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Targeting adhesion G protein-coupled receptors. Current status and future perspectives.
Structure
December 2024
Rudolf Schönheimer Institute of Biochemistry, Medical Faculty, Leipzig University, 04103 Leipzig, Saxony, Germany. Electronic address:
Article Synopsis
- * The unique structure and complex interactions of aGPCRs pose challenges in pharmacological studies, despite recent advancements in understanding their activation mechanisms and structures.
- * This review focuses on small molecule ligands for the ADGRGs subfamily of aGPCRs, discussing the hurdles in drug discovery and the potential of these ligands for developing new therapies against various diseases.
Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury.
Cell Metab
November 2024
Department of Cell Biology, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan 250012, China. Electronic address:
Article Synopsis
- G protein-coupled receptors (GPCRs) play a key role in how cells respond to hormones and environmental signals, and this study focuses on their involvement in ferroptosis and liver injury.
- Researchers found that the receptor GPR56 helps cells resist ferroptosis, and its absence worsens liver damage caused by drugs or lack of oxygen.
- The study highlights 17α-hydroxypregnenolone (17-OH PREG) as a potential therapeutic agent that activates GPR56 to protect against ferroptosis and maintain liver health, while mutant forms of GPR56 fail to respond to this hormone.
The genetic cause of neurodevelopmental disorders in 30 consanguineous families.
Front Med (Lausanne)
August 2024
Department of Ophthalmology, University of Lausanne, Jules Gonin Eye Hospital, Fondation Asile Des Aveugles, Lausanne, Switzerland.
Objective: This study aims to clinically and genetically assess 30 unrelated consanguineous Pakistani families from various ethnic backgrounds, all exhibiting features of neurodevelopmental disorders (NDDs).
Methods: We conducted clinical, genetic, biochemical, and molecular analyses on 30 consanguineous families with NDDs enrolled from various regions of Pakistan. The likely molecular causes of primary microcephaly and NDDs were identified.
LRG1 Contributes to the Pathogenesis of Multiple Kidney Diseases: A Comprehensive Review.
Kidney Dis (Basel)
June 2024
Department of Burn Surgery, Department of Urology, Taizhou Central Hospital (Taizhou University Hospital), Taizhou, China.
Background: The increasing prevalence of kidney diseases has become a significant public health issue, with a global prevalence exceeding 10%. In order to accurately identify biochemical changes and treatment outcomes associated with kidney diseases, novel methods targeting specific genes have been discovered. Among these genes, leucine-rich α-2 glycoprotein 1 (LRG1) has been identified to function as a multifunctional pathogenic signaling molecule in multiple diseases, including kidney diseases.
View Article and Find Full Text PDFHexahydroquinoline Derivatives Are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1/GPR56.
Mol Pharmacol
July 2023
Department of Pharmacology, University of Michigan School of Medicine, Ann Arbor, Michigan (A.L.V., M.Y., G.G.T.); and
GPR56 is a widely expressed adhesion GPCR (AGPCR) that has pleotropic roles in brain development, platelet function, cancer, and more. Nearly all AGPCRs possess extracellular regions that bind protein ligands and conceal a cryptic tethered peptide agonist. AGPCR reception of mechanical or shear force is thought to release the tethered agonist permitting its binding to the AGPCR orthosteric site for consequent activation of G protein signaling.
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