The relevance of the family of G protein-coupled receptor kinases (GRKs) is based on its key participation in the regulation and intracellular dynamics of the largest family of membrane receptors, namely G protein-coupled receptors (GPCRs) [...].
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http://dx.doi.org/10.3390/cells12010023 | DOI Listing |
Brain Res
December 2024
Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen 2100, Denmark. Electronic address:
Psychedelics show promise in treating psychiatric disorders. Therapeutic effects appear to involve activation of the 5-Hydroxytryptamine 2A receptor (5-HTR), a G protein-coupled receptor (GPCR). Several SNPs of the 5-HTR naturally occur, which are associated with differences in receptor function and altered responsiveness to treatments.
View Article and Find Full Text PDFCell Death Dis
December 2024
Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, China.
Radiotherapy resistance is one of the main reasons for the dismal clinical outcome of patients with esophageal squamous cell carcinoma (ESCC). Therefore, clarifying the targets and molecular mechanisms of radiotherapy resistance in ESCC is of great theoretical and clinical significance to enhance the efficacy of radiotherapy. In this study, GPR37 was identified as a key factor facilitating ESCC radiosensitization.
View Article and Find Full Text PDFNat Commun
December 2024
Experimental Medicine & Immunotherapeutics, University of Cambridge, Cambridge, UK.
We describe a structural and functional study of the G protein-coupled apelin receptor, which binds two endogenous peptide ligands, apelin and Elabela/Toddler (ELA), to regulate cardiovascular development and function. Characterisation of naturally occurring apelin receptor variants from the UK Genomics England 100,000 Genomes Project, and AlphaFold2 modelling, identifies T89 as important in the ELA binding site, and R168 as forming extensive interactions with the C-termini of both peptides. Base editing to introduce an R/H168 variant into human stem cell-derived cardiomyocytes demonstrates that this residue is critical for receptor binding and function.
View Article and Find Full Text PDFCancer Genomics Proteomics
December 2024
University Medical Center Göttingen, Department of Gynecology and Obstetrics, Göttingen, Germany
Background/aim: G protein-coupled estrogen receptor 1 (GPER1) appears to play a tumor-suppressive role in cervical squamous cell carcinoma (CSCC)GPER1 suppression leads to significantly increased expression of serpin family E member 1 (SERPINE1)/protein plasminogen activator inhibitor type 1 (PAI-1). The question arises, what role does SERPINE1/PAI-1 play in GPER1-dependent tumorigenic potential of CSCC.
Materials And Methods: SiHa and C33A CSCC cells were treated with GPER1 agonist G1 or antagonist G36.
J Biol Chem
December 2024
Department of Biosystems Science, Institute for Life and Medical Sciences, Kyoto University, Kyoto 606-8507, Japan; Department of Mammalian and Regulatory Networks, Graduate School of Biostudies, Kyoto University, Kyoto 606-8502, Japan; Department of Homeostatic Medicine, Medical Research Laboratory, Institute of Integrated Research, Institute of Science Tokyo, Yushima Bunkyo-ku, Tokyo 113-8510, Japan. Electronic address:
Alpha-1-antitrypsin (AAT), a circulating serine protease inhibitor, is an acute inflammatory response protein with anti-inflammatory functions. The C-terminal peptides of AAT are found in various tissues and have been proposed as putative bioactive peptides with multiple functions, but its mechanism of action remains unclear. We previously reported that a mouse AAT C-terminal peptide of 35 amino acids (mAAT-C) penetrates plasma membrane and associates guanine nucleotide-binding protein subunit alpha 13 (Gα13).
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