Fluorous Iminoalditols: A New Family of Glycosidase Inhibitors and Pharmacological Chaperones

A collection of new reversible glycosidase inhibitors of the iminoalditol type featuring N‐substituents containing perfluorinated regions has been prepared for evaluation of physicochemical, biochemical and diagnostic properties. The vast variety of feasible oligofluoro moieties allows for modular approaches to customised structures according to the intended applications, which are influenced by the fluorine content as well as the distance of the fluorous moiety from the ring nitrogen. The first examples, in particular in the D ‐galacto series, exhibited excellent inhibitory activities. A preliminary screen with two human cell lines showed that, at subinhibitory concentrations, they are powerful pharmacological chaperones enhancing the activities of the catalytically handicapped lysosomal D ‐galactosidase mutants associated with GM1 gangliosidosis and Morquio B disease.     

Composite gel-filled giant vesicles: Membrane homogeneity and mechanical properties

We further investigate the properties of composite Poly(NIPAM) (poly(N-isopropylacrylamide)) gel-filled giant vesicles, focusing here on i) the homogeneity of the membrane, ii) its coupling to the inner gel under strong suction pressures, and iii) the relation between the final elastic modulus of the vesicles and the amount of crosslinker in the pre-gel medium. We show that whereas the photo-polymerization process induces a decrease of the membrane homogeneity at the micrometer size range, the membrane still remains strongly coupled to the internal gel network. The vesicles studied here display average moduli in the range [0.5–25] kPa, confirming their potential as biomimetic mechanical systems.     

Wasserstoffinduzierte Spannungsrißkorrosion an unverzinkten und verzinkten Baustählen

Hydrogen induced stress corrosion cracking of non galvanized and galvanized construction steels The processes of atmospheric corrosion and corrosion in collected water which may lead to hydrogen induced stress corrosion cracking of high-strength reinforcing steels in casing tubes before injection with concrete are discussed. Hydrogen uptake during corrosion occurs in weakly acid solutions as well as in neutral or alkaline aqueous solutions. The hydrogen uptake by proton discharge in acid solutions decreases with increasing pH of the electrolyte. Hydrogen can also be absorbed in neutral to weakly alkaline solutions if steels are plastically deformed and water reacts with the fresh iron surface. In alkaline solutions, hydrogen uptake is possible if, at the generally passivated steel surface, localized corrosion (pitting or crevice corrosion), local galvanic cells and a sufficient decrease in the pH of the pit electrolyte occurs. In the case of galvanized steels with damaged zinc layers, hydrogen uptake may result from the cathodic polarization of the free steel surface by zinc dissolution. The absorbed hydrogen interacts with the microstructure of the steels and weakens the bonds between the iron atoms. The influence of the microstructure of high-strength steels on the fracture behaviour is discussed on the basic of the so-called decohesion theory.     

The dynamic neural filter: a binary model of spatiotemporal coding

We describe and discuss the properties of a binary neural network that can serve as a dynamic neural filter (DNF), which maps regions of input space into spatiotemporal sequences of neuronal activity. Both deterministic and stochastic dynamics are studied, allowing the investigation of the stability of spatiotemporal sequences under noisy conditions. We define a measure of the coding capacity of a DNF and develop an algorithm for constructing a DNF that can serve as a source of given codes. On the basis of this algorithm, we suggest using a minimal DNF capable of generating observed sequences as a measure of complexity of spatiotemporal data. This measure is applied to experimental observations in the locust olfactory system, whose reverberating local field potential provides a natural temporal scale allowing the use of a binary DNF. For random synaptic matrices, a DNF can generate very large cycles, thus becoming an efficient tool for producing spatiotemporal codes. The latter can be stabilized by applying to the parameters of the DNF a learning algorithm with suitable margins.     

Path-breaking books in regional science

This article presents a collection of regional science books that longstanding members of the Regional Science Association International (RSAI) identified as path-breaking books. The most frequently nominated books include the classics by Isard, the seminal books in urban economics by Alonso, Muth and Mills, methods books by Miernyk, Wilson, Anselin, and Cliff and Ord, textbooks by Beckmann and Richardson, as well as the recent contribution by Fujita, Krugman and Venables. Reviews of these books, written by leading scholars from different continents, make up the major contribution of this article and are a testimony to the far-reaching influence of regional science in the academic literature.JEL Classification: A2, B2, B3, C00, R00With contributions by Michael Batty, Manas Chatterji, Kieran Donaghy, Bernard Fingleton, Arthur Getis, Michael J. Greenwood, Daniel P. McMillen, Gordon F. Mulligan, Jan Oosterhaven,Peter V. Schaeffer, Daniel Shefer. See the Appendix for contributors affiliations and contact information.     

