As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design. We are eye-witnessing tremendous progresses made recently in the understanding of their structure-function relationships that facilitated drug development at an unprecedented pace. This article intends to provide a comprehensive overview of this important field to a broader readership that shares some common interests in drug discovery.
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http://dx.doi.org/10.1038/s41392-020-00435-w | DOI Listing |
Nutrients
January 2025
Department of Medical Sciences, University of Trieste, 34100 Trieste, Italy.
Background/objectives: The SNP has previously been associated with sweet taste, diet, and health status, although never comprehensively in a single study. Also, associations between and sweet taste might be body mass index (BMI)-dependent. Therefore, this study aimed to conduct a comprehensive investigation of and sweet taste intensity and liking, food liking, and diet and health status whilst considering BMI.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
State Key Laboratory of Reproductive Regulation and Breeding of Grassland Livestock, College of Life Science, Inner Mongolia University, Hohhot 010070, China.
N6-methyladenosine (m6A) modification is a key methylation modification involved in reproductive processes. gene editing (MT) in cattle is known to enhance muscle mass and productivity. However, the changes in m6A modification in MT bull sperm remain poorly understood.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Microbiology and Immunology, Graduate School of Biomedical Sciences, College of Medicine, Chang Gung University, Taoyuan 33302, Taiwan.
G protein-coupled receptors (GPCRs), critical for cellular communication and signaling, represent the largest cell surface protein family and play important roles in numerous pathophysiological processes. Consequently, GPCRs have become a primary focus in drug discovery efforts. Beyond their traditional G protein-dependent signaling pathways, GPCRs are also capable of activating alternative signaling mechanisms, including G protein-independent signaling, biased signaling, and signaling crosstalk.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Gastroenterology and Hepatology, University Hospital Zürich, University of Zürich, 8091 Zürich, Switzerland.
Tumor-associated macrophages (TAMs) in the colorectal cancer (CRC) microenvironment promote tumor progression but can be reprogrammed into a pro-inflammatory state with anti-cancer properties. Activation of the G protein-coupled receptor 84 (GPR84) is associated with pro-inflammatory macrophage polarization, making it a potential target for CRC therapy. This study evaluates the effects of the GPR84 agonists 6-OAU and ZQ-16 on macrophage activation and anti-cancer efficacy.
View Article and Find Full Text PDFMicroorganisms
January 2025
Shanghai Public Health Clinical Center, Fudan University, Shanghai 201508, China.
Tuberculosis (TB) remains the major cause of mortality and morbidity, causing approximately 1.3 million deaths annually. As a highly successful pathogen, () has evolved numerous strategies to evade host immune responses, making it essential to understand the interactions between and host cells.
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