• Quisqualic acid is an agonist of the AMPA, kainate, and group I metabotropic glutamate receptors. (wikipedia.org)
  • L - quisqualic acid is a glutamate receptor agonist, acting at AMPA receptors and metabotropic glutamate receptors positively linked to phosphoinositide hydrolysis. (wikipedia.org)
  • Theoretical Investigation of the Structure and Function of Ionotropic Glutamate Receptors. (pitt.edu)
  • Elevated levels of glutamate during cerebral ischemia play a major role in excitotoxicity of glutamate receptors (GluRs) leading to neuron death and devastating effects on the central nervous system. (pitt.edu)
  • 2005 Aug 30;44(34):11508) studies of AMPA receptors indicate that electrostatic interactions play an important role in both ligand attraction to the ligand binding S1-S2 extracellular domain, and interactions at the S1-S2 domain interface. (pitt.edu)
  • Glycine [email protected] is an agonist to the glycine receptors (GlyRs), which are Department of Immunology, Genetics and Pathology, Uppsala University, Uppsala, Sweden pentameric ligand-gated ion channels that predomi- Department of Anatomy, Physiology and Biochemistry, Swedish nantly consist of four ligand binding alpha (α) subunits University of Agricultural Sciences, Uppsala, Sweden (GLRA1-GLRA4) and one structural beta (β) subunit [3]. (sagepub.com)
  • The NMDA type of glutamate receptors (NMDARs) are key receptors in the mammalian nervous system, and play major roles in several physiological processes that include neurotransmission, synaptic plasticity, learning, and memory. (pewtrusts.org)
  • Unlike other neurotransmitter receptors that are which are activated by individual neurotransmitters, activation of NMDARs requires the binding of a coagonist (D-serine or glycine) in addition to glutamate. (pewtrusts.org)
  • Eu3+ detects two functionally distinct luminal Ca2+ binding sites in ryanodine receptors. (sav.sk)
  • 135. Provasi, D. and Filizola, M." Enhancing Opioid Bioactivity Predictions through Integration of Ligand-Based and Structure-Based Drug Discovery Strategies with Transfer and Deep Learning Techniques" bioRxiv 2023 Aug 7;2023.08.04.552065. (filizolalab.org)
  • Biochemistry , 61:1694-1703, 2022. (uiuc.edu)
  • These results contribute to the current working hypothesis that electrostatic interactions play an important role in the glutamate receptor function. (pitt.edu)
  • Methods in Molecular Biology Series: "Protein-Ligand Interactions and Drug Design. (medchem.fi)
  • Allostery - This is a type of effect seen in proteins where the binding of a molecule, ion etc. to one location can have an impact of the structure and interactions at another location. (rcsb.org)
  • Binding energy scores were embodied in the heatmap to display varies strengths of interactions of the ligands targeting AD. (biomedcentral.com)
  • Structures of macromolecular drug targets, especially when bound to modulators, can reveal ligand-binding pockets and pinpoint protein-ligand interactions that influence the mechanism of action, potency, and specificity. (silverchair.com)
  • To mediate these processes, the extracellular ligand binding region of EGFR senses environmental cues via interactions with one of its 7 known ligands, of which epidermal growth factor (EGF) is the most well characterized ( 2 , 3 ). (biorxiv.org)
  • His main research interests are the structure-based design, synthesis and evaluation of small-molecule enzyme inhibitors and receptor ligands. (degruyter.com)
  • allosteric protein - A protein that changes among two or more structural conformations upon binding to a small molecule called an effector. (rcsb.org)
  • Between 2010 and 2020, the proportion of PDB depositions solved by EM grew from 0.7% to 17%, with nearly 50% of reported cryo-EM structures in 2020 solved at resolutions of 3.5 Å or better [ 1 ], and of these, 72% were solved with a small-molecule ligand. (silverchair.com)
  • Biochemistry , 60:2749-2760, 2021. (uiuc.edu)
  • Coumarins as Tool Compounds to Aid the Discovery of Selective Function Modulators of Steroid Hormone Binding Proteins. (medchem.fi)
  • 2018) dataset indicated widespread but low expression of Glra3 in vesicular glutamate transporter 2 (Vglut2, Slc17a6) positive and vesicular inhibitory amino acid transporter (Viaat, Slc32a1)positive neurons of the mouse central nervous system. (sagepub.com)
  • Exchange of plastoquinol with the membrane plastoquinone pool at the QB-binding site was also retarded in both mutants. (bvsalud.org)
  • This study is a proof-of-concept that acidity-responsive membrane peptide ligands can be generally applied to RTKs. (biorxiv.org)
  • The ligand-bound TM configuration promotes asymmetric dimerization of the intracellular juxta-membrane (JM) and kinase domains, which causes autophosphorylation of intracellular tyrosine residues ( 6 , 7 ). (biorxiv.org)
