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.
Article
Cell Biology
Silke Griepke, Mette Trauelsen, Michelle D. Nilsson, Jakob Hansen, Lasse B. Steffensen, Thue W. Schwartz, Daniel F. J. Ketelhuth
Summary: This study found that the complete removal of GPR91 signaling does not influence the chronic inflammatory process of atherosclerosis, as well as the cellular infiltration and macrophage polarization associated with the disease.
Review
Immunology
Jianan Zhao, Kai Wei, Ping Jiang, Cen Chang, Lingxia Xu, Linshuai Xu, Yiming Shi, Shicheng Guo, Dongyi He
Summary: In this review, the role of G-protein-coupled receptors (GPCRs) in the mechanisms of rheumatoid arthritis (RA) is discussed, and the latest clinical trials on GPCR targeting are summarized, providing a theoretical basis and guidance for the development of innovative GPCR-based clinical drugs for RA.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Valentina Bordano, Gemma K. Kinsella, Stefania Cannito, Chiara Dianzani, Casimiro Luca Gigliotti, John C. Stephens, Chiara Monge, Claudia Bocca, Arianna C. Rosa, Gianluca Miglio, Umberto Dianzani, John B. C. Findlay, Elisa Benetti
Summary: This study evaluated the role of GPR21 in human macrophages, finding its involvement in cell migration and cytokine release, and the inhibition of its activity by the drug GRA2. GRA2 reduced the release of inflammatory cytokines from M1 macrophages and promoted the migration of M2 macrophages. Thus, pharmacological inhibition of GPR21 may be important in pathological conditions characterized by low-grade chronic inflammation.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
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)
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
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
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)
Article
Biochemistry & Molecular Biology
Wojciech Pietrus, Rafal Kurczab, Dagmar Stumpfe, Andrzej J. Bojarski, Juergen Bajorath
Summary: The study showed that introducing fluorine can significantly increase ligand potency, but the effect of fluorination on affinity varies depending on the fluorination position. Fluorination of the aromatic ring at the ortho position is favorable for potency enhancement, while fluorination of aliphatic fragments more often leads to a decrease in biological activity.
Article
Chemistry, Multidisciplinary
Yunfang Xiong, Ran Ke, Qingyu Zhang, Wenjun Lan, Wanjun Yuan, Karol Nga Ieng Chan, Tom Roussel, Yifan Jiang, Jing Wu, Shuai Liu, Alice Sze Tsai Wong, Joong Sup Shim, Xuanjun Zhang, Ruiyu Xie, Nelson Dusetti, Juan Iovanna, Nagy Habib, Ling Peng, Leo Tsz On Lee
Summary: This study reports the effective modulation of a GPCR for cancer treatment using small activating RNAs (saRNAs) for the first time. The saRNAs promote the expression of MAS1, a GPCR that counteracts cancer cell proliferation and migration. By enhancing MAS1 expression, these saRNAs suppress tumorigenesis and inhibit tumor progression in multiple cancer models. This research not only provides a new strategy for cancer therapy by targeting the renin-angiotensin system, but also offers a new avenue to modulate GPCR signaling through RNA activation.
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)
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)
Review
Chemistry, Multidisciplinary
Xin-heng He, Chong-zhao You, Hua-liang Jiang, Yi Jiang, H. Eric Xu, Xi Cheng
Summary: G protein-coupled receptors (GPCRs) are important drug targets that play crucial roles in various physiological processes. Although extensive efforts have been made in the field of structural biology, a significant number of GPCR structures remain unsolved due to their structural instability. Recently, AlphaFold2 has been developed as a tool to predict the structure models of GPCRs and other functionally important proteins. However, our evaluation reveals several differences between the predicted models and experimental structures, such as the assembly of domains, shape of ligand-binding pockets, and conformation of binding interfaces. These differences hinder the use of predicted structure models in functional studies and structure-based drug design, where reliable high-resolution structural information is required.
