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TRAF6-mediated ubiquitination of AKT in the nucleus is a critical event underlying the desensitization of G protein-coupled receptors
BackgroundDesensitization of G protein–coupled receptors (GPCRs) refers to the attenuation of receptor responsiveness by prolonged or intermittent...
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Ca2+/calmodulin-mediated desensitization of glutamate receptors shapes plant systemic wound signalling and anti-herbivore defence
Plants rely on systemic signalling mechanisms to establish whole-body defence in response to insect and nematode attacks. GLUTAMATE RECEPTOR-LIKE ( GLR ...
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Sequestration of Gβγ by deubiquitinated arrestins into the nucleus as a novel desensitization mechanism of G protein–coupled receptors
BackgroundDesensitization of G protein–coupled receptors (GPCRs) refers to a rapid attenuation of responsiveness that occurs with repeated or...
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Altered Signaling and Desensitization Responses in PTH1R Mutants Associated with Eiken Syndrome
The parathyroid hormone receptor type 1 (PTH1R) is a G protein-coupled receptor that plays key roles in regulating calcium homeostasis and skeletal...
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Gustatory habituation to essential oil induces reduced feeding deterrence and neuronal desensitization in Spodoptera litura
The tobacco cutworm, Spodoptera litura , is one of the most important agricultural insect pests. Plant essential oils can be considered potential...
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Structural mechanism of muscle nicotinic receptor desensitization and block by curare
Binding of the neurotransmitter acetylcholine to its receptors on muscle fibers depolarizes the membrane and thereby triggers muscle contraction. We...
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Modulation of GluA2–γ5 synaptic complex desensitization, polyamine block and antiepileptic perampanel inhibition by auxiliary subunit cornichon-2
Synaptic complexes of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors (AMPARs) with auxiliary subunits mediate most excitatory...
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Molecular Regulation of Lysophosphatidic Acid Receptor 1 Maturation and Desensitization
Lysophosphatidic acid receptor 1 (LPA1) belongs to the G protein-coupled receptor family. The ligand for LPA1 is LPA, the simplest lysophospholipid....
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Interactions between AT1R and GRKs: the determinants for activation of signaling pathways involved in blood pressure regulation
The success of Angiotensin II receptor blockers, specifically Angiotensin II type 1 receptor (AT1R) antagonists as antihypertensive drug emphasizes...
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Clinical and functional consequences of GRIA variants in patients with neurological diseases
AMPA receptors are members of the glutamate receptor family and mediate a fast component of excitatory synaptic transmission at virtually all central...
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Disease-associated nonsense and frame-shift variants resulting in the truncation of the GluN2A or GluN2B C-terminal domain decrease NMDAR surface expression and reduce potentiating effects of neurosteroids
N -methyl- d -aspartate receptors (NMDARs) play a critical role in normal brain function, and variants in genes encoding NMDAR subunits have been...
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Structural Insights into Function of Ionotropic Glutamate Receptors
Abstract —Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission. They are implicated in nervous system development and...
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Vascular nitric oxide resistance in type 2 diabetes
Vascular nitric oxide (NO•) resistance, manifested by an impaired vasodilator function of NO• in both the macro- and microvessels, is a common state...
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Generation of nanobodies acting as silent and positive allosteric modulators of the α7 nicotinic acetylcholine receptor
The α7 nicotinic acetylcholine receptor (nAChR), a potential drug target for treating cognitive disorders, mediates communication between neuronal...
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Role of the V2R–βarrestin–Gβγ complex in promoting G protein translocation to endosomes
Classically, G protein-coupled receptors (GPCRs) promote signaling at the plasma membrane through activation of heterotrimeric Gαβγ proteins,...
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How Structural Biology Has Directly Impacted Our Understanding of P2X Receptor Function and Gating
P2X receptors are ATP-gated ion channels expressed in a wide variety of eukaryotic cells. They play key roles in diverse processes such as platelet...
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Nocistatin and Products of Its Proteolysis Are Dual Modulators of Type 3 Acid-Sensing Ion Channels (ASIC3) with Algesic and Analgesic Properties
AbstractThe neuropeptide nocistatin (NS) is expressed by the nervous system cells and neutrophils as a part of a precursor protein and can undergo...
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QR code model: a new possibility for GPCR phosphorylation recognition
G protein-coupled receptors (GPCRs) are the largest family of membrane proteins in the human body and are responsible for accurately transmitting...
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Fast functional map** of ligand-gated ion channels
Ligand-gated ion channels are formed by three to five subunits that control the opening of the pore in a cooperative fashion. We developed a...
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Tyrosine phosphorylation differentially fine-tunes ionotropic and metabotropic responses of human α7 nicotinic acetylcholine receptor
The α7 nicotinic acetylcholine receptor is involved in neurological, neurodegenerative, and inflammatory disorders. It operates both as a...