87Sr/86Sr from rock and soil into vine and wine

For provenance assignments of wines strontium isotope ratios can be used because soils from different wine-growing regions, and hence the wines grown there, each show specific ratios. Some successful applications are demonstrated.

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⁸⁷Sr/⁸⁶Sr aus Gestein und Boden in Rebe und Wein

Zusammenfassung Zur Herkunftsbestimmung von Weinen können Strontium-Isotopenverhältnisse herangezogen werden, da die Böden verschiedener Weinbaugebiete, und damit die dort gezogenen Weine, jeweils spezifische Verhältnisse aufweisen. Einige erfolgreiche Anwendungen werden demonstriert.

     

Modélisation par méthode de propagation de faisceau à partir d’un coupleur à champ évanescent

We present numerical results obtained by 3D-BPM concerning evanescent field coupling in monomode fibres. At first we study the coupling between a monomode fibre and a mode sink. We show the existence or the absence of guided modes. BPM, is also applied to the study of directional couplers consisting of two fibres separated by an index liquid. The transmission coefficient is computed for various geometries and the electric field intensity is visualised by plotting isovalues.     

Influence of Host-Plant Surface Chemicals on the Oviposition of the Cereal Stemborer Busseola Fusca

The chemical composition of plant surfaces plays a role in selection of host plants by herbivorous insects. Once the insect reaches the plant, these cues determine host acceptance. Laboratory studies have shown that the stem borer Busseola fusca (Lepidoptera: Noctuidae), an important pest of sorghum and maize in sub-Saharan Africa, is able to differentiate between host and non-host plant species. However, no information is available on the cues used by this insect to seek and accept the host plant. Thus, the role of surface phytochemical stimuli on host selection and oviposition by B. fusca was studied in the laboratory using two host plants, sorghum, Sorghum bicolor, and maize, Zea mays, and one non-host plant, Napier grass, Pennisetum purpureum. The numbers of eggs and egg masses deposited on the three plant species were compared first under no-choice and choice conditions. In both cases, more eggs and egg masses were laid on maize and sorghum than on the non-host. Artificial surrogate stems treated with a water or chloroform surface extract of each plant were then compared with surrogate stems treated with, respectively, water or chloroform as controls, under similar conditions. Surrogate stems treated with plant water extracts did not show an increase in oviposition when compared to controls, indicating that the major compounds in these extracts, i.e., simple sugars and free amino acids, are not significantly responsible for the oviposition preference. By contrast, a chloroform extract of sorghum enhanced oviposition on the surrogate stems compared to the control, while those of maize and Napier grass showed no significant effects. Analysis of the chloroform extract of sorghum showed higher amounts of α-amyrin, ß-amyrin, and n-nonacosane compared to those of maize and Napier grass. A blend of the three chemicals significantly increased oviposition compared to the chloroform-treated control, indicating that these compounds are part of the surface chemical signature of the plant responsible for host recognition and oviposition by B. fusca.     

The Tyrosine Gate of the Bacterial Lectin FimH: A Conformational Analysis by NMR Spectroscopy and X‐ray Crystallography

Urinary tract infections caused by uropathogenic E. coli are among the most prevalent infectious diseases. The mannose‐specific lectin FimH mediates the adhesion of the bacteria to the urothelium, thus enabling host cell invasion and recurrent infections. An attractive alternative to antibiotic treatment is the development of FimH antagonists that mimic the physiological ligand. A large variety of candidate drugs have been developed and characterized by means of in vitro studies and animal models. Here we present the X‐ray co‐crystal structures of FimH with members of four antagonist classes. In three of these cases no structural data had previously been available. We used NMR spectroscopy to characterize FimH–antagonist interactions further by chemical shift perturbation. The analysis allowed a clear determination of the conformation of the tyrosine gate motif that is crucial for the interaction with aglycone moieties and was not obvious from X‐ray structural data alone. Finally, ITC experiments provided insight into the thermodynamics of antagonist binding. In conjunction with the structural information from X‐ray and NMR experiments the results provide a mechanism for the often‐observed enthalpy–entropy compensation of FimH antagonists that plays a role in fine‐tuning of the interaction.