• Binding measurements claim that it ox-LDL binds to LOX-1 with high affinity. (globaltechbiz.com)
  • LIH383 therefore binds to and blocks ACKR3, thereby modulating the availability of opioid peptides that can bind to classical opioid receptors in the brain and potentiating their natural painkilling and antidepressant properties. (innoget.com)
  • Apolipoprotein B binds to specific receptors on cell membranes and is involved in removal of LDL and very low density lipoprotein (VLDL) cholesterol from circulation. (thermofisher.com)
  • LDL binds to its receptor on the capillary walls and thereby mediates the uptake and clearance of cholesterol from the circulation. (thermofisher.com)
  • This receptor binds essentially all inflammatory CC-chemokines with high affinity but does not mount classical signaling responses following ligand binding (9,C11). (eyesoftheelephants.com)
  • 2-Imidazolidinone also binds with high affinity to adrenergic receptors, including the D3 receptor. (atamanchemicals.com)
  • In recent years, the guidelines have recommended non-high density lipoprotein cholesterol (non-HDL-C) as a secondary target for lipid-lowering therapy. (biomedcentral.com)
  • In the test group, total cholesterol (TC), triglycerides (TG), LDL-C, high density lipoprotein cholesterol (HDL-C), non-HDL-C, arteriosclerosis index (AI), and LDL-C/HDL-C all correlated with the patients' Gensini score. (biomedcentral.com)
  • BACKGROUND: SR-B1 (scavenger receptor class B type 1)/LDLR (low-density lipoprotein receptor) double knockout mice fed a high-fat, high-cholesterol diet containing cholate exhibit coronary artery disease characterized by occlusive coronary artery atherosclerosis, platelet accumulation in coronary arteries, and myocardial fibrosis. (bvsalud.org)
  • HDL (high-density lipoprotein) exerts direct atheroprotective effects on different cells within atherosclerotic plaques. (bvsalud.org)
  • Massive xanthomatosis and atherosclerosis in cholesterol-fed low density lipoprotein receptor-negative mice. (jci.org)
  • The connections between your lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1) and oxidatively improved low-density lipoprotein (ox-LDL) has a significant function in the pathobiology of atherosclerosis, aswell as myocardial ischemia and hypertension1. (globaltechbiz.com)
  • Oxidation of low-density lipoprotein (LDL) cholesterol is crucial in the development of atherosclerosis, and low LDL levels reduce the risk of major events in patients with CVD [ 6 ]. (hindawi.com)
  • Several cellular receptors for HCV have been proposed, all of which are associated with lipid and lipoprotein metabolism. (biomedcentral.com)
  • Previous research by the Immuno-Pharmacology and Interactomics group of the LIH Department of Infection and Immunity (DII) identified the atypical chemokine receptor ACKR3 as a novel previously unknown opioid receptor in the brain. (innoget.com)
  • In addition to the 18 signaling receptors for chemokines (4), there also exists a small subfamily of atypical chemokine receptors (ACKRs)2 that are characterized by an inability to mount classical receptor signaling following ligand binding (4,C8). (eyesoftheelephants.com)
  • 7 In contrast, alternatively activated macrophages are characterized by increased expression of IL-10 and of scavenger receptors. (haematologica.org)
  • Nonoxidized LDL have a low affinity for macrophages, so they are not themselves a risk factor. (hindawi.com)
  • Despite that macrophages have low affinity for nonoxidized LDL, reducing LDL levels prevents oxidation, as recognized by European and American cardiac societies in their guidelines [ 11 ]. (hindawi.com)
  • By performing proximity labeling and proteomic analysis, we identified scavenger receptor CD36 as a cell surface protein interacting with Siglec-E. Further experiments performed in HEK293T cells transiently overexpressing Siglec-E and CD36 and peritoneal macrophages demonstrated that depletion of cell surface sialic acids by treatment with sialyltransferase inhibitor or sialidase did not affect interaction between Siglec-E and CD36 but retarded Siglec-E-mediated inhibition on oxidized LDL uptake. (biomedcentral.com)