ACTA PHARMACOLOGICA SINICA
(2023)
Review
Endocrinology & Metabolism
Siyuan Shen, Chang Zhao, Chao Wu, Suyue Sun, Ziyan Li, Wei Yan, Zhenhua Shao
Summary: GPCRs, as the largest family of transmembrane proteins, regulate various physiological processes. However, their complicated signal transduction pathways and difficulties in drug development have presented challenges. By identifying new ligands that bind to allosteric sites, safer drugs for treating various diseases can be designed.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Eugenia Gkaliagkousi, Antonios Lazaridis, Soner Dogan, Emil Fraenkel, Bilge Guvenc Tuna, Ioana Mozos, Milica Vukicevic, Ozlem Yalcin, Kristina Gopcevic
Summary: Vascular aging, characterized by structural and functional changes in the vascular wall, is a significant marker of aging and is closely associated with cardiovascular mortality and age-related vascular pathologies. Understanding the molecular mechanisms involved in vascular aging could provide new insights into the complex biology of this irreversible process and guide future interventions to improve longevity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biotechnology & Applied Microbiology
Ting Li, Lei Guan, Guangbo Tang, Bing He, Lili Huang, Juan Wang, Mingyue Li, Yanxia Bai, Xinyuan Li, Huqin Zhang
Summary: During long-term carcinogenesis, cells accumulate mutations leading to changes in cell proliferation. Downregulation of TMEM220 is associated with poor prognosis in HCC patients, while overexpression slows cancer cell proliferation. Mechanistic studies suggest TMEM220 may inhibit HCC progression by regulating pathways involved in cell proliferation.
CANCER GENE THERAPY
(2022)
Article
Pharmacology & Pharmacy
Qingfeng Rong, Baosheng Han, Yafeng Li, Haizhen Yin, Jing Li, Yanjuan Hou
Summary: Berberine can alleviate diabetic renal tubulointerstitial injury by improving lipid metabolism, relieving lipid accumulation, and protecting mitochondria.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Plant Sciences
Lina Dong, Xiuzhao Fan, Qian Li, Jiankuan Li, Guangxin Chen, Dong Yang, Yafeng Li, Liping Zhao, Haizhen Yin, Xiaoyan Wang, Xiaojing Liu, Zhonghua Zhao, Shumei Lin
Summary: This study investigates the potential therapeutic value and mechanism of Anemone chinensis Bunge (AB) aqueous enema for ulcerative colitis (UC). The network pharmacology analysis demonstrated that AB may affect key targets and proteins related to UC. In a mouse model, AB aqueous enema alleviated colonic damage, restored tight junction proteins, and improved the diversity of gut microbiota.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Biotechnology & Applied Microbiology
Jianbo Qing, Wenzhu Song, Lingling Tian, Sonia Biju Samuel, Yafeng Li
Summary: In this study, 23 hub genes closely related to interferon production and function were identified, and their expression was found to be positively correlated with immune cell infiltration in LN patients. Additionally, six small molecules were selected as potential drugs for treating lupus nephritis.
BIOMED RESEARCH INTERNATIONAL
(2022)
Article
Immunology
Jian-Bo Qing, Wen-Zhu Song, Chang-Qun Li, Ya-Feng Li
Summary: This study investigates the diagnostic and predictive significance of DIRGs in IgAN, and finds that the imbalance between macrophages and CD4+ immune cells may be an important pathomechanism of IgAN.
JOURNAL OF IMMUNOLOGY RESEARCH
(2022)
Article
Medicine, General & Internal
Wenqiang Zhi, Wenzhu Song, Yasin Abdi Saed, Yi Wang, Yafeng Li
Summary: This report presents a case of IgA nephropathy (IgAN) in which FMT treatment was administered to a patient who showed an acute exacerbation with massive proteinuria and diarrhea. The treatment resulted in significant improvement in the patient's condition.
FRONTIERS IN MEDICINE
(2022)
Review
Medicine, General & Internal
Yi Wang, Lingling Tian, Lin Sun, Wenjing Zhou, Wenqiang Zhi, Jianbo Qing, Yasin Abdi Saed, Lina Dong, Xiadong Zhang, Yafeng Li
Summary: The interaction mechanism between gut microbiota and host plays a crucial role in the pathogenesis and treatment of IgA Nephropathy.
