Synthesis,Characterization, and Biological Evaluation of a Dual-Action Ligand Targeting αvβ3 Integrin and VEGF Receptors

A dual-action ligand targeting both integrin α_Vβ₃ and vascular endothelial growth factor receptors (VEGFRs), was synthesized via conjugation of a cyclic peptidomimetic α_Vβ₃ Arg-Gly-Asp (RGD) ligand with a decapentapeptide. The latter was obtained from a known VEGFR antagonist by acetylation at the Lys13 side chain. Functionalization of the precursor ligands was carried out in solution and in the solid phase, affording two fragments: an alkyne VEGFR ligand and the azide integrin α_Vβ₃ ligand, which were conjugated by click chemistry. Circular dichroism studies confirmed that both the RGD and VEGFR ligand portions of the dual-action compound substantially adopt the biologically active conformation. In vitro binding assays on isolated integrin α_Vβ₃ and VEGFR-1 showed that the dual-action conjugate retains a good level of affinity for both its target receptors, although with one order of magnitude (10/20 times) decrease in potency. The dual-action ligand strongly inhibited the VEGF-induced morphogenesis in Human Umbilical Vein Endothelial Cells (HUVECs). Remarkably, its efficiency in preventing the formation of new blood vessels was similar to that of the original individual ligands, despite the worse affinity towards integrin α_Vβ₃ and VEGFR-1.     

Thermal stresses in plane elasticity: Numerical solutions based only on harmonic functions

Summary A theoretical treatment is outlined allowing solution of thermal stress problems in plane elasticity by using only numerical methods suited to solving — in 2 D — the Laplace equation. Only one type of element matrix (supposing for the sake of simplicity F.E.M.s are used) and only one mesh would thus be required, both for the determination of the thermal field and of the displacement/stress field. The numerical solutions required in the plane domain of interest entail, consequently, only one variable per node in place of two. Even if numerous unit solutions are required in order to impose arbitrary boundary conditions, this reduction of nodal variables allows to spend less computation time in solving linear systems, at least for problems of a certain extent.

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Sommario Si delinea una tecnica che permette di risolvere i problemi di coazioni termiche in elasticità piana facendo uso solo di metodi numerici atti a risolvere l'equazione di Laplace. Un solo tipo di matrice degli elementi (nel caso si usi una formulazione a E. F.) e una sola reticolazione sono pertanto richiesti tanto per il problema termico come per quello elastico. Ne consegue altresì il vantaggio che le soluzioni numeriche richieste nel dominio di interesse cornportano una sola variabile per nodo, anzichè due; anche tenuto conto che sono richieste numerose soluzioni unitarie per poter imporre condizioni al contorno comunque definite, ne deriva per problemi di una certa ampiezza una riduzione del tempo di calcolo speso nella soluzione di sistemi.

     

Diffeomorphism-invariant properties for quasi-linear elliptic operators

For quasi-linear elliptic equations we detect relevant properties which remain invariant under the action of a suitable class of diffeomorphisms. This yields a connection between existence theories for equations with degenerate and nondegenerate coerciveness.     

Investigation of the Homologous Series of 4-Acetyl-4′-n-Alkanoyloxyazobenzenes by X-ray Diffraction

This paper reports an investigation by X-ray diffraction of the homologous series of liquid crystalline 4-acetyl-4′-n-alkanoyloxyazobenzenes. By using two independent parameters, namely the temperature and the paraffinic chain length, it was possible to obtain some structural information on two solid phases for comparison with a previously reported model for the S_A phase of the same series. In particular, the molecular layer thickness and, by using previously reported dilatometric data, the aromatic sublayer thickness, the methylene group thickness, the molecular area and the aromatic stem inclination angle were obtained for the different phases.     

Existence of maximizers for Sobolev–Strichartz inequalities

We prove the existence of maximizers of Sobolev–Strichartz estimates for a general class of propagators, involving relevant examples, as for instance the wave, Dirac and the hyperbolic Schrödinger flows.     

Synthesis of aggregation pheromone components of cerambycid species through α-hydroxylation of alkylketones

The synthesis of 3-hydroxy-2-hexanone and 2,3-hexanediol, two components of the aggregation pheromone of several cerambycid species, is disclosed in here. Starting from 2-hexanone, through an α-hydroxylation using (diacetoxyiodo)benzene, 3-hydroxy-2-hexanone is obtained in good yield. Further reduction of this compound, gives 2,3-hexanediol in excellent yield. A study of the α-hydroxylation reaction of several alkylketones using an hypervalent iodine reagent is also disclosed in here. The synthesis of optically active compounds (R)- and (S)-3-hydroxy-2-hexanone was achieved starting from 2-hexanone with nitrosobenzene and l- and d-proline respectively, in several reaction media.     

Ionic electroactive polymer metal composites: Fabricating,modeling, and applications of postsilicon smart devices

Smart systems adapt to the surrounding environments in a number of ways. They are capable to scavenge energy from available sources, sense and elaborate external stimuli and adequately react. Electro Active Polymers are playing a main role in the realization of smart systems for applications if fields such as bio inspired and autonomous robotics, medicine, and aerospace. This paper focus on the possibility to use Ionic Polymer Metal Composites as a class of materials relevant to the realization of post silicon smart systems. The three main aspects of this new technology, i.e., fabrication methods, modeling, and applications are described with emphasis to most recent results. Attention is given to main challenges and shortcomings to be solved for technology, modelling, and control of IPMC based devices that need to be solved before this new technology can be fully exploited in real world applications. © 2013 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2013