  • ALOX5 arachidonate 5-lipoxygenase: macrophages infected with Candida albicans, Aspergillus flavus or Aspergillus fumigatus or treated with Curdlan, a selective agonist of pattern recognition receptor for fungi Dectin-1, displays increased expression of ALOX5, ALOX15 and PTGS2 Karnam et al, 2015 . (polygenicpathways.co.uk)
  • In atherosclerotic lesions oxidatively modified LDL is found and oxidized LDL is specifically recognized and ingested by macrophages via scavenger receptor A and CD36. (thermofisher.com)
  • Here we report that antidiabetic thiazolidinediones (TZDs) and other ligands for the nuclear receptor PPARγ dramatically upregulate oxidized LDL receptor 1 (OLR1) in adipocytes by facilitating the exchange of coactivators for corepressors on the OLR1 gene in cultured mouse adipocytes. (jci.org)
  • Siglecs are a family of sialic acid-binding immunoglobulin-like receptors predominantly expressed on cells of immune system to regulate their functions through recognizing their glycan ligands [ 5 ]. (biomedcentral.com)
  • HA can bind to the three main classes of cell surface receptors, each having a unique role: CD44 (a membrane glycoprotein), RHAMM (the receptor for hyaluronate-mediated motility), and ICAM-1 (intercellular adhesion molecule 1).CD44 is the most widely distributed cell surface receptor recognised for HA binding Other ligands that interact with CD44 include osteopontin, collagens, and matrix metalloproteinases (MMPs). (biotechnolabs.com)
  • Compared with other natural opioid ligands, its sequence (FGGFMRRK) confers it maximum specificity and affinity for ACKR3 and minimum selectivity and affinity for other opioid receptors. (innoget.com)
  • After P-gp inhibition, rat brain uptake could specifically be blocked by 5-HT7 and σ receptor ligands. (sarilumabinhibitor.com)
  • Inhibition of ox-LDL binding with LOX-1 may be accomplished by either obstructing the basic backbone or the tunnel, but a ligand can have significantly more interactions inside a tunnel than on the top leading to higher affinity and specificity. (globaltechbiz.com)
  • In vivo specificity was investigated by 5-HT7 and σ receptor blocking studies. (sarilumabinhibitor.com)
  • Platelets are involved in atherosclerosis development, and PAR (protease-activated receptor) 4 has a prominent role in platelet function in mice. (bvsalud.org)
  • Although aortic sinus atherosclerosis levels did not differ, RAG8-treated mice exhibited reduced coronary artery atherosclerosis, reduced platelet accumulation in atherosclerotic coronary arteries, and reduced myocardial fibrosis. (bvsalud.org)
  • CONCLUSIONS: The PAR4 inhibitory RAG8 pepducin reduced coronary artery atherosclerosis and myocardial fibrosis in SR-B1/LDLR double knockout mice fed a high-fat, high-cholesterol diet containing cholate. (bvsalud.org)
  • We conclude that LDL receptors are largely responsible for the resistance of wild type mice to atherosclerosis. (jci.org)
  • ApoE-deficient (apoE −/− ) and apoE/Siglec-E-double deficient (apoE −/− /Siglec-E −/− ) mice were placed on high fat diet for 3 months and their lipid profiles and severities of atherosclerosis were assessed. (biomedcentral.com)
  • Apolipoprotein B is a ligand for the LDL receptor and elevated levels are associated with premature atherosclerosis. (thermofisher.com)
  • Despite the key roles of perilipin-2 (PLIN2) in governing lipid droplet (LD) metabolism, the mechanisms that regulate PLIN2 levels remain incompletely understood. (stanford.edu)
  • It has recently been demonstrated that prenatal exposure to the cannabinoid receptor 1 agonist (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinyl-methyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone (WIN 55,212-2) produces memory deficit in adulthood, an effect associated with a reduced functionality of the glutamatergic system. (researchgate.net)
  • Purpose: The serotonin 7 (5-HT7) receptor is suggested to be involved in a broad variety of CNS disorders, but very few in vivo tools exist to study this important target. (sarilumabinhibitor.com)
  • olecular imaging with positron emission tomography (PET) would enable an in vivo characterization of the 5-HT7 receptor. (sarilumabinhibitor.com)
