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Highly Hydrophobic (highly + hydrophobic)
Selected AbstractsSolution Structure of , -Am2766: A Highly Hydrophobic , -Conotoxin from Conus amadis That Inhibits Inactivation of Neuronal Voltage-Gated Sodium ChannelsCHEMISTRY & BIODIVERSITY, Issue 4 2005Siddhartha The three-dimensional (3D) NMR solution structure (MeOH) of the highly hydrophobic , -conotoxin , -Am2766 from the molluscivorous snail Conus amadis has been determined. Fifteen converged structures were obtained on the basis of 262 distance constraints, 25 torsion-angle constraints, and ten constraints based on disulfide linkages and H-bonds. The root-mean-square deviations (rmsd) about the averaged coordinates of the backbone (N, C,, C) and (all) heavy atoms were 0.62±0.20 and 1.12±0.23,Ĺ, respectively. The structures determined are of good stereochemical quality, as evidenced by the high percentage (100%) of backbone dihedral angles that occupy favorable and additionally allowed regions of the Ramachandran map. The structure of , -Am2766 consists of a triple-stranded antiparallel , -sheet, and of four turns. The three disulfides form the classical ,inhibitory cysteine knot' motif. So far, only one tertiary structure of a , -conotoxin has been reported; thus, the tertiary structure of , -Am2766 is the second such example. Another Conus peptide, Am2735 from C. amadis, has also been purified and sequenced. Am2735 shares 96% sequence identity with , -Am2766. Unlike , -Am2766, Am2735 does not inhibit the fast inactivation of Na+ currents in rat brain Nav1.2 Na+ channels at concentrations up to 200,nM. [source] Novel ,-carboxyglutamic acid-containing peptides from the venom of Conus textileFEBS JOURNAL, Issue 12 2006Eva Czerwiec The cone snail is the only invertebrate system in which the vitamin K-dependent carboxylase (or ,-carboxylase) and its product ,-carboxyglutamic acid (Gla) have been identified. It remains the sole source of structural information of invertebrate ,-carboxylase substrates. Four novel Gla-containing peptides were purified from the venom of Conus textile and characterized using biochemical methods and mass spectrometry. The peptides Gla(1),TxVI, Gla(2),TxVI/A, Gla(2),TxVI/B and Gla(3),TxVI each have six Cys residues and belong to the O -superfamily of conotoxins. All four conopeptides contain 4- trans -hydroxyproline and the unusual amino acid 6- l -bromotryptophan. Gla(2),TxVI/A and Gla(2),TxVI/B are isoforms with an amidated C-terminus that differ at positions +1 and +13. Three isoforms of Gla(3),TxVI were observed that differ at position +7: Gla(3),TxVI, Glu7,Gla(3),TxVI and Asp7-Gla(3),TxVI. The cDNAs encoding the precursors of the four peptides were cloned. The predicted signal sequences (amino acids ,46 to ,27) were nearly identical and highly hydrophobic. The predicted propeptide region (,20 to ,1) that contains the ,-carboxylation recognition site (,-CRS) is very similar in Gla(2),TxVI/A, Gla(2),TxVI/B and Gla(3),TxVI, but is more divergent for Gla(1),TxVI. Kinetic studies utilizing the Conus,-carboxylase and synthetic peptide substrates localized the ,-CRS of Gla(1),TxVI to the region ,14 to ,1 of the polypeptide precursor: the Km was reduced from 1.8 mm for Gla (1),TxVI lacking a propeptide to 24 µm when a 14-residue propeptide was attached to the substrate. Similarly, addition of an 18-residue propeptide to Gla(2),TxVI/B reduced the Km value tenfold. [source] Reversibly Light-Switchable Wettability of Hybrid Organic/Inorganic Surfaces With Dual Micro-/Nanoscale RoughnessADVANCED FUNCTIONAL MATERIALS, Issue 8 2009Gianvito Caputo Abstract Here, an approach to realize "smart" solid substrates that can convert their wetting behavior between extreme states under selective light irradiation conditions is described. Hybrid organic/inorganic surfaces are engineered by exploiting photolithographically tailored SU-8 polymer patterns as templates for accommodating closely packed arrays of colloidal