1,721,118 research outputs found

    Cis-(hydrido)hydrocarbylplatinum(IV) complexes as intermediates in the Pt(II)-C bond breaking

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    The geometrical isomerism at equilibrium of Pt(IV) derivatives of general formula [Pt(CH3)2(R)X(NN)] (NN2,9-dimethyl-1,10-phenanthroline or 1,10-phenanthroline; R sigma C-bonded ligand; X halide) has been investigated by variation of R, X, and NN. The complexes have been obtained mainly through oxidative addition of RX to [Pt(CH3)2(NN)]. Some general trends can be traced in the relative stability of the geometrical isomers of the complexes, and attempts to discriminate sterical and electronic factors have been presented. The first attainment of a compound of the general formula [Pt(CH3)2(R)R(NN)] containing three different types of s C-bonded groups is also reported

    Peptide containing vesicles as selective nanocarriers for therapeutics and diagnostics.

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    One strategy to achieve cancer-targeted drug delivery is the labeling of the supramol. aggregates with bioactive markers such as peptides. Through design, synthesis, and physicochem. characterization, target-specific supramol. aggregates, contg. a surface-exposed bioactive CCK8 peptide for selective delivery, were developed. The peptide contg. supramol. aggregates were obtained by mixing two different amphiphilic monomers: one of them contg. a chelating agent able to complex a metal ion and the other the bioactive CCK8 peptide able to bind, with nanomolar affinity, cholecystokinin subtype receptors. In vitro and in vivo biol. tests on 111In labeled vesicles confirm that peptide contg. supramol. aggregates give the desired specific receptor targeting, thus indicating that CCK8 peptide adopts the expected conformation also when it is bound to supramol. aggregates. The demonstrated efficiency of surface exposed peptides in homing nanovectors to a specific target, the long plasma half-life and the no acute toxicity of the studied aggregates, give promising opportunities for the development of pharmaceutical agents with high specificity toward the biol. target and reduced toxic side effects on non-target organs

    Esercitazioni Numeriche e di Laboratorio di Chimica di Base

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    Il testo si propone di introdurre i concetti della chimica di base per gli studenti delle lauree triennali mediante esercitazioni pratiche numeriche e di laboratorio

    Liposomes derivatized with tetrabranched Neurotensin peptide via click chemistry reactions

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    Liposomes decorated with Neurotensin tetramers are obtained by using a post-liposomal derivatization method in which a click-chemistry reaction between liposomes containing azido functions on the external surface and branched neurotensin peptides modified for the presence of a C-C triple-bond is performed

    Receptor binding peptides for target-selective delivery of nanoparticles encapsulated drugs

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    Active targeting by means of drug encapsulated nanoparticles decorated with targeting bioactive moieties represents the next frontier in drug delivery; it reduces drug side effects and increases the therapeutic index. Peptides, based on their chemical and biological properties, could have a prevalent role to direct drug encapsulated nanoparticles, such as liposomes, micelles, or hard nanoparticles, toward the tumor tissues. A considerable number of molecular targets for peptides are either exclusively expressed or overexpressed on both cancer vasculature and cancer cells. They can be classified into three wide categories: integrins; growth factor receptors (GFRs); and G-protein coupled receptors (GPCRs). Therapeutic agents based on nanovectors decorated with peptides targeting membrane receptors belonging to the GPCR family overexpressed by cancer cells are reviewed in this article. The most studied targeting membrane receptors are considered: somatostatin receptors; cholecystokinin receptors; receptors associated with the Bombesin like peptides family; luteinizing hormone-releasing hormone receptors; and neurotensin receptors. Nanovectors of different sizes and shapes (micelles, liposomes, or hard nanoparticles) loaded with doxorubicin or other cytotoxic drugs and externally functionalized with natural or synthetic peptides are able to target the overexpressed receptors and are described based on their formulation and in vitro and in vivo behaviors
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