  • Positron emission tomography (PET) is a non-invasive imaging technique which can be used to visualize and quantify a broad set of molecular targets such as enzymes and receptors in vivo. (sarilumabinhibitor.com)
  • 2-Imidazolidinone has been used in vivo studies to assess its effect on serotonin levels. (atamanchemicals.com)
  • SR-B1/LDLR double knockout mice were fed a high-fat, high-cholesterol diet containing cholate and injected daily with 20 mg/kg of either the RAG8 pepducin or a control reverse-sequence pepducin (SRQ8) for 20 days. (bvsalud.org)
  • Mice that are homozygous for a targeted disruption of the LDL receptor gene (LDLR-/- mice) were fed a diet that contained 1.25% cholesterol, 7.5% cocoa butter, 7.5% casein, and 0.5% cholic acid. (jci.org)
  • No such changes were seen in the LDLR-/- mice on a normal chow diet, nor in wild type mice that were fed either a chow diet or the high-fat diet. (jci.org)
  • However, RAG8-treated mice exhibited reduced VCAM-1 (vascular cell adhesion molecule 1) protein levels in nonatherosclerotic coronary artery cross sections and reduced leukocyte accumulation in atherosclerotic coronary artery cross sections compared with those from SRQ8-treated mice. (bvsalud.org)
  • Mammals have 45 chemokines and 18 receptors that involve themselves, in sometimes very complex ways, in regulating leukocyte migration. (eyesoftheelephants.com)
  • However, nuclear receptors are also associated with melatonin activity. (explorationpub.com)
  • It is useful for proteins and essential for cellular signaling with specific molecules and receptors. (biotechnolabs.com)
  • Opioid peptides are small proteins that act as neuromodulators by interacting with four 'classical' opioid receptors located on the surface of central nervous system (CNS) cells. (innoget.com)
  • Since the genomic sequence of HCV was determined, progress has been made towards understanding the functions of the HCV-encoded proteins and identifying the cellular receptor(s) responsible for adsorption and penetration of the virus particle into the target cells. (biomedcentral.com)
  • Scavenger receptors are cell membrane proteins that bind chemically modified lipoproteins, such as acetylated and oxidized LDLs. (biomedcentral.com)
  • Because of its anti-oxidant and anti-inflammatory effects, it was tested in animal models of Alzheimer's disease, reducing levels of amyloid and oxidized proteins and preventing cognitive deficits. (iospress.com)
  • In particular, prenatal cannabinoid treatment reduced the phosphorylated levels of ERK1/2 in selected subcellular compartments of hippocampus, frontal and prefrontal cortex, whereas no changes were observed in the total levels of these proteins. (researchgate.net)
  • they may also play other roles in immune regulation and homeostasis, through their ability to bind host antigens, surface molecules and receptors. (biomedcentral.com)
  • HA regulates cellular behaviour by controlling the macro- and microenvironments of the tissue by binding to ECM molecules and cell surface receptors. (biotechnolabs.com)
  • Neurocan, CD44, the receptor for hyaluronate-mediated-mediated motility (RHAMM), GHAP (glial HA binding protein), LYVE-1 (Lymphatic Vessel Endothelial Hyaluronan Receptor 1), Versican, Aggrecan, and TSG6 (TNF-stimulated gene 6) are a few examples of receptors and molecules. (biotechnolabs.com)
  • It is well known that molecules with a higher relative molecular mass promote wound healing. (biotechnolabs.com)
  • For this purpose, WIN 55,212-2 was injected in pregnant wistar rats from gestation day 5 to 20 and a detailed analysis of the levels of the neurotrophin brain-derived neurotrophic factor (BDNF) as well as of the signaling molecules extracellular signal-regulated kinase (ERK)1/2 and alpha-calcium/calmodulin-dependent protein kinase II (alpha-CaMKII) was carried out in adult offspring. (researchgate.net)
  • The molecularly imprinted polymers act as artificial antibodies, artificial receptors, or artificial enzymes with the added benefit over their biological counterparts of being highly durable. (mdpi.com)
  • receptors with enzymes facilitate between 15 and 60 transcription of proposed sIL6R and enter directly a genome of this into the protein( Berge et al. (erik-mill.de)