anatase TiO2 nanorods, which are able to respond to UV light by reversibly changing their surface chemistry. The TiO2 -covered SU-8 substrates are characterized by a dual micro-/nanoscale roughness, arising from the overlapping of surfactant-capped inorganic nanorods onto micrometer-sized polymer pillars. Such combined architectural and chemical surface design enables the achievement of UV-driven reversible transitions from a highly hydrophobic to a highly hydrophilic condition, with excursions in water contact angle values larger than 100°. The influence of the geometric and compositional parameters of the hybrid surfaces on their wettability behavior is examined and discussed within the frame of the available theoretical models. [source] Separation and quantification of 9-(alkylthio)acridines by capillary micellar electrokinetic chromatography and capillary liquid chromatographyJOURNAL OF SEPARATION SCIENCE, JSS, Issue 13 2007Jana Nejmanová Abstract Various thioacridine derivatives are potential chemotherapeutics against various diseases which are intensively synthesized, characterized, and investigated by many research groups. Efficient, fast, and reliable separation and quantification methods for their analysis are still to be developed. MEKC and capillary LC (CLC) were applied for the separation and quantification of five highly hydrophobic, weakly basic, and structurally similar 9-(alkylthio)acridines. Since the common anionic and cationic surfactants failed to separate the strongly hydrophobic thioacridines by MEKC, sodium cholate was used in an alkaline BGE and successfully employed for their fast separation. In CLC, the weakly basic nature of the thioacridines necessitated use of LiChrosorb RP-select B sorbent as the stationary phase, which combined with a very simple mobile phase methanol/water yielded an efficient chromatographic separation system. Both, the MEKC and CLC optimized separation methods were then applied to quantify the thioacridines within a concentration range of 1.0×10,5,1.0×10,3 mol/L and the obtained experimental results were critically compared. In practical terms, the MEKC analytical method can quantify the analytes much faster but with a lower reliability while the CLC method performs slower analysis with a higher repeatability of the experimental results. [source] Synthesis of Poly(lauryl acrylate) by Single-Electron Transfer/Degenerative Chain Transfer Living Radical Polymerization Catalyzed by Na2S2O4 in WaterMACROMOLECULAR CHEMISTRY AND PHYSICS, Issue 11 2007Jorge F. J. Coelho Abstract Living radical polymerization of lauryl acrylate was achieved by SET/DTLRP in water catalyzed by sodium dithionite. The work describes the synthesis of a highly hydrophobic and polar monomer in aqueous medium. The plots of versus conversion and ln[M]0/[M] versus time are linear, indicating a controlled polymerization. This method leads to ,,, -diiodopoly(lauryl acrylate)s that can be further functionalized. The MWDs were determined using a combination of three detectors: RALLS, DV, and RI. The method studied in this work represents a possible route to prepare well-tailored macromolecules made of LA in environment friendly reaction medium. The syndiotactic content is 75%. [source] Enhanced resolution of glycosylphosphatidylinositol-anchored and transmembrane proteins from the lipid-rich myelin membrane by two-dimensional gel electrophoresisPROTEINS: STRUCTURE, FUNCTION AND BIOINFORMATICS, Issue 7 2003Christopher M. Taylor Abstract Two-dimensional gel electrophoresis (2-DE) has become a powerful and widely used technique for proteomic analyses. However, the limited ability of 2-DE to resolve transmembrane and glycosylphosphatidylinositol (GPI)-anchored proteins has slowed the identification of proteins from membrane-rich biological samples. Myelin is an unusually lipid-rich membrane with relatively few major proteins but many quantitatively minor proteins, most of which have an unknown identity and/or function. The