Search results for "IPR"

The size of aryl linker between two polyaza-cyclophane moieties controls the binding selectivity to ds-RNA vs ds-DNA

2013

Aryl-linked (pyridine- vs. phenanthroline-) bis-polyaza pyridinophane scorpiands PYPOD and PHENPOD strongly bind to the double stranded DNA and RNA, whereby very intriguing RNA over DNA selectivity is finely tuned by aryl-linker length and aromatic surface. Moreover, PYPOD and PHENPOD dimer formation at high compound/polynucleotide ratios is highly sensitive to the fine interplay between the steric and binding properties of compound-dimers and the DNA minor groove/RNA major groove. That is demonstrated by significantly different induced CD spectra, which allow spectroscopic differentiation between various DNA/RNA secondary structures. A significantly higher (micromolar) antiproliferative ef…

RIPRODUZIONE E CICLO CELLULARE

2007

Simultaneous stimulation of GABA and beta adrenergic receptors stabilizes isotypes of activated adenylyl cyclase heterocomplex

2004

Abstract Background We investigated how the synthesis of cAMP, stimulated by isoproterenol acting through β-adrenoreceptors and Gs, is strongly amplified by simultaneous incubation with baclofen. Baclofen is an agonist of δ-aminobutyric acid type B receptors [GABAB], known to inhibit adenylyl cyclase via Gi. Because these agents have opposite effects on cAMP levels, the unexpected increase in cAMP synthesis when they are applied simultaneously has been intensively investigated. From previous reports, it appears that cyclase type II contributes most significantly to this phenomenon. Results We found that simultaneous application of isoproterenol and baclofen specifically influences the assoc…

The legal balance between liberty and equality

2021

The paper explores the specific legal balance between liberty and equality, distinguishing it from political theories and constitutional settings, where they are often considered in opposition. In order to find the specific legal balance between liberty and equality, and after identifying some of their relevant meanings for the purpose, it becomes necessary to focus on the rule of law, and to examine the relationship between liberty and equality in its different versions. Once the core meaning of the rule of law in terms of liberty and equality is enucleated, it is possible to consider extending it to the international field.

Improved comparison of bar P and P charge-to-mass ratios

1995

The measured ratio of charge-to-mass ratios for the antiproton and proton is 1.000 000 001 5 ± 0.000 000 001 1. This 1 part in 109 comparison (1 ppb) is possible because a single or p is now directly observed while trapped in an open access Penning trap. The comparison is the most accurate mass spectrometry of particles with opposite charge and is the most sensitive test of CPT invariance for a baryon system. It is 40 times more accurate than our earlier comparison with many trapped antiprotons and protons, and is more than 45 000 times more accurate than earlier comparisons made with other techniques.

Ladri di luce. Leonardo Sciascia e Piero Guccione tra bellezza e verità

2023

The unpublished correspondence between Leonardo Sciascia and Piero Guccione from 1975 to 1989 shows the profound charge of humanity that innervates the friendship between these two great Enlightenment leaders "upside down". A "correspondence of amorous senses", despite the inevitable ideological differences, which the letters reproduced here for the first time and the original contributions of the volume give us back, under the banner of the binomial "beauty-truth".

Synthesis, antiproliferative activity, and mechanism of action of new benzamido derivatives

2011

The cinnamoyl anthranilamides represent a class of biological active substances of great importance in medicinal chemistry. Moreover, despite their wide range of biological activities, a review of the literature revealed that no anticancer activity is described for this kind of substances. Starting from the 2-cinnamamido-5-iodobenzamide, resulted able to inhibit the leukemic cell line K-562 proliferation with a percent of inhibition of 74% at 10M concentration, we undertake the following structural modifications on cinnamamidobenzamide skeleton: the introduction of various substituents both on the benzamido and the cinnamamido moieties, the substitution of olefinic bond with the ethane, et…

Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis

2018

Abstract: Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence, there is a need to identify new molecular scaffolds and targets as potential therapeutics for the treatment of this disease. We report a small series of 1,2‐substituted‐1H‐benzo[d]imidazole derivatives (9ad) showing affinity in the submicromolar range (Ki = 0.150.69 μM) toward Leishmania mexicanaCPB2.8ΔCTE, one of the more promising targets for antileishmanial drug design. The compounds confirmed activity in vitro against intrace…

Effect of Graphene Nanoplatelets on the Physical and Antimicrobial Properties of Biopolymer-Based Nanocomposites

2016

In this work, biopolymer-based nanocomposites with antimicrobial properties were prepared via melt-compounding. In particular, graphene nanoplatelets (GnPs) as fillers and an antibiotic, i.e., ciprofloxacin (CFX), as biocide were incorporated in a commercial biodegradable polymer blend of poly(lactic acid) (PLA) and a copolyester (BioFlex®). The prepared materials were characterized by scanning electron microscopy (SEM), and rheological and mechanical measurements. Moreover, the effect of GnPs on the antimicrobial properties and release kinetics of CFX was evaluated. The results indicated that the incorporation of GnPs increased the stiffness of the biopolymeric matrix and allowed for the t…

GEOCHEMICAL AND MINERALOGICAL FINGERPRINTS OF THE SEDIMENTS SUPPLY AND EARLY DIAGENETIC PROCESSES IN THE BIZERTE LAGOON (TUNISIA)

2016

International audience; The Bizerte Lagoon (Tunisia) functions as a sedimentation environment characterized by receiving allochthonous sediments mainly transported by the Ben Hassine, Rharek and Guenich streams, as well as marine sediments from the Mediterranean Sea. It is subjected to significantenvironmental changes due to the natural and anthropic influences altering the natural patterns of circulation, extraction and/or deposition of mineralogical materials. The aim of this investigation is to analyze the sediments supply and early diagenetic processes in Bizerte Lagoon. Thephyicochemical parameter of the sediment pore water, as well as their texture, mineralogical composition (X-Ray di…