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Showing 1 to 18 of 18 for “"natural ligands"”.
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Biochemical Characterization of CXCR4 Interactions With HIV -1, Natural Ligands and De Novo Designed Inhibitors
… chemokine coreceptor, usually CXCR4 or CCR5. The natural ligand of CXCR4 is stromal cell-derived factor (SDF)-1alpha. Whereas the overlap between HIV-1 and SDF-1alpha functional sites on the extracellular domains of CXCR4 has been well documented, it is yet to be determined whether there are sites …
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COMPLEXATION AND PARTICLE-WATER INTERACTIONS OF NICKEL IN ESTUARIES
… in the Mersey, was bound to a class of strong ligands (log K'NIL = 19.0 ± 0.4 and 18.7 ± 0.5, respectively), which were saturated by the ambient concentrations of Ni throughout the estuaries, suggesting that the ligands are highly specific towards Ni. Irradiation of riverwater samples with UV …
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Recombinant CXCR4/CCR5 hybrid receptors as tools for studies of HIV-1 receptor usage
… use and a reduced sensitivity to inhibition by natural CCR5 ligands has also been described. With the aim to study interactions of natural ligands and HIV-1 isolates with these chemokine receptors, a set of hybrid CXCR4/CCR5 receptors were constructed. Signalling response to their respective …
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Iron limitation and the role of Siderophores in marine Synechococcus
… and compose an important portion of the pool of natural ligands that bind >99% of all soluble Fe. In bottle incubations from the Sargasso Sea we found the addition of Fe complexed to an excess of the siderophore desferrioxamine B (DFB) limited Synechococcus growth and stimulated the growth of …
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Novel genotoxins that target estrogen receptor- and androgen receptor- positive cancers : identification of DNA adducts, pharmacokinetics, and mechanism
… agents that contain an aniline mustard linked to ligands for tumor specific hormone receptors. To target ER(+) breast cancers, an aniline mustard was linked to estradiol at the 7[alpha] position (E2-7[alpha]), and to target AR(+) prostate cancer, the aniline mustard was linked to estradien-3-one …
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Iron limitation and the role of siderophores in marine Synechococcus
… and compose an important portion of the pool of natural ligands that bind >99% of all soluble Fe. In bottle incubations from the Sargasso Sea we found the addition of Fe complexed to an excess of the siderophore desferrioxamine B (DFB) limited Synechococcus growth and stimulated the growth of …
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A role for polyunsaturated fatty acids in Th1-mediated disease
… from CD4' T cells. PUFA are reported to be natural ligands for PPARy, therefore we investigated whether they exerted their effects on DC maturation by activation of this nuclear receptor. We found PPARy expression was enhanced in PUFA-treated DC, and confocal microscopy revealed an increased …
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OPENING NEW CHEMICAL SPACE IN DRUG DISCOVERY
… structure or mimicking the structure of known natural ligands. Their synthesis can be planned effectively with retrosynthetic analysis (Target-Oriented Synthesis, TOS). However, when the precise nature of the biological target is unknown, the structural features required in potentially …
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A Screen For Peptides Targeting Chemoresistant Metastatic Triple-Negative Breast Cancer
… phage-displayed cyclic peptides that mimic the natural ligands of novel receptors expressed by chemoresistant metastatic TNBC tumor cells. These peptides were termed Breast Lung Metastasis Peptides (BLMPs), owing to their pulmonary metastases-specific tropism. Two lead BLMPs were validated in …
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Organic Copper Binding Ligands and Thiol Compounds Produced by Bacteria and in the Elizabeth River, Virginia
… focusing on copper and organic copper binding ligands in laboratory cultures and the Elizabeth River, Virginia. Laboratory cultures of the marine bacterium <em>Vibrio parahaemolyticus </em>were used to demonstrate the influence of elevated copper concentrations on copper-complexing ligand and …
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Nanosecond Pulsed Electric Field Effects on Cell Cycle and Apoptosis
… has been extensively studied when induced by natural ligands, irradiation (IR), ultraviolet (UV) light, and chemical stimuli. Recently, apoptosis has been studied using a new technology that targets intracellular structures entitled nanosecond pulsed electric fields (nsPEF). NsPEF are high …
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Analysis of the function and subcellular localization of FAT/CD36 in hepatocytes and transfected cell lines of hepatic and non-hepatic origin.
… B scavenger receptor family. It has a number of natural ligands and has different functions at various locations in the body. It contributes to adhesion of platelets via its binding to thrombospondin-1. In monocytes and macrophages, it contributes to recognition and phagocytosis of apoptotic …
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The development of small molecule inhibitors for fibrosis drug discovery
… designed to mimic the tripeptide sequence of the natural ligands (arginine-glycine-aspartic acid); however, the RGD-mimetic antagonists for one particular RGD integrin (αIIbβ3) have been shown to cause partial agonism, leading to the opposite pharmacological effect.The challenge of obtaining oral …
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Controlling Microbial Multicellular Behaviors With Saccharide Derivatives
… unable to swarm on semi-solid agar gel. When the natural ligands, rhamnolipids were externally added into the semi-solid agar gel in a concentration dependent manner, the swarming of the rhlA mutant reactivated at lower concentrations (10 μM) and then at relatively higher concentrations (15 μM), …
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Copper and Zinc Speciation in the Tamar Estuary
… (DOC) on metal toxicity, the effectiveness of ligands from varying sources and of potentially variable composition in controlling speciation has not been studied in detail in estuarine waters. In addition, the effect of DOC on radionuclide contaminants in combination with trace metals has not …
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Natürliche Lebensmittelinhaltsstoffe als Liganden des Ah Rezeptors - Identifizierung und Charakterisierung von Beta-Carbolinen mit AhR Ligandenpotential mittels funktioneller Bioassays
In der vorliegenden Arbeit werden Studien zur Identifizierung und Charakterisierung von Lebensmittelinhaltsstoffen als natürliche Liganden des Ah Rezeptors („aryl hydrocarbon receptor“) vorgestellt. Der Ah Rezeptor ist ein liganden-abhängiger Transkriptionsfaktor, der an der Expression zahlreicher …
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Investigating spatial distribution and dynamics of membrane proteins in polymer-tethered lipid bilayer systems using single molecule-sensitive imaging techniques
… of membrane CHOL level versus binding of native ligands on the oligomerization state and distribution of GPI-anchored urokinase plasminogen activator receptor (uPAR) and the transmembrane protein αvβ3 integrin. Experiments on uPAR showed that receptor oligomerization and raft sequestration are …
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Investigation of Gut-Derived Circulating Succinate in Metabolism and Liver Signaling
… succinate and α-ketoglutarate are specific natural ligands for previously orphan receptors GPR91 (Sucnr1) and GPR99 (Oxgr1), respectively. The function of Sucnr1 is more extensively studied and its activation by succinate regulates pleiotropic biological processes. The physiological range of …