Filtered By:
Specialty: Chemistry
Nutrition: Calcium

This page shows you your search results in order of relevance.

Order by Relevance | Date

Total 22 results found since Jan 2013.

Ischemic stroke and kynurenines: medicinal chemistry aspects.
Abstract Ischemic stroke is one of the leading causes of mortality and permanent disability in developed countries. Stroke induces massive glutamate release, which in turn causes N-Methyl-D-aspartate (NMDA) receptor over-excitation and thus calcium overload in neurons leading to cell death via apoptotic cascades. The kynurenine pathway is a complex enzymatic cascade of tryptophan catabolism, generating various neuroactive metabolites. One metabolite, kynurenic acid (KYNA), is a potent endogenous NMDA glutamate receptor antagonist, making it a possible therapeutic tool to decrease excitotoxicity and neuroinflammati...
Source: Current Medicinal Chemistry - March 12, 2018 Category: Chemistry Authors: Hertelendy P, Toldi J, Fulop F, Vecsei L Tags: Curr Med Chem Source Type: research

Molecules, Vol. 27, Pages 5488: The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke
Kiseleva Vadim V. Negrebetsky Yuri I. Baukov Ischemic stroke triggers a whole cascade of pathological changes in the brain, one of which is postischemic inflammation. Since in such cases thrombolytic therapy is often not possible, methods that modulate inflammation and affect microglia become particularly interesting. We synthesized 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate calcium(II) (Compound 4) and studied its anti-inflammatory activity in in vitro and in vivo models of inflammation and ischemia. Macrophage cell line RAW 264.7 was treated with lipopolysaccharides (LPS) and Compound 4 at various dosa...
Source: Molecules - August 26, 2022 Category: Chemistry Authors: Denis A. Borozdenko Tatiana A. Shmigol Aiarpi A. Ezdoglian Darya I. Gonchar Natalia. Y. Karpechenko Dmitri N. Lyakhmun Anastasia D. Shagina Elvira A. Cherkashova Daria D. Namestnikova Ilya L. Gubskiy Anastasia A. Chernysheva Nina M. Kiseleva Vadim V. Negr Tags: Article Source Type: research

In situ metabolite and lipid analysis of GluN2D-/- and wild-type mice after ischemic stroke using MALDI MSI.
Abstract The N-methyl-D-aspartate (NMDA) receptor is a crucial mediator of pathological glutamate-driven excitotoxicity and subsequent neuronal death in acute ischemic stroke. Although the roles of the NMDAR's composite GluN2A-C subunits have been investigated in this phenomenon, the relative importance of the GluN2D subunit has yet to be evaluated. Herein, GluN2D-/- mice were studied in a model of ischemic stroke using MALDI FT-ICR mass spectrometry imaging to investigate the role of the GluN2D subunit of the NMDA receptor in brain ischemia. GluN2D-/- mice underwent middle cerebral artery occlusion (MCAO) and bra...
Source: Analytical and Bioanalytical Chemistry - February 27, 2020 Category: Chemistry Authors: Andrews WT, Donahue D, Holmes A, Balsara R, Castellino FJ, Hummon AB Tags: Anal Bioanal Chem Source Type: research

Design and synthesis of novel GluN2A NMDAR positive allosteric modulators via scaffold hopping strategy as anti-stroke therapeutic agents
This study reported a series of GluN1/2A positive allosteric modulators as neuroprotective agents, and provided a potential opportunity to discover new drugs for stroke treatment.PMID:36934527 | DOI:10.1016/j.bmc.2023.117236
Source: Bioorganic and Medicinal Chemistry - March 19, 2023 Category: Chemistry Authors: Xin Chen Hongyu Zhu Xuequan Liu Qihong Li Mingxin Dong Source Type: research

Serum calcium channel subunit α2δ-1 concentrations and outcomes in patients with acute spontaneous intracerebral hemorrhage
CONCLUSIONS: Serum α2δ-1 subunit concentrations are intimately correlated with illness severity and are independently associated with poor 90-day outcome, substantializing serum α2δ-1 subunit as a potential prognostic biomarker for ICH.PMID:35007528 | DOI:10.1016/j.cca.2022.01.002
Source: International Journal of Clinical Chemistry - January 10, 2022 Category: Chemistry Authors: Hao Zhang Ze-Sheng Wu Jing-Quan Liu Huan Huang Source Type: research

Novel 2,6-disubstituted benzofuran-3-one analogues improve cerebral ischemia/reperfusion injury via neuroprotective and antioxidative effects
Bioorg Chem. 2023 Jan 8;132:106346. doi: 10.1016/j.bioorg.2023.106346. Online ahead of print.ABSTRACTThere are no highly effective and safe medicines for clinical treatment of ischemic stroke, although the natural product 3-n-butylphthalide (NBP) has been approved in China for mild and moderate ischemic stroke. To discover more potent anti-cerebral ischemic agents and overcome the low stability by phthalide derivatives, benzofuran-3-one was selected as a core moiety and two types of nitric oxide (NO)-donating groups were incorporated into the structure. In this work, a series of 2,6-disubstituted benzofuran-3-one derivativ...
Source: Bioorganic Chemistry - January 13, 2023 Category: Chemistry Authors: Zunhua Yang Gengzhuo Luo Yuqing Ying Huilan Li Yang Wan Guoliang Xu Mingdong Li Yang Xian Yulin Feng Yuanying Fang Source Type: research