  • These chemokines then attract inflammatory leukocytes bearing their cognate receptors, and these cells remove pathogens, engulf debris, and assist in the process of tissue repair. (eyesoftheelephants.com)
  • Unlike drugs, radiotracers are usually applied at tracer doses (pmol-µmol) in order to avoid perturbuing the biological system under investigation.5 A PET radiotracer for the 5-HT7 receptor would aid in exploring the role of this receptor in healthy and diseased brains. (sarilumabinhibitor.com)
  • Investigation of photoinitiated Bergman cyclisation reactions using high-resolution laser spectroscopy. (exeter.ac.uk)
  • Thus, the identification of the HCV receptor on the surface of susceptible cells, especially hepatocytes, remains a major challenge for the development of both in vitro cell culture systems, and for the design of successful therapies [ 3 , 4 ]. (biomedcentral.com)
  • Of most known scavenger receptors, LOX-1 may be the predominant scavenger receptor in vascular endothelial cell3,4. (globaltechbiz.com)
  • Several functions have been proposed for natural antibodies, including a first-line role in the defense against infections, a scavenger-like activity to apoptosis by-products and a turn-off, regulative role in the maintenance of immune homeostasis [ 7 , 14 ]. (biomedcentral.com)
  • IL-2 and IFN-γ), immune checkpoint blockade (ICB) therapy (e.g., anti-PD-1/PD-L1 antibodies), and adoptive T-cell transfer (e.g., chimeric antigen receptor (CAR) T-cell therapy) [ 3 - 5 ]. (thno.org)
  • In this review, we summarized the current knowledge of hemocyte-mediated phagocytosis, in particular focusing on the related receptors for recognition and internalization of pathogens as well as the downstream signal pathways and intracellular regulators involved in the process of hemocyte phagocytosis. (frontiersin.org)
  • Phagocytosis currently is described as an endocytic process that endogenous foreign particles or pathogens larger than 0.5 μm were first recognized by phagocyte surface receptor and then uptaken and engulfed into a plasma-membrane device, known as phagosome, following initiation of a signaling cascade to generate phagolysosome by fusion of phagosome with lysosomes. (frontiersin.org)
  • Higher molecular mass HA has been shown to support tissue integrity by forming minute fragments that initiate linkages that nurse an inflammatory response throughout an injury. (biotechnolabs.com)
  • Given this complexity, it is common to simplify chemokine, and chemokine receptor, biology by referring to them as being either homeostatic or inflammatory according to the contexts in which they predominantly function (2, 3). (eyesoftheelephants.com)
  • In contrast, inflammatory chemokines and their receptors are largely involved in responding to tissue insults, injuries, or infections. (eyesoftheelephants.com)
  • Inflammatory chemokines are not expressed at high levels at steady state but are rapidly and substantially transcriptionally activated following an inflammatory insult. (eyesoftheelephants.com)
  • We and others have demonstrated that ACKR2 is a highly efficient binder, internalizer, and scavenger of inflammatory CC-chemokines (12, 13). (eyesoftheelephants.com)
  • 6. Chimerical peptides according to the claim 1, characterized by containing a segment inhibitor of the activation of the NS3pro protease which comprise the region Asp50-Glu62 of the NS2B protein from DV2 or the structurally equivalent segment of the protein NS2B from other Flavivirus, or an amino acid sequence showing a sequence similarity higher of equal to the 80% identity. (patentsencyclopedia.com)
  • 8. Chimerical peptides according to the claim 1, characterized by containing a segment inhibitor of the activation of the NS3pro protease which comprise the region Thr20-Leu31 of the NS4A protein from HCV or the structurally equivalent segment of the protein NS4A from other Hepacivirus, or an amino acid sequence showing a sequence similarity higher of equal to the 80% identity. (patentsencyclopedia.com)
  • functions serve a catalytic non-muscle of folded, 18-21 wide scavenger sequence VDACs. (erik-mill.de)
  • The incidence of target organ damage associated to CVD increases with age, and gender studies show global higher incidence in men for stroke and coronary artery disease (CAD) [ 10 ]. (hindawi.com)
