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.
Article
Chemistry, Physical
Forough Ghasem Zadeh Moslabeh, Farzaneh Fouladgar, Amir Jafari, Neda Habibi
Summary: This study demonstrates the possibility of substrate-free peptide self-assembly through acoustic levitation and investigates the effects of peptide concentration and acoustic wave velocity amplitude on the resultant nano-structures.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2023)
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)
Article
Chemistry, Physical
Roman V. Rodik, Sergiy O. Cherenok, Viktoriia Y. Postupalenko, Sule Oncul, Vladyslava Brusianska, Petro Borysko, Vitaly I. Kalchenko, Yves Mely, Andrey S. Klymchenko
Summary: This study reports on the self-assembly behavior of anionic amphiphilic calixarenes in aqueous media. The calixarenes with phosphonate groups and alkyl chains can form micelles of about 10 nm diameter and complex cationic peptides into nanoparticles. Cellular studies show that these anionic amphiphilic calixarenes have low cytotoxicity and enable the internalization of fluorescently labeled peptides into live cells.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2022)
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)
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)
Article
Chemistry, Multidisciplinary
Florian Mahler, Annette Meister, Carolyn Vargas, Gregory Durand, Sandro Keller
Summary: The use of specific amphiphilic molecules can directly assemble lipids and membrane proteins to form native nanodiscs, rather than mixed micelles. Detailed investigation into the lipid bilayer integrity and membrane protein activity in these nanodiscs reveals gentle effects.
Review
Biotechnology & Applied Microbiology
Zhi-Min Zhao, Zhi-Hua Liu, Tongtong Zhang, Rongqian Meng, Zhiqun Gong, Yibing Li, Jing Hu, Arthur J. Ragauskas, Bing-Zhi Li, Ying-Jin Yuan
Summary: Bioconversion of bioresources/wastes using Rhodococcus is a promising approach for producing lipid-derived bioproducts. However, bioconversion involves living cells and is a complex system that requires further understanding. This review highlights the potential of Rhodococcus for producing lipids from various wastes and presents genetic modifications using emerging tools for promoting bioconversion. Additionally, strategies for enhancing the bioaccessibility of lignin and its derived aromatics and synthesizing biodiesel and aviation fuels from lignin and lipids are discussed. The synergistic modification of microbial strains, substrates, and fermentation processes is proposed for sustainable biological lignin valorization.
BIOTECHNOLOGY ADVANCES
(2024)
Review
Biotechnology & Applied Microbiology
Maddy L. Newby, Joel D. Allen, Max Crispin
Summary: A key aspect of successful viral vaccine design is the elicitation of neutralizing antibodies targeting viral attachment and fusion glycoproteins. Glycosylation can influence the antigenicity and immunogenicity of vaccines, with native-like glycosylation potentially enhancing immunogenicity. Understanding viral glycosylation can guide the development of future vaccines in various enveloped viruses.
BIOTECHNOLOGY ADVANCES
(2024)
Review
Biotechnology & Applied Microbiology
Uganeeswary Suparmaniam, Man Kee Lam, Jun Wei Lim, Inn Shi Tan, Bridgid Lai Fui Chin, Siew Hoong Shuit, Steven Lim, Yean Ling Pang, Peck Loo Kiew
Summary: Microalgae have the ability to synthesize high-value phytochemicals, and subjecting them to abiotic stress can enhance the accumulation of valuable metabolites within their cells. This study explores the effects of manipulating abiotic stress on microalgae yields and discusses approaches to increase HVPCs production using abiotic stress.
BIOTECHNOLOGY ADVANCES
(2024)
Review
Biotechnology & Applied Microbiology
Pei Zhou, Cong Gao, Wei Song, Wanqing Wei, Jing Wu, Liming Liu, Xiulai Chen
Summary: The engineering status of protein is crucial for the efficient bioproduction in microbial cell factories. Strategies such as protein engineering, protein modification, and protein assembly can effectively modify the protein status and enhance production efficiency.
BIOTECHNOLOGY ADVANCES
(2024)