MDEG Hyperactivation Induces Caspase-8 Activation Molecular Bases of Disease
Intracellular calcium overload plays a critical role in numerous pathological syndromes such as heart failure, brain ischemia, and stroke. Hyperactivation of the acid-sensing ion channels including degenerin/epithelial amiloride-sensitive sodium (DEG/ENaC) channels has been shown to elevate intracellular calcium and cause subsequent neuronal cell death that is independent of the canonical Egl-1/Ced-9/Ced-4/Ced-3 apoptotic pathway in Caenorhabditis elegans. In mammalian cells, hyperactivation of the DEG/ENaC channels can also lead to cell death, although the underlying mechanism remains largely unknown. Here, we use a tetra...
Source: Journal of Biological Chemistry - February 1, 2013 Category: Chemistry Authors: Pan, J.-A., Fan, Y., Gandhirajan, R. K., Madesh, M., Zong, W.-X. Tags: Cell Biology Source Type: research

The Sur1-Trpm4 Channel Molecular Bases of Disease
The sulfonylurea receptor 1 (Sur1)-NCCa-ATP channel plays a central role in necrotic cell death in central nervous system (CNS) injury, including ischemic stroke, and traumatic brain and spinal cord injury. Here, we show that Sur1-NCCa-ATP channels are formed by co-assembly of Sur1 and transient receptor potential melastatin 4 (Trpm4). Co-expression of Sur1 and Trpm4 yielded Sur1-Trpm4 heteromers, as shown in experiments with Förster resonance energy transfer (FRET) and co-immunoprecipitation. Co-expression of Sur1 and Trpm4 also yielded functional Sur1-Trpm4 channels with biophysical properties of Trpm4 and pharmacologic...
Source: Journal of Biological Chemistry - February 1, 2013 Category: Chemistry Authors: Woo, S. K., Kwon, M. S., Ivanov, A., Gerzanich, V., Simard, J. M. Tags: Membrane Biology Source Type: research

Calcineurin-Drp1 Docking in Neuronal Injury Neurobiology
Fission and fusion events dynamically control the shape and function of mitochondria. The activity of the mitochondrial fission enzyme dynamin-related protein 1 (Drp1) is finely tuned by several post-translational modifications. Phosphorylation of Ser-656 by cAMP-dependent protein kinase (PKA) inhibits Drp1, whereas dephosphorylation by a mitochondrial protein phosphatase 2A isoform and the calcium-calmodulin-dependent phosphatase calcineurin (CaN) activates Drp1. Here, we identify a conserved CaN docking site on Drp1, an LXVP motif, which mediates the interaction between the phosphatase and mechanoenzyme. We mutated the L...
Source: Journal of Biological Chemistry - April 26, 2013 Category: Chemistry Authors: Slupe, A. M., Merrill, R. A., Flippo, K. H., Lobas, M. A., Houtman, J. C. D., Strack, S. Tags: Signal Transduction Source Type: research

GluN2A and 2B in Neuronal Signaling and Death Cell Biology
GluN2A and GluN2B are the major subunits of functional NMDA receptors (NMDAR). Previous studies have suggested that GluN2A and GluN2B may differentially mediate NMDAR function at synaptic and extrasynaptic locations and play opposing roles in excitotoxicity, such as neurodegeneration triggered by ischemic stroke and brain injury. By using pharmacological and molecular approaches to suppress or enhance the function of GluN2A and GluN2B in cultured cortical neurons, we examined NMDAR-mediated, bidirectional regulation of prosurvival signaling (i.e. the cAMP response element-binding protein (CREB)-Bdnf cascade) and cell death...
Source: Journal of Biological Chemistry - August 16, 2013 Category: Chemistry Authors: Zhou, X., Ding, Q., Chen, Z., Yun, H., Wang, H. Tags: Neurobiology Source Type: research

Drp1 in Ischemic Neuronal Death: An Unusual Suspect.
Abstract Mitochondria play a crucial role in multitude of cellular processes including energy production, calcium signaling, and apoptosis. This remarkable organelle constantly undergoes a complex cycle of fusion and fission, a crucial quality control system for maintaining homeostasis of the cell. Any impairment in this dynamic behavior is linked to a wide range of cellular abnormalities. Consistent with this concept, neuronal apoptosis often emanates in conjunction with rampant mitochondrial fragmentation. The mitochondrial dynamics are tightly regulated by a master mediator called Dynamin related protein 1 (Drp...
Source: Current Medicinal Chemistry - December 28, 2013 Category: Chemistry Authors: Pradeep H, Sharma B, Rajanikant GK Tags: Curr Med Chem Source Type: research

Tonicity-induced Relocalization of Aquaporin 4 Membrane Biology
The aquaporin family of integral membrane proteins is composed of channels that mediate cellular water flow. Aquaporin 4 (AQP4) is highly expressed in the glial cells of the central nervous system and facilitates the osmotically driven pathological brain swelling associated with stroke and traumatic brain injury. Here we show that AQP4 cell surface expression can be rapidly and reversibly regulated in response to changes of tonicity in primary cortical rat astrocytes and in transfected HEK293 cells. The translocation mechanism involves PKA activation, influx of extracellular calcium, and activation of calmodulin. We identi...
Source: Journal of Biological Chemistry - July 2, 2015 Category: Chemistry Authors: Kitchen, P., Day, R. E., Taylor, L. H. J., Salman, M. M., Bill, R. M., Conner, M. T., Conner, A. C. Tags: Cell Biology Source Type: research