FRONTIERS IN MEDICINE
(2022)
Article
Immunology
Jianbo Qing, Changqun Li, Xueli Hu, Wenzhu Song, Hasna Tirichen, Hasnaa Yaigoub, Yafeng Li
Summary: This study investigated the shared gene effects and potential immune mechanisms in IgA nephropathy (IgAN) and inflammatory bowel disease (IBD). Through analyzing gene expression data and using bioinformatics methods, the study identified shared differentially expressed genes, transcription factors, and microRNAs in IgAN and IBD. The study found that the differentiation of Th17 cells may play a crucial role in IgAN and IBD patients, and identified potential biomarkers and therapeutic targets.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Immunology
Jianbo Qing, Xueli Hu, Changqun Li, Wenzhu Song, Hasna Tirichen, Hasnaa Yaigoub, Yafeng Li
Summary: In IgA nephropathy, an increase in macrophage infiltration and a decrease in CD4+ T cells, especially induced regulatory T cells (iTregs), were observed in glomeruli. Analysis identified 15 hub genes related to inflammation, with 14 of them showing increased expression with the severity of IgAN inflammation.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Medicine, General & Internal
Wenzhu Song, Xiaoshuang Zhou, Qi Duan, Qian Wang, Yaheng Li, Aizhong Li, Wenjing Zhou, Lin Sun, Lixia Qiu, Rongshan Li, Yafeng Li
Summary: This study aimed to classify glomerular injury (GI) and tubular injury (TI) of chronic kidney disease (CKD) using machine learning algorithms. Through feature selection and model construction, Random Forest demonstrated superior performance in early diagnosis of GI and TI, providing potential benefits for the progression of CKD.
FRONTIERS IN MEDICINE
(2022)
Article
Immunology
Hasnaa Yaigoub, Nada Fath, Hasna Tirichen, Changxin Wu, Rongshan Li, Yafeng Li
Summary: This article discusses the relationship between gut microbiota and systemic lupus erythematosus, highlighting the association between gut dysbiosis and the development of autoimmune diseases. It also proposes targeting gut microbiota as a potential therapeutic approach for SLE.
CLINICAL IMMUNOLOGY
(2022)
Article
Immunology
Qi Duan, Lingling Tian, Jiabing Feng, Xinbo Ping, Lihong Li, Hasnaa Yaigoub, Rongshan Li, Yafeng Li
Summary: This study aimed to investigate the protective effects of Trametenolic acid (TA) on diabetic nephropathy (DN) and its underlying mechanism. The results showed that TA administration significantly alleviated renal histopathological changes and improved renal function in DN mice. Furthermore, TA activated the Nrf2/HO-1 signaling pathway, inhibited NF-kappa B signaling, and reduced inflammation. These findings suggest that TA exhibits renoprotective effects by ameliorating oxidative stress and inflammation.
JOURNAL OF IMMUNOLOGY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Jianbo Qing, Fang Zheng, Huiwen Zhi, Hasnaa Yaigoub, Hasna Tirichen, Yaheng Li, Juanjuan Zhao, Yan Qiang, Yafeng Li
Summary: This study identified 274 common up-regulated or down-regulated immune-related genes (DIRGs) in the glomeruli and tubulointerstitium of various glomerulonephritis (GN) subtypes. These DIRGs are mainly involved in T-cell differentiation, the RAS signaling pathway, and the MAPK signaling pathway. Single-sample gene set enrichment analysis (ssGSEA) showed significant increases in dendritic cells (DC) and macrophages in glomeruli, and significant decreases in neutrophils and NKT cells. A nomogram model based on 7 DIRGs was constructed to predict GN, and 20 DIRGs for each GN subtype in glomeruli and tubulointerstitium were identified as characteristic genes.
Article
Pharmacology & Pharmacy
Xinyuan Li, Shan He, Jaya Thomas, Bonnie Wu, Tong-Yuan Yang, Michael Swanson
Summary: Cell and gene therapies show impressive efficacy in human diseases, but cellular immune response is a challenge for long-lasting clinical efficacy. This study investigates the impact of blood sample processing time on the measurement of antigen-specific cellular responses and successfully recovers ELISpot signals by optimizing processing parameters.
Article
Mathematical & Computational Biology
Wenzhu Song, Lixia Qiu, Jianbo Qing, Wenqiang Zhi, Zhijian Zha, Xueli Hu, Zhiqi Qin, Hao Gong, Yafeng Li
Summary: This study used Bayesian Network model and algorithm to explore the risk factors for stroke, and found that age, fasting plasma glucose, systolic blood pressure, and family history of stroke are direct risk factors, while sex, educational levels, high density lipoprotein cholesterol, diastolic blood pressure, and urinary albumin-to-creatinine ratio are indirect risk factors.
MATHEMATICAL BIOSCIENCES AND ENGINEERING
(2022)