  • Such vaccination significantly improves protection against a new high-dose virulent challenge versus that in non-vaccinated convalescent animals. (nature.com)
  • We found that exposure to WIN 55,212-2 significantly reduced BDNF levels in hippocampus and frontal cortex. (researchgate.net)
  • It is an octapeptide (short chain of eight amino acids) with high selectivity and subnanomolar affinity for ACKR3. (innoget.com)
  • Instead, ACKR3 acts as a scavenger that sequestrates the secreted opioid peptides, thereby reducing the levels that can bind to traditional receptors and dampening their analgesic and antianxiety activity. (innoget.com)
  • ACKR3 is therefore a negative regulator of the opioid system with dual chemokine-opioid 'scavenging'activity and high drug targeting potential. (innoget.com)
  • high-specific S-IgA were observed in mucosal secretions, where showed a stronger anti-bacterial activity than their serum counterparts, supporting the primary role of S-IgA in controlling mucosal infections. (biomedcentral.com)
  • Relevant cellular senescence markers, such as X-gal staining, cell cycle regulator levels, and the percentage of cell cycle-arrested cells, were found to be reduced in the presence of naringenin. (hindawi.com)
  • Various cellular senescence hallmarks (the percentage of X-gal staining cells, the mRNA levels of the p16 and p21 cell cycle regulators, and the percentage of cell cycle-arrested cells) were investigated. (hindawi.com)
  • These isozymes synthesise different sizes of HA polymers, which are differentially regulated at the transcriptional, translational, and post-translational levels, which include epigenetic processes, sub-cellular localization, and alternative splicing. (biotechnolabs.com)
  • According to the studies, higher- and lower-MW HA interact with CD44 receptors to produce several biological effects through different molecular and cellular pathways. (biotechnolabs.com)
  • This article reviews the cellular receptors for HCV and suggests a general model for HCV entry into cells, in which lipoproteins play a crucial role. (biomedcentral.com)
  • In addition, cardiac markers of aging-induced damage, including radical oxidative species levels, mitochondrial metabolic activity, mitochondrial calcium buffer capacity, and estrogenic signaling functions, were also modulated by the compound. (hindawi.com)
  • in 2000 and in the original publication, the affinity of this compound for the 5-HT7 receptor was determined to be 10 nM15. (sarilumabinhibitor.com)
  • Selectivity profiling revealed high affinity for the 5-HT7 (Ki = 18 nM), σ-1 (Ki = 9.2 nM) and σ-2 (Ki = 1.6 nM) receptors. (sarilumabinhibitor.com)
  • Instead, we suggest exploration of this structural class, as results indicate that selective 5-HT7 receptor imaging might be possible when more selective non-P-gp substrates are identified. (sarilumabinhibitor.com)
  • HA may inhibit signal transmission via the HA receptors CD44 and RHAMM. (biotechnolabs.com)
  • Overall, B-DCs demonstrated higher expression of CD86 and CD172α than L-DCs, but both cell types expressed high levels of MHC class II and CD44, as well as moderate amounts of CD163, CD204, and Bla36. (biomedcentral.com)
  • HA is gaining recognition as a high-quality biomaterial scaffold in tissue engineering due to its biocompatibility and widespread presence in the ECM of tissues. (biotechnolabs.com)
  • In pig, high brain uptake and specific 5-HT7 and σ-receptor binding was found for [11C]Cimbi-701 without P- gp inhibition. (sarilumabinhibitor.com)
  • Conclusions: Both the specific σ-receptor binding and the low brain uptake of [11C]Cimbi- 701 displayed in baboons, discouraged further translation to humans. (sarilumabinhibitor.com)
  • According to the study, the HA-binding area on the cell surface is where PGs interact with HA receptors. (biotechnolabs.com)
  • all, at higher fragments, description deoxycorticosterone flux will interact again launched for absent configuration. (erik-mill.de)
  • We demonstrate that targeting the receptor-binding domain (RBD) of the SARS-CoV-2 spike protein to CD40 (αCD40.RBD) induces significant levels of specific T and B cells, with long-term memory phenotypes, in a humanized mouse model. (nature.com)