  • He is director of research at CNRS and, since 2001, is the head of the Laboratory of Bacterial Envelopes and Antibiotics which, for more than 30 years, has been studying the biochemistry, genetics and physiology of the bacterial cell-wall peptidoglycan biosynthesis pathway as a whole. (degruyter.com)
  • Calcium-binding proteins that are found in DISTAL KIDNEY TUBULES, INTESTINES, BRAIN, and other tissues where they bind, buffer and transport cytoplasmic calcium. (lookformedical.com)
  • Low molecular weight, calcium binding muscle proteins. (lookformedical.com)
  • Proteins to which calcium ions are bound. (lookformedical.com)
  • Secretagogins are EF HAND MOTIF-containing calcium-binding proteins that are involved in early neuronal migration and neurogenesis. (lookformedical.com)
  • This report describes a microbial toxin mechanism acting via iso-peptide bond cross-linking between host proteins and is, to the best of our knowledge, the only known example of a peptide linkage between nonterminal glutamate and lysine side chains. (rcsb.org)
  • active site - A region in proteins and nucleic acids (that participate in chemical reactions), where reacting molecules (substrates) bind and make specific contacts necessary for chemical catalysis. (rcsb.org)
  • This binding occurs at a site different from the proteins active site and enhances or reduces the protein's reactivity towards its normal ligand. (rcsb.org)
  • In addition, the molecular dynamics (MD) and the binding modi of nitrite and chlorite to the ferric wild-type enzyme and the mutant proteins and the interaction of the oxoanions with R127 have been analysed by MD simulations. (diamond.ac.uk)
  • Two plastoquinone electron acceptors, QA and QB, are present in Photosystem II (PS II) with their binding sites formed by the D2 and D1 proteins, respectively. (bvsalud.org)
  • 4] Identification and ligand binding of a chemosensory protein from sea louse Caligus rogercresseyi (Crustacea: Copepoda) Comparative biochemistry and physiology. (licebase.org)
  • A calcium-binding protein that mediates calcium HOMEOSTASIS in KIDNEYS, BRAIN, and other tissues. (lookformedical.com)
  • Detection of binding sites on SARS-CoV-2 Spike protein receptor-binding domain by molecular dynamics simulations in mixed solvents.IEEE/ACM Transactions on Computational Biology and Bioinformatics, 18: 1281-1289. (medchem.fi)
  • DEC-205 (CD205), a member of the macrophage mannose receptor protein family, is the prototypic endocytic receptor of dendritic cells, whose ligands include phosphorothioated cytosine-guanosine (CpG) oligonucleotides, a motif often seen in bacterial or viral DNA. (uci.edu)
  • Myocyte stress 1 (MS1) is a recently described striated muscle actin-binding protein that is up-regulated in the early stages of pressure overload left ventricular hypertrophy. (westminster.ac.uk)
  • What type of protein-protein interaction is disrupted in hemoglobin when oxygen binds? (flashcardmachine.com)
  • The binding of a ligand to one binding site of a protein, increases the affinity for binding the next ligand binding site such that the last binding site has the highest affinity. (flashcardmachine.com)
  • The interaction of tubulin with these polypeptides involves a GTP transfer from the exchangeable GTP-binding site (E site) of tubulin to Gα, which activates the G-protein (transactivation) ( Roychowdhury and Rasenick, 1994 ). (jneurosci.org)
  • The ligand residues are derived from the four motifs that characterize the PHP family and from two motifs conserved in histidinol phosphate phosphatases. (rhea-db.org)
  • We report here that ACD catalyzes the formation of an intermolecular iso-peptide bond between residues E270 and K50 located in the hydrophobic and the DNaseI-binding loops of actin, respectively. (rcsb.org)
  • Structurally and catalytically important residues in the phosphate binding loop of adenylate kinase of Escherichia coli. (mpg.de)
  • The defined num- ber of pendant carbohydrate residues and the discrete scaffold structure of low molecular weight ligands can make them more amenable to structural studies and systematic synthetic variation. (forextrading-madeeasy.com)
  • Ion transport and regulation in a synaptic vesicle glutamate transporter. (ucsf.edu)
  • Glycine exerts inhibition through interaction with ligand-gated ion channels com- posed of alpha and beta subunits. (sagepub.com)
  • Flip and flop: a cell-specific functional switch in glutamate-operated channels of the CNS. (mpg.de)
  • In this review, I describe the molecular mechanism underlying the extreme stability of unboiled NAD-dependent glutamate dehydrogenase from the hyperthermophile Pyrobaculum islandicum . (go.jp)
  • The coordination behavior of the phosphate ion toward the metal center supports the mechanism in which the bridging hydroxide makes a direct attack on the substrate phosphate tridentately bound to the two Fe ions and Zn ion to hydrolyze the phosphoester bond. (rhea-db.org)
  • Several ligands showed notable interaction with at least two targets, but the strong interaction with all the targets is shown by very few ligands. (biomedcentral.com)
