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
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)
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
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
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)
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
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
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
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
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
Jace Jones-Tabah
Summary: Parkinson's disease (PD) is a progressive neurodegenerative disease characterized by the deterioration of dopaminergic neurons and motor impairment. Although there is no cure for PD, dopamine replacement therapies like L-DOPA can alleviate motor symptoms. However, non-motor symptoms and the progression of neurodegeneration still lack effective treatments. This review focuses on G protein-coupled receptors (GPCRs) as potential targets for treating PD and discusses various therapeutic strategies.
JOURNAL OF MOLECULAR BIOLOGY
(2023)
Article
Multidisciplinary Sciences
Bastian Heim, Rene Handrick, Marcus D. Hartmann, Hans Kiefer
Summary: This study presents a generic approach to assess and optimize GPCR refolding from E. coli inclusion bodies through thermostability analysis. By adapting a technique based on cysteins exposed upon thermal denaturation with fluorescent dye CPM, successful expression, purification and refolding of GPCRs S1P(1) and GPR3 were demonstrated. Refolded receptors were then subjected to lipidic cubic phase crystallization screening.
Review
Genetics & Heredity
Abhijit Sreepada, Mansi Tiwari, Kasturi Pal
Summary: This article provides an overview of the classification of human G protein-coupled receptors (GPCRs) and the characteristics of adhesion GPCRs (aGPCRs). It discusses the crucial roles of aGPCRs in organ development, their involvement in various physiological processes, and their association with diseases.
JOURNAL OF MOLECULAR MEDICINE-JMM
(2022)
Article
Biochemistry & Molecular Biology
Andras D. Toth, Susanne Prokop, Pal Gyombolai, Peter Varnai, Andras Balla, Vsevolod V. Gurevich, Laszlo Hunyady, Gabor Turu
JOURNAL OF BIOLOGICAL CHEMISTRY
(2018)
Article
Biochemical Research Methods
Shih-Chia Tso, Qiuyan Chen, Sergey A. Vishnivetskiy, Vsevolod V. Gurevich, T. M. Iverson, Chad A. Brautigam
ANALYTICAL BIOCHEMISTRY
(2018)
Article
Cell Biology
Whitney M. Cleghorn, Nada Bulus, Seunghyi Kook, Vsevolod V. Gurevich, Roy Zent, Eugenia V. Gurevich
CELLULAR SIGNALLING
(2018)
Review
Biochemistry & Molecular Biology
Qiuyan Chen, Tina M. Iverson, Vsevolod V. Gurevich
TRENDS IN BIOCHEMICAL SCIENCES
(2018)
Review
Pharmacology & Pharmacy
Vsevolod V. Gurevich, EugeniaV. Gurevich
TRENDS IN PHARMACOLOGICAL SCIENCES
(2018)
Article
Neurosciences
Srimal Samaranayake, Xiufeng Song, Sergey A. Vishnivetskiy, Jeannie Chen, Eugenia V. Gurevich, Vsevolod V. Gurevich
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2018)
Editorial Material
Biochemistry & Molecular Biology
Vsevolod V. Gurevich, Eugenia Gurevich
Article
Chemistry, Multidisciplinary
Wooseok Han, Xiaolei Ma, Carl J. Balibar, Christopher M. Baxter Rath, Bret Benton, Alun Bermingham, Fergal Casey, Barbara Chie-Leon, Min-Kyu Cho, Andreas O. Frank, Alexandra Frommlet, Chi-Min Ho, Patrick S. Lee, Min Li, Andreas Lingel, Sylvia Ma, Hanne Merritt, Elizabeth Ornelas, Gianfranco De Pascale, Ramadevi Prathapam, Katherine R. Prosen, Dita Rasper, Alexey Ruzin, William S. Sawyer, Jacob Shaul, Xiaoyu Shen, Steven Shia, Micah Steffek, Sharadha Subramanian, Jason Vo, Feng Wang, Charles Wartchow, Tsuyoshi Uehara
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2020)
Article
Engineering, Electrical & Electronic
Yi-Lin Tsai, Sheng-Kai Huang, Huang-Hsiung Huang, Shu-Mei Yang, Kai-Ling Liang, Wei-Hung Kuo, Yen-Hsiang Fang, Chih- Wu, Shou-Wei Wang, Hsiang-Yun Shih, Zhiyu Xu, Minkyu Cho, Shyh-Chiang Shen, Chien-Chung Lin
IEEE PHOTONICS JOURNAL
(2020)
Article
Engineering, Electrical & Electronic
Marzieh Bakhtiary-Noodeh, Minkyu Cho, Hoon Jeong, Zhiyu Xu, Chuan-Wei Tsou, Can Cao, Shyh-Chiang Shen, Theeradetch Detchprohm, Russell D. Dupuis
Summary: The article discusses the growth of front-illuminated GaN-based p-i-n ultraviolet avalanche photodiodes using metalorganic chemical vapor deposition on a free-standing GaN substrate. The study confirms high crystal quality and low surface roughness of the grown structure. Through ion-implantation isolation, sidewall leakage current is reduced, reliability is improved, and devices demonstrate low leakage current density and a maximum gain.
JOURNAL OF ELECTRONIC MATERIALS
(2021)
Article
Nanoscience & Nanotechnology
Varnakavi Naresh, Min-Kyu Cho, Pil-Ryung Cha, Nohyun Lee
Summary: In this study, a series of Mn-doped CsPbCl3 perovskite nanocrystals (PNCs) were synthesized using a facile, one-step, polar-solvent-free sonochemical method. The structure, morphology, and temperature-dependent photoluminescence properties of the Mn-doped PNCs were investigated. The substitution of Pb2+ with Mn2+ in CsPbCl3 PNCs caused lattice contraction without altering the morphology and structure. The Mn-doped PNCs exhibited dual-wavelength photoluminescence profiles and increased photoluminescence quantum yield and decay lifetimes compared to pure CsPbCl3.
ACS APPLIED NANO MATERIALS
(2023)
Meeting Abstract
Ophthalmology
Sergey Vishnivetskiy, Lori S. Sullivan, Sara J. Bowne, Stephen P. Daiger, Eugenia Gurevich, Vsevolod V. Gurevich
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2018)
Meeting Abstract
Ophthalmology
Srimal Aminda Samaranayake, Sergey A. Vishnivetskiy, Kimberly C. Thibeault, Eugenia Gurevich, Vsevolod V. Gurevich
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2018)
Meeting Abstract
Ophthalmology
Vsevolod V. Gurevich, Ned Van Eps, Sergey Vishnivetskiy, Luwi Shamambo, Nicole A. Perry, Wayne L. Hubbell
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2018)
Article
Ophthalmology
Sergey A. Vishnivetskiy, Lori S. Sullivan, Sara J. Bowne, Stephen P. Daiger, Eugenia V. Gurevich, Vsevolod V. Gurevich
INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE
(2018)