  • Some of these depend on the SR-B1 (scavenger receptor class B type I) and the adapter protein PDZK1 (postsynaptic density protein/Drosophila disc-large protein/Zonula occludens protein containing 1). (bvsalud.org)
  • Serum oxLDL levels are decreased in both lean and obese diabetic animals treated with TZDs. (jci.org)
  • Latest studies also show that blockade of LOX-1 by anti-sense oligo or antibody may decrease myocardial ischemic damage, genesis of hypertension and level of atherosclerosis5,6,7,8. (globaltechbiz.com)
  • The points in the figures showing no-observed-adverse-effect levels (NOAELs) or lowest- observed-adverse-effect levels (LOAELs) reflect the actual doses (levels of exposure) used in the studies. (cdc.gov)
  • Immunohistochemical and immunochemical investigations confirmed these observations at the protein level. (researchgate.net)
  • However, lowering LDL levels is a common clinical practice to reduce oxidation and the risk of major events in patients with cardiovascular diseases (CVD). (hindawi.com)
  • However, no clinical PET radiotracer exists for this receptor and thus we aimed to develop such a tracer. (sarilumabinhibitor.com)
  • As such, PET is a valuable tool to study the physiology of a respective biological system and to determine its involvement in certain diseases.5-7 PET can also be used during drug development processes and determine target engagement of a specific drug towards an enzymatic or receptor system.6 This information is very valuable for determining optimal dose regimes in clinical trials. (sarilumabinhibitor.com)
  • In binding humans, experimental phase tissues are also more severe than larger moderator receptors alveolar to the dimerization of architecture they are. (erik-mill.de)
  • The emergence of multifunctional nanomaterials can expectedly endow these therapeutic cargoes with high solubility, favorable pharmacokinetic distribution, cell-specific delivery, and controlled release. (thno.org)
  • Instead, these authors proposed that CD81 may be an attachment receptor with poor capacity to mediate the viral entry, and that reducing environments may not not favor CD81-HCV interaction. (biomedcentral.com)
  • In summary, the present data suggest that deficits of BDNF levels and signaling through ERK1/2 and alpha-CaMKII might contribute to cognitive and neuroplastic defects associated with prenatal exposure to cannabinoids. (researchgate.net)
  • The cardioprotective effects of Nar are well documented in the healthy state, in myocardial infarction, and in daunorubicin-, doxorubicin-, and high-glucose-induced cardiotoxicity [ 2 , 12 - 17 ]. (hindawi.com)
  • The distinction between 'less serious' effects and 'serious' effects is considered to be important because it helps the users of the profiles to identify levels of exposure at which major health effects start to appear. (cdc.gov)
  • Public health officials and others concerned with appropriate actions to take at hazardous waste sites may want information on levels of exposure associated with more subtle effects in humans or animals (LOAELs) or exposure levels below which no adverse effects (NOAELs) have been observed. (cdc.gov)
  • Molecular imprinting is a technology that facilitates the production of artificial receptors toward compounds of interest. (mdpi.com)
  • In this study, the binding affinity and mechanism of human odor-binding protein OBP2a to 14 typical odorants in water were first assessed using fluorescent competitive binding assays and molecular docking techniques. (springeropen.com)
  • Levels of significant exposure for each route and duration are presented in tables and illustrated in figures. (cdc.gov)
  • The significance of the exposure levels shown in the Levels of Significant Exposure (LSE) tables and figures may differ depending on the user's perspective. (cdc.gov)
  • The purpose of the present study was to determine whether mechanisms important for chemokine interactions with conventional chemokine receptors are conserved in the related atypical receptor ACKR2. (eyesoftheelephants.com)
  • Feature papers represent the most advanced research with significant potential for high impact in the field. (mdpi.com)