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Non-canonical signaling initiated by hormone-responsive G protein-coupled receptors from subcellular compartments.
Pharmacol Ther
December 2024
Fang Zongxi Center for Marine EvoDevo, MoE Key Laboratory of Marine Genetics and Breeding, College of Marine Life Sciences, Ocean University of China, Qingdao 266003, China; Insititute of Evolution & Marine Biodiversity, Ocean University of China, Qingdao 266003, China.. Electronic address:
G protein-coupled receptors (GPCRs), the largest family of membrane receptors in the mammalian genomes, regulate almost all known physiological processes by transducing numerous extracellular stimuli including almost two-thirds of endogenous hormones and neurotransmitters. The traditional view held that GPCR signaling occurs exclusively at the cell surface, where the receptors bind with the ligands and undergo conformational changes to recruit and activate heterotrimeric G proteins. However, with the application of advanced biochemical and biophysical techniques, this conventional model is challenged by the elucidation of spatiotemporal GPCR activation with the evidence that receptors can signal from subcellular compartments to exhibit various molecular and cellular responses with physiological and pathophysiological relevance.
View Article and Find Full Text PDFA-mediated synaptic glutamate dynamics and calcium dynamics in astrocytes associated with Alzheimer's disease.
Cogn Neurodyn
December 2024
School of Mathematics and Statistics, Shaanxi Normal University, Xi'an, 710119 People's Republic of China.
The accumulation of amyloid peptide is assumed to be one of the main causes of Alzheimer's disease . There is increasing evidence that astrocytes are the primary targets of A. A can cause abnormal synaptic glutamate, aberrant extrasynaptic glutamate, and astrocytic calcium dysregulation through astrocyte glutamate transporters facing the synaptic cleft (GLT-syn), astrocyte glutamate transporters facing the extrasynaptic space (GLT-ess), metabotropic glutamate receptors in astrocytes (mGluR), N-methyl-D-aspartate receptors in astrocytes (NMDAR), and glutamatergic gliotransmitter release (Glio-Rel).
View Article and Find Full Text PDFPharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators.
ACS Pharmacol Transl Sci
December 2024
Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, VIC 3052, Australia.
Metabotropic glutamate receptors are a family of eight class C G protein-coupled receptors regulating higher order brain functions including cognition and motion. Metabotropic glutamate receptors have thus been heavily investigated as potential drug targets for treating neurological disorders. Drug discovery efforts directed toward metabotropic glutamate receptor subtype 5 (mGlu) have been particularly fruitful, with a wealth of drug candidates and pharmacological tools identified.
View Article and Find Full Text PDFExpression of group II mGluRs in the inferior colliculus, medial geniculate body, and auditory cortex increases with age.
Neuroscience
December 2024
Northeast Ohio Medical University, Anatomy and Neurobiology, Rootstown, OH, USA. Electronic address:
Metabotropic glutamate receptors (mGluRs) are widely expressed throughout the central nervous system. They are linked to G-protein coupled receptors and are known to modulate synaptic transmission. The data regarding their expression in auditory structures are not systematic and mainly originate from physiological studies where expression was used to support physiological findings.
View Article and Find Full Text PDFDiscovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.
ACS Med Chem Lett
December 2024
Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, Tennessee 37232, United States.
This Letter details our efforts to develop novel, non-acetylene-containing metabotropic glutamate receptor subtype 5 (mGlu) negative allosteric modulators (NAMs) with improved pharmacological properties. This endeavor involved replacing the ether-linked pyrimidine moiety, a metabolic liability, with various 5-membered heterocycles. From this exercise, we identified , a highly brain penetrant and selective mGlu NAM which displayed moderate potency against both human and rat mGlu.
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