRF2R bound to UCN1 and coupled to G proteins G(11) and G(o), and compares them with the structure of CRF2R bound to G(s), uncovering the structural differences that determine the selective coupling of G protein subtypes by CRF2R.
NATURE COMMUNICATIONS
(2022)
Article
Microbiology
Peng-Peng Wang, Xuefeng Jiang, Liying Zhu, Dan Zhou, Mingyang Hong, Lu He, Lumeng Chen, Shijie Yao, Yan Zhao, Guang Chen, Chengqi Wang, Liwang Cui, Yaming Cao, Xiaotong Zhu
Summary: GPR180 is involved in signal transduction during gametogenesis in malaria parasites and its deletion impairs gametogenesis and reduces transmission to mosquitoes.
MICROBIOLOGY SPECTRUM
(2022)
Review
Engineering, Biomedical
Yuhong Jiang, Yuke Li, Xiujuan Fu, Yue Wu, Rujing Wang, Mengnan Zhao, Canquan Mao, Sanjun Shi
Summary: The translation article introduces the interaction between G protein-coupled receptors (GPCRs) and nanotechnology, as well as how nanotechnology can improve the efficacy and safety of GPCR-related drugs. Nanotechnology can encapsulate GPCR ligands to construct synthetic nano-GPCRs and precisely initiate sustained endosomal signal transduction through nanoparticles. Moreover, nanoparticles can enhance the potency of delivery systems by actively targeting specific cells through ligand-receptor binding and receptor-dependent endocytosis.
ACTA BIOMATERIALIA
(2023)
Article
Biochemistry & Molecular Biology
Abul K. Azad, Maikel A. Farhan, Cameron R. Murray, Kunimasa Suzuki, Gary Eitzen, Nicolas Touret, Ronald B. Moore, Allan G. Murray
Summary: Angiogenesis is essential in embryonic development and tissue repair. FGD5, an endothelial Rho GTP/GDP exchange factor, has been found to regulate CXCR4-dependent signals in endothelial cells and play a role in angiogenesis. Inhibition of FGD5 activity may complement current angiogenesis inhibitor drugs.
Review
Biochemistry & Molecular Biology
Roberto Maggio, Irene Fasciani, Marco Carli, Francesco Petragnano, Francesco Marampon, Mario Rossi, Marco Scarselli
Summary: The passage discusses the importance of information exchange and interpretation in biology, particularly in how cells integrate signals from various molecules. G protein-coupled receptors (GPCRs) play a crucial role in signal recognition and transduction within cells, and their formation of higher order oligomers helps organize cell compartments along the membrane. This structural basis allows for cells to perceive and discriminate localized increases in second messengers, contributing to the understanding of physiological roles played by receptor homo- and hetero-oligomerization in cell biology.
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
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)
Article
Biology
Rajesh Sharma, Jeong Joo Kim, Liying Qin, Philipp Henning, Madoka Akimoto, Bryan VanSchouwen, Gundeep Kaur, Banumathi Sankaran, Kevin R. MacKenzie, Giuseppe Melacini, Darren E. Casteel, Friedrich W. Herberg, Choel Kim
Summary: This study reveals the mechanisms of auto-inhibition and cGMP relief in PKG I beta through crystal structures and biochemical analysis. The findings suggest that auto-inhibition of PKG I beta is mediated by internal contacts within each monomer, and a model for the regulation and cooperative activation of PKGs is proposed based on the available structural and biochemical data.
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.
Article
Biochemistry & Molecular Biology
Dike Qiu, Ke Xu, Namjin Chung, Jennifer Robbins, Robert Luo, Michael Lawrence, Aiqing He, Fei Yu, Andrew Alt, Michael M. Miller, Jon Hangeland, John N. Feder, Dietmar Seiffert, Brian J. Arey
Summary: Vascular endothelial cells are influenced by mechanical forces and the patterns of these forces can regulate endothelial cell function and cardiovascular health. The transcription factor KLF2 plays a key role in the positive effects of laminar flow patterns on endothelial cell phenotype. Identifying endothelial regulators of the KLF2 program could lead to new therapeutic approaches for treating cardiovascular disease. GPCR targets that modulate KLF2 expression were identified through genetic screening, and several GPCRs were found to affect KLF2 transcriptional activation. These targets could be potential candidates for novel treatments targeting the endothelium. Initiating drug discovery efforts for LGR4 and finding synthetic ligands for this receptor demonstrate the potential for identifying new drug targets through pathway-directed phenotypic screening.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Genevieve A. Secker, Natasha L. Harvey
Summary: The importance of lymphatic vessels in human diseases, the initiation of lymphatic vascular development during embryogenesis, and the role of VEGF/VEGFR signaling in driving the construction of lymphatic vessels were discussed in this review.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biochemistry & Molecular Biology
Fujie Xu, Jipeng Ma, Xiaowu Wang, Xiaoya Wang, Weiyi Fang, Jingwei Sun, Zilin Li, Jincheng Liu
Summary: This article summarizes the function, tissue localization, ligands, and signaling pathways of GPER in different physiological and diseased conditions. It emphasizes the role of GPER in vascular pathology and physiology and presents evidence of GPER as a promising therapeutic target in hypertension, pulmonary hypertension, and atherosclerosis.
Review
Cell Biology
Lorena Perez-Gutierrez, Napoleone Ferrara
Summary: The formation of new blood vessels, known as angiogenesis, is regulated by various factors, with vascular endothelial growth factor A (VEGFA) and its receptors VEGFR1 and VEGFR2 being key components. The VEGF pathway is the main target of anti-angiogenic drugs approved by the FDA, which are widely used in oncology and the treatment of neovascular eye disorders. In this Review, the molecular basis of VEGFA action, its interactions with other pathways, and its role in regenerative medicine are discussed.
NATURE REVIEWS MOLECULAR CELL BIOLOGY
(2023)
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
Cell Biology
Odilia B. J. Corneth, Stefan F. H. Neys, Rudi W. Hendriks
Summary: This review discusses the importance of abnormal B cell signaling in autoimmune diseases, focusing on aberrant B cell receptor (BCR) signaling and other signal transduction pathways. Therapeutic strategies for interfering with B cell signal transduction are also briefly discussed.