Article
Biochemistry & Molecular Biology
Jing Li, Haixiang Lv, Xuchao Li, Yongsheng Yao, Jianhong Li, Kangsheng Ma
Summary: G protein-coupled receptors (GPCRs) are important for signal transduction and physiological processes. In this study, 87 GPCRs were identified in Aphis gossypii, including different families. Most of these GPCRs showed sequence similarity and conserved transmembrane domains. The newly identified GPCRs were differentially expressed and some were found to be highly overexpressed in a sulfoxaflor-resistant strain. Silencing of these highly overexpressed GPCRs increased susceptibility to sulfoxaflor, suggesting their involvement in resistance. These findings provide potential targets for developing insecticides to manage this pest.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Entomology
Yasser Abobakr, Faisal I. Al-Hussein, Alaa E. Bayoumi, Ali A. Alzabib, Ali S. Al-Sarar
Summary: The house fly, Musca domestica L., is an important pest associated with humans and livestock that has developed high levels of resistance to organophosphate insecticides in field populations collected from Riyadh, Saudi Arabia. Replacing these insecticides with novel ones that have different modes of action is urgent for effective pest control programs. Monitoring resistance development in house fly populations and understanding its mechanisms are essential for designing successful management strategies.
Article
Entomology
Lei Guo, Zhuang Zhang, Wei Xu, Jiangya Ma, Ni Liang, Changyou Li, Dong Chu
Summary: This study reveals that the P450 gene CYP402C1 is associated with the resistance of Bemisia tabaci to imidacloprid. Knocking down CYP402C1 significantly reduces the resistance of B. tabaci, while overexpressing CYP402C1 in transgenic Drosophila melanogaster increases resistance. Heterologous expression of CYP402C1 shows its ability to metabolize imidacloprid.
Article
Agronomy
Chunmei You, Chao Shan, Zhuo Ma, Yi Zhang, Rui Zhao, Xiwu Gao
Summary: The control of housefly heavily relies on insecticide application, with propoxur being widely used for vector control. High propoxur resistance in housefly populations is associated with mutations and overexpression of acetylcholinesterase. However, the roles of cytochrome P450 monoxygenases (P450s) in propoxur resistance remain poorly understood, with up-regulation and mutations of CYP6G4 gene being strongly associated with resistance.
PEST MANAGEMENT SCIENCE
(2021)
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
Biochemistry & Molecular Biology
Jiang Zhu, Jing Feng, Kai Tian, Chong Li, Mei Li, Xinghui Qiu
Summary: This study investigates the involvement of overexpressed cytochrome P450 enzyme CYP6G4 in the metabolism and resistance of the insecticide propoxur in house flies. The researchers found that CYP6G4 could transform propoxur and identified six metabolites. Furthermore, they demonstrated that overexpression of CYP6G4 in fruit flies increased their tolerance to propoxur, indicating its role in resistance.
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
(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
Caleb B. Hubbard, Alec C. Gerry
Summary: Research shows that house flies have developed resistance to the commonly used neonicotinoid insecticide imidacloprid through both physiological and behavioral mechanisms. Behavioral resistance is found to be located on autosomes 1 and 4, and inheritance of resistance is not fully dominant or recessive. This study opens up new avenues for understanding inherited behavior in house flies and other animals.
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Chunmei You, Lulu Zhang, Jiajia Song, Lei Zhang, Congai Zhen, Xiwu Gao
Summary: Long-term and excessive use of insecticides has led to environmental problems and insecticide resistance in pests. The variation in a P450 gene, CYP6G4, is found to be the main driver of carbamate resistance in house flies. Understanding the molecular mechanisms of insecticide resistance is crucial for effective resistance management strategies.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
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
Immunology
Mert Sudagidan, Veli Cengiz Ozalp, Ozge Can, Hakan Eligul, Mediha Nur Zafer Yurt, Behiye Busra Tasbasi, Elif Esma Acar, Murat Kavruk, Oner Kocak
Summary: This study investigated the surface microbiota of houseflies and identified the presence of Staphylococcus, Bacillus, and Enterococcus. Staphylococcus strains were selectively isolated and found to carry virulence genes and exhibit antibiotic resistance. Biofilm formation was observed in some strains, which played an important role in bacterial transmission on the surface of houseflies. The study sheds light on the composition and carriage of pathogenic staphylococci on housefly surfaces.
MICROBIAL PATHOGENESIS
(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.