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Highest Binding Affinity (highest + binding_affinity)
Selected AbstractsBinding Properties of 2-Pentyl Pyridine to Soy Protein as Measured by Solid Phase MicroextractionJOURNAL OF FOOD SCIENCE, Issue 1 2002A. Zhou ABSTRACT: The binding properties of 2-pentyl pyridine (2-pp) were investigated for soybean protein isolates (SPI) and the beta-conglycinin and glycinin soy protein fractions. The glycinin fraction had the highest binding affinities for 2-pp, followed by beta-conglycinin fraction, and then SPI. More 2-pp was bound by SPI and beta-conglycinin or glycinin fractions under alkaline conditions than under neutral conditions, which exhibited more binding than acidic conditions. More 2-pp was also bound at high temperature (74 °C) than at 25 °C, but greater binding affinity of 2-pp was observed at 4 °C than at 25 °C. With increased NaCl concentrations, the binding affinity of 2-pp decreased. Exposure to UV light increased binding of 2-pp to all types of soy protein. [source] Small potent ligands to the insulin-regulated aminopeptidase (IRAP)/AT4 receptorJOURNAL OF PEPTIDE SCIENCE, Issue 7 2007Andreas Axén Abstract Angiotensin IV analogs encompassing aromatic scaffolds replacing parts of the backbone of angiotensin IV have been synthesized and evaluated in biological assays. Several of the ligands displayed high affinities to the insulin-regulated aminopeptidase (IRAP)/AT4 receptor. Displacement of the C -terminal of angiotensin IV with an o -substituted aryl acetic acid derivative delivered the ligand 4, which exhibited the highest binding affinity (Ki = 1.9 nM). The high affinity of this ligand provides support to the hypothesis that angiotensin IV adopts a ,-turn in the C -terminal of its bioactive conformation. Ligand (4) inhibits both human IRAP and aminopeptidase N-activity and induces proliferation of adult neural stem cells at low concentrations. Furthermore, ligand 4 is degraded considerably more slowly in membrane preparations than angiotensin IV. Hence, it might constitute a suitable research tool for biological studies of the (IRAP)/AT4 receptor. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd. [source] Synthesis of 2-Fluoro N10 -Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation StudiesARCHIV DER PHARMAZIE, Issue 11 2009Yergeri C. Mayur Abstract A series of 2-fluoro N10 -substituted acridone derivatives with varying alkyl side chain length with propyl, butyl substitution, and a tertiary amine group at the terminal end of the alkyl side chain were synthesized and screened against cancer cell lines SW 1573, SW 1573 2R 160 (P-gp substrate) which are non-small lung cancer cell lines, MCF-7, MCF-7/MR (BCRP substrate) are breast cancer cell lines, 2008 WT, 2008MRP1, 2008MRP2, 2008MRP3 are ovarian cancer cell lines, and human embryo kidney cell lines like HEK293, HEK293 MRP4, and HEK293 MRP5i. The propyl-series compounds showed lipophilicity in the range of 1.93 to 4.40 and the butyl series in the range of 2.37 to 4.78. The compounds 4, 7, and 8 showed good cytotoxicity against the 60 human cancer cell line panel of the National Cancer Institute, USA. The compounds 14 and 15 showed a better cytotoxicity in most of the cancer cell lines compared to other compounds tested. The DNA-binding properties of the compounds were evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compound 11 bearing planar tricyclic ring linked with a butyl methylpiperazino side chain showed the highest binding affinity with a binding constant (Ki) of 10.38×10 M,1. Evaluation of the compounds in cell lines with an overexpression of various multidrug resistance-related protein (MRP), P-glycoprotein (P-gp), or Breast Cancer Resistance Protein (BCRP) showed that all compounds are not substrates for any of these transporters. [source] SALIVATION TRIGGERED BY PILOCARPINE INVOLVES AQUAPORIN-5 IN NORMAL RATS BUT NOT IN IRRADIATED RATSCLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 5-6 2009Tetsuya Asari SUMMARY 1Using rats, we examined the muscarinic receptor subtype mediating pilocarpine-induced parotid salivary secretion and the contributions of ion transporter systems (effluxes of K+ and Cl - ) and aquaporin-5 (AQP5) translocation to this response in parotid glands in irradiated-induced xerostomia. 2Salivary secretion was significantly lower in irradiated compared with sham-irradiated (normal) rats. In xerostomia rats, 0.4 and 0.8 mg/kg pilocarpine significantly increased parotid salivary secretion, although the salivary volume was still significantly less than in normal rats after the same dose of pilocarpine. 3Pirenzepine (1 × 10,6 to 1 × 10,1 mol/L), AF-DX 116 (3 × 10,6 to 3 × 10,2 mol/L) and N -2-chloroethyl-4-piperidinyl diphenylacetate (4-DAMP; 1 × 10,8 to 1 × 10,2 mol/L) dose-dependently displaced radioligand binding to M1, M2 and M3 receptors, respectively, in parotid membranes from both normal and irradiated rats. In each group of rats, 4-DAMP had the highest binding affinity. Pretreatment with 4-DAMP or pirenzepine dose-dependently inhibited pilocarpine-induced parotid secretion in both normal and irradiated rats, with 4-DAMP being markedly more potent than pirenzepine. 4Normal and irradiated-rat parotid cells did not differ significantly in terms of pilocarpine-induced changes in [Ca2+]i, [K+]i and [Cl - ]i. Pilocarpine markedly increased the amount of AQP5 in the apical plasma membrane of parotid cells isolated from normal but not irradiated rats. 5Thus, pilocarpine induces parotid salivary secretion mainly via the M3 receptor subtype in both irradiated and normal rats. The reduction in this pilocarpine-induced secretion seen in irradiated rats is due not to disturbances of intracellular Ca2+ mobilization or ion transporter systems, but rather to a disturbance of AQP5 translocation, which may be involved in the pathogenesis of X-ray irradiation-induced xerostomia. [source] | ||||||||||