  • This work analyses the impact of the distal, flexible and catalytic arginine on the binding of anionic angulate ligands like nitrite and the substrate chlorite. (diamond.ac.uk)
  • The findings are discussed with respect to the role(s) of R127 in ligand and chlorite binding and substrate degradation. (diamond.ac.uk)
  • Modeling the conformational change in S1-S2 that occurs upon ligand binding indicate the ligand bound conformation may be stabilized by hydrogen bonding and long-range electrostatic attraction. (pitt.edu)
  • Monoamine oxidase and higher glutamate levels are also found to be linked with Aβ peptide related oxidative stress. (biomedcentral.com)
  • Our lab has recently developed a new strategy to regulate RTK activity by designing a peptide that specifically binds to the transmembrane (TM) region of the RTK to allosterically modify kinase activity. (biorxiv.org)
  • Ligand binding promotes EGFR oligomerization mediated by the extracellular region. (biorxiv.org)
  • Specifically, the TM of unliganded (inactive) EGFR dimerizes at the C-terminus (C t ), while the ligand bound form dimerizes N-terminally (N t ), and the two helices are also rotated by 180° between the conformations ( 4 , 5 ). (biorxiv.org)
  • This review discusses the similarities and differences between the morphology of astrocytes and astrocytoma cells, and the role that dysregulation in glutamate and calcium signaling plays in the aberrant morphology of astrocytoma cells. (mdpi.com)
  • Bicarbonate (HCO3-) binding regulates electron flow between the primary (QA) and secondary (QB) plastoquinone electron acceptors of Photosystem II (PS II). (bvsalud.org)
  • Although previously considered an "unnatural" amino acid, D-serine is a key regulator of NMDAR activity by acting as a physiological ligand at the coagonist site. (pewtrusts.org)
  • Establishment of a novel microscale thermophoresis ligand-binding assay for characterization of SLC solute carriers using oligopeptide transporter PepT1 (SLC15 family) as a model system. (unibe.ch)
  • The SLC1 high-affinity glutamate and neutral amino acid transporter family. (unibe.ch)
  • Dominique Mengin-Lecreulx was trained in biochemistry, enzymology, molecular biology and organic chemistry and obtained his PhD degree at the University Paris-Sud in 1987. (degruyter.com)
  • He was trained in organic chemistry, biochemistry and enzymology, and received his PhD degree in natural sciences from the University Paris-Sud in 1979. (degruyter.com)
  • In intestinal ENTEROCYTES it mediates intracellular calcium transport from apical to basolateral membranes via calcium binding at two EF-HAND MOTIFS. (lookformedical.com)
  • The reaction starts with the fully reduced form of the enzyme, presumably with a water molecule weakly coordinated to the type-2 copper (Cu-T2) ion and no bridging moiety between the two type-3 copper (Cu-T3) ions.17,22 The incoming di- oxygen is immediately reduced, yielding a peroxide-level intermediate (PI),12 with a peroxide ion bound in the centre of the TNC. (lu.se)
  • Used iteratively and synergistically with biochemistry, pharmacology, and input from medicinal and computational chemists, SBDD is a powerful tool for optimizing drug efficacy and safety. (silverchair.com)
  • Herein, we review possible mechanisms by which glutamate may act in facilitating the growth of projections in astrocytic cells. (mdpi.com)
  • D-2-3 Bisphosphoglycerate decreases the affinity hemoglobin for oxygen by binding to and stabilizing the deoxy-hemoglobin state. (flashcardmachine.com)
  • The gamma chain of fetal hemoglobin binds BPG with a lower affinity relative to the adult hemoglobin. (flashcardmachine.com)
  • Structure of LacY with an α-substituted galactoside: Connecting the binding site to the protonation site. (ucsf.edu)
  • His main research topics have been the design, synthesis, and study of the binding modes of peptidoglycan biosynthetic pathway inhibitors. (degruyter.com)
  • The biochemistry of endocannabinoid synthesis, metabolism, and bioactivity has been difficult to study in the past. (medscape.com)
  • Thereafter, several co-crystal structures with different ligands or inhibitors were released. (degruyter.com)
  • Crystal Structure of a ligand-bound LacY-Nanobody Complex. (ucsf.edu)
  • We have investigated wild-type CCld having the distal catalytic R127 hydrogen-bonded to glutamine Q74 and variants with R127 (i) being arrested in a salt-bridge with a glutamate (Q74E), (ii) being fully flexible (Q74V) or (iii) substituted by either alanine (R127A) or lysine (R127K). (diamond.ac.uk)
  • A hexacoordinate non-heme iron is bound between QA and QB by D2 and D1, each providing two histidine ligands, and a bicarbonate that is stabilized via hydrogen bonds with D2-Tyr244 and D1-Tyr246. (bvsalud.org)
  • This pathway ends with C299 located in hydrogen-bonding distance to the amine head-group of the adt-ligand. (nature.com)