• protein
  • Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (springer.com)
  • This includes integral membrane proteins, that is, proteins that completely traverse the lipid bilayer sometimes more than once such as membrane receptors, as well as peripheral membrane proteins such as the guanosine-triphosphate (GTP) binding protein ("G-protein") subunits and cell-cell recognition molecules such as LFA-2 (lymphocyte function-associated antigen-2), which are only associated with the membrane and do not traverse it. (springer.com)
  • Biochemical receptors are large protein molecules that can be activated by the binding of a ligand such as a hormone or a drug. (wikipedia.org)
  • yielding semi-quantitative estimates of actual system parameters based on Hill's unlikely simultaneity model for G protein-coupled receptors. (biomedsearch.com)
  • By homologous recombination mediated gene targeting those mice became deficient in mGlu receptor 1 protein. (wikipedia.org)
  • Chimeric G-protein-coupled receptors obviate the need for a particular agonist ligand when the ligand is resistant to purification or, in the case of orphan receptors, is not known. (aspetjournals.org)
  • This protein kinase can regulate keratinocyte differentiation by activating the MAP kinase MAPK13 (p38delta)-activated protein kinase cascade that targets CCAAT/enhancer-binding protein alpha (CEBPA). (genecards.org)
  • Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in the regulation of cell differentiation in keratinocytes and pre-B cell receptor, mediates regulation of epithelial tight junction integrity and foam cell formation, and is required for glioblastoma proliferation and apoptosis prevention in MCF-7 cells. (genecards.org)
  • Striatin-1 is a B subunit of protein phosphatase PP2A that regulates dendritic arborization and spine development in striatal neurons. (yale.edu)
  • 5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the HTR2B gene. (wikipedia.org)
  • The existence of these specific complexes (illustrated in Figure 1 ) governed by protein-protein interactions (PPIs) creates an opportunity for new therapeutic strategies to control cAMP dependent signaling that is out of tune or involved in pathologies. (frontiersin.org)
  • interactions
  • Binding occurs as a result of non-covalent interactions between the receptor and its ligand, at locations called the binding site on the receptor. (wikipedia.org)
  • RESULTS: I show here that Hall's model for interactions between an orthoster, an alloster, and a receptive unit is the best choice of model both for simulation and analysis of allosteric concentration-responses at equilibrium or steady-state. (biomedsearch.com)
  • Another interesting aspect of δ-opioid receptor function is the suggestion of mu/delta opioid receptor interactions. (wikipedia.org)
  • Relying on RET, Javitch and coworkers showed that RET signals were more characteristic of random proximity between receptors, rather than an actual bond formation between receptors, suggesting that discrepancies in binding profiles may be the result of downstream interactions, rather than novel effects due to oligomerization. (wikipedia.org)
  • plasma membrane
  • As we saw in the previous chapter, direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid bilayer. (springer.com)
  • Ammonium chloride affects receptor number and lateral mobility of the vasopressin V2-type receptor in the plasma membrane of LLC-PK, renal epithelial cells: role of the cytoskeleton. (springer.com)
  • Raff MC, De Petris S. Movement of lymphocyte surface antigens and receptors: the fluid nature of the lymphocyte plasma membrane and its immunological significance. (springer.com)
  • pathological
  • The 5-HT2B receptor stimulation can also lead to pathological proliferation of cardiac valves fibroblasts, which with chronic overstimulation of 5-HT2B can lead to a severe valvulopathy. (wikipedia.org)
  • NMDA
  • Noonan Syndrome-Associated SHP2 Dephosphorylates GluN2B to Regulate NMDA Receptor Function. (yale.edu)
  • modulation
  • the basal ganglia, which is heavily GABA populated, has been linked to major depressive disorder, suggesting a possible role for the δ-opioid receptor in mood modulation. (wikipedia.org)
  • antagonism
  • It narrows the definition of antagonism to consider only those compounds with opposing activities at a single receptor. (wikipedia.org)
  • These results show that dopamine D4 receptor antagonism in the brain does not result in the same neurochemical consequences (increased dopamine metabolism or hyperprolactinemia) observed with typical neuroleptics. (aspetjournals.org)
  • In contrast, the EPS and hyperprolactinemia associated with neuroleptics is thought to be a reflection of D2 receptor antagonism in the striatum and pituitary, respectively. (aspetjournals.org)
  • GABAA
  • Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. (wikipedia.org)
  • mice
  • Using knockout mice, we have found that β2-containinc nicotinic receptors appear to be more important for the initiation of nicotine self-administration during the first few weeks, whereas α7 nicotinic receptors appear to be more important for the long-term consumption of nicotine over a period of 5 months. (duke.edu)
