Results 91 to 100 of about 22,949 (304)
Advanced Science, EarlyView.We uncover a large variety of putative inhibitory ligand‐gated ion channels (LGICs) in the phylum Cnidaria, the sister group to all bilaterian animals. Phylogenetic analysis suggests a complex evolutionary history of inhibitory LGICs with diverse neurotransmitter ligands.
Abhilasha Ojha +13 more
wiley +1 more source
Vesicular glutamate release from central axons contributes to myelin damage
Nature Communications, 2018 Neuronal activity can lead to vesicular release of glutamate. Here the authors demonstrate that vesicular release of glutamate occurs in axons during ischemic conditions, and that an allosteric modulator of GluN2C/D is protective in models of ischemic ...
Sean Doyle +7 more
doaj +1 more source
Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
eLife, 2017 Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e. chronic pain). JF-NP-26 is an inactive photocaged derivative of the metabotropic glutamate type
Joan Font +17 more
doaj +1 more source
Machine learning approaches in predicting allosteric sites
Allosteric regulation is a fundamental biological mechanism that can control critical cellular processes via allosteric modulator binding to protein distal functional sites.
Zoe, Cournia, Francho, Nerín-Fonz
core +1 more source
Two allosteric modulators each binding to its own site.
, 2019 Allosteric interaction between tracer X and allosteric modulators A and B at receptor R. Each allosteric modulator binds to its own site, with cooperative interaction between the two sites.
Esam E. El-Fakahany (339452) +3 more
core +1 more source
Advanced Science, EarlyView.This study identifies an immunometabolic axis wherein SAM‐driven PRMT1 methylates LDHA, enhancing its activity. The resultant lactate induces STAT3 K709 lactylation, which stabilizes an active conformation to promote STAT3 phosphorylation and IL‐10 expression.
Hui Wang +12 more
wiley +1 more source
Advanced Science, EarlyView.Neuronal PKM2‐driven glycolysis generates excess lactate that triggers histone H3K18 lactylation (H3K18la), establishing a pathogenic metabolic‐epigenetic axis in epilepsy. Elevated H3K18la enriches the Cop1 promoter, transcriptionally upregulating the E3 ubiquitin ligase COP1, which subsequently drives proteasomal degradation of GABAARβ2 and impairs ...
Yuan Meng +8 more
wiley +1 more source
Progress in GABAA receptor agonists for insomnia disorder
Frontiers in PharmacologyInsomnia is the most common sleep disorder in which an individual has trouble falling or staying asleep. Chronic sleep loss interferes with daily functioning and adversely affects health.
Weiyi Wang +5 more
doaj +1 more source
GPCRs in CAR‐T Cell Immunotherapy: Expanding the Target Landscape and Enhancing Therapeutic Efficacy
Advanced Science, EarlyView.Chimeric antigen receptor T cell therapy faces dual challenges of target scarcity and an immunosuppressive microenvironment in solid tumors. This review highlights how G protein‐coupled receptors can serve as both novel targets to expand the therapeutic scope and functional modules to enhance CAR‐T cell efficacy.
Zhuoqun Liu +11 more
wiley +1 more source
Identification of a unique Ca2+-binding site in rat acid-sensing ion channel 3
Nature Communications, 2018 Acid-sensing ion channels (ASICs) sense changes in extracellular acidity with Ca2+ as an allosteric modulator and channel blocker. Here authors use electrophysiology and molecular dynamics simulation to identify the residue in ASIC3 which modulates ...
Zhicheng Zuo +7 more
doaj +1 more source