goal of this study was to identify the optimal conditions of 2-DE for the separation of myelin proteins. We have identified two detergents, the nonionic n -dodecyl ,- D -maltoside and the zwitterionic amidosulfobetaine ASB-14, that are more effective in solubilizing myelin proteins than the commonly used zwitterionic detergent 3-[(3-cholamidopropyl)- dimethylammonio]-1-propanesulfonate (CHAPS). These detergents significantly enhance the solubility of both transmembrane (e.g., the highly hydrophobic and multiply acylated myelin proteolipid protein) and GPI-anchored (e.g., contactin and neuronal cell adhesion molecule) myelin proteins and enable their resolution by 2-DE. We conclude that these detergents are effective tools for the 2-DE analysis of myelin, and that they may be more generally useful for the analysis of membrane-rich biological samples. [source] Controllable microfluidic synthesis of multiphase drug-carrying lipospheres for site-targeted therapyBIOTECHNOLOGY PROGRESS, Issue 4 2009Kanaka Hettiarachchi Abstract We report the production of micrometer-sized gas-filled lipospheres using digital (droplet-based) microfluidics technology for chemotherapeutic drug delivery. Advantages of on-chip synthesis include a monodisperse size distribution (polydispersity index (,) values of <5%) with consistent stability and uniform drug loading. Photolithography techniques are applied to fabricate novel PDMS-based microfluidic devices that feature a combined dual hydrodynamic flow-focusing region and expanding nozzle geometry with a narrow orifice. Spherical vehicles are formed through flow-focusing by the self-assembly of phospholipids to a lipid layer around the gas core, followed by a shear-induced break off at the orifice. The encapsulation of an extra oil layer between the outer lipid shell and inner bubble gaseous core allows the transport of highly hydrophobic and toxic drugs at high concentrations. Doxorubicin (Dox) entrapment is estimated at 15 mg mL,1 of particles packed in a single ordered layer. In addition, the attachment of targeting ligands to the lipid shell allows for direct vehicle binding to cancer cells. Preliminary acoustic studies of these monodisperse gas lipospheres reveal a highly uniform echo correlation of greater than 95%. The potential exists for localized drug concentration and release with ultrasound energy. © 2009 American Institute of Chemical Engineers Biotechnol. Prog., 2009 [source] Solution Structure of , -Am2766: A Highly Hydrophobic , -Conotoxin from Conus amadis That Inhibits Inactivation of Neuronal Voltage-Gated Sodium ChannelsCHEMISTRY & BIODIVERSITY, Issue 4 2005Siddhartha The three-dimensional (3D) NMR solution structure (MeOH) of the highly hydrophobic , -conotoxin , -Am2766 from the molluscivorous snail Conus amadis has been determined. Fifteen converged structures were obtained on the basis of 262 distance constraints, 25 torsion-angle constraints, and ten constraints based on disulfide linkages and H-bonds. The root-mean-square deviations (rmsd) about the averaged coordinates of the backbone (N, C,, C) and (all) heavy atoms were 0.62±0.20 and 1.12±0.23,Ĺ, respectively. The structures determined are of good stereochemical quality, as evidenced by the high percentage (100%) of backbone dihedral angles that occupy favorable and additionally allowed regions of the Ramachandran map. The structure of , -Am2766 consists of a triple-stranded antiparallel , -sheet, and of four turns. The three disulfides form the classical ,inhibitory cysteine knot' motif. So far, only one tertiary structure of a , -conotoxin has been reported; thus, the tertiary structure of , -Am2766 is the second such example. Another Conus peptide, Am2735 from C. amadis, has also been purified and sequenced. Am2735 shares 96% sequence identity with , -Am2766. Unlike , -Am2766, Am2735 does not inhibit the fast inactivation of Na+ currents in rat brain Nav1.2 Na+ channels at concentrations up to 200,nM. [source] | |||||||||||||