  • In this article, we use mGlu receptor-deficient mice to investigate the relative contribution of mGlu2 and mGlu3 receptors in mediating the antipsychotic profile of LY404039 in the phencyclidine (PCP) and d- amphetamine (AMP) models of psychosis. (aspetjournals.org)
  • To further explore the mechanism of action of LY404039, we compared the drugs' ability to block PCP-induced hyperlocomotion to that of atypical antipsychotics in wild-type and mice lacking mGlu2/3 receptors. (aspetjournals.org)
  • In contrast, the atypical antipsychotic drugs clozapine and risperidone inhibited PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice. (aspetjournals.org)
  • high doses of the δ agonist peptide DPDPE produced respiratory depression in sheep, but in tests on mice the non-peptide δ agonist SNC-80 produced respiratory depression only at the very high dose of 40 mg/kg. (wikipedia.org)
  • affinity
  • Evidence for high and low affinity alpha 2-receptors. (wikipedia.org)
  • L-745,870 displaced specific binding of 0.2 nM [ 3 H] spiperone to cloned human dopamine D4 receptors with a binding affinity ( K i ) of 0.43 nM which was 5- and 20-fold higher than that of the standard antipsychotics haloperidol and clozapine, respectively. (aspetjournals.org)
  • MDMA (Ecstasy) MDA MEM Pergolide Cabergoline Norfenfluramine Chlorphentermine Aminorex mCPP Bromo-dragonfly DMT 5-MeO-DMT LSD-25 - About equal affinity for human cloned 5-HT2B and 5-HT2A receptors. (wikipedia.org)
  • downstream
  • The discovery of functional selectivity and that ligand-specific receptor conformations occur and can affect interaction of receptors with different second messenger systems may mean that drugs can be designed to activate some of the downstream functions of a receptor but not others. (wikipedia.org)
  • The literature highlights more than 100 examples using this strategy to address issues such as the molecular nature of the ligand binding domain, the roles of specific transmembrane spanning segments (TMS), and the nature of the cytoplasmic domains in defining downstream signaling and receptor regulation/trafficking ( Table 1 ). (aspetjournals.org)
  • In the pre-B cell receptor signaling, functions downstream of BLNK by up-regulating IRF4, which in turn activates L chain gene rearrangement. (genecards.org)
  • lipid bilayer
  • The ligand binding domain of GPCRs is not uniform with respect to the role of the N terminus, because for many GPCRs (e.g., adrenergic and serotonergic receptors), the ligand binding occurs somewhere within in the lipid bilayer ( Tota and Strader, 1990 ), although the N terminus and exofacial "loops" must contribute to the forces that organize the binding pocket for the ligand in these receptors. (aspetjournals.org)
  • amino
  • It is, therefore, proposed that putative NMDAR-C-C chemokine receptor type 2 (CCR2), NMDAR-C-X-C chemokine receptor type 4 (CXCR4), and NMDAR- interleukin 1 receptor type II (IL1R2) heteromers can be formed in the neuronal networks in mild neuroinflammation due to demonstration of Gly-Leu-Leu (GLL), Val-Ser-Thr (VST), and/or Ser-Val-Ser (SVS) amino acid homologies between these receptor protomers. (frontiersin.org)
  • Molecular
  • We are trying to understand the molecular mechanisms by which the destruction complex degrades beta-catenin, how binding of Wnts to their receptors turns off beta-catenin destruction, and how beta-catenin serves as a scaffold to link the sequence-specific Tcfs to components of the general transcription machinery. (stanford.edu)
  • modulates
  • The adrenergic system modulates the fight-or-flight response. (wikipedia.org)
  • It is also suggested however that the pain modulated by the mu-opioid receptor and that modulated by the δ-opioid receptor are distinct types, with the assertion that DOR modulates the nociception of chronic pain, while MOR modulates acute pain. (wikipedia.org)
  • GPCRs
  • Many important discoveries in the structure, function, and biology of GPCRs are the result of innovative use of chimeric receptors composed of domains of various GPCRs in an attempt to overcome formidable obstacles. (aspetjournals.org)
  • The central thrust of this review is to ascertain how the chimeric receptor strategy has been applied to studies of GPCRs and what we have learned about the values and limitations of the approach. (aspetjournals.org)
  • activate
  • Group I includes GRM1 and GRM5 and these receptors have been shown to activate phospholipase C. Group II includes GRM2 and GRM3 while Group III includes GRM4, GRM6, GRM7 and GRM8. (wikipedia.org)
  • morphine
  • The evidence for this stems from the different binding profiles of typical mu and delta agonists such as morphine and DAMGO respectively, in cells that coexpress both receptors compared to those in cells that express them individually. (wikipedia.org)
  • atypical
  • These data demonstrate that the antipsychotic-like effects of the mGlu2/3 receptor agonist LY404039 in psychostimulant models of psychosis are mechanistically distinct from those of atypical antipsychotic drugs and are dependent on functional mGlu2 and not mGlu3 receptors. (aspetjournals.org)