Search results for " INO"
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A Co36Cluster Assembled from the Reaction of Cobalt Pivalate with 2,3-Dicarboxypyrazine
2009
A record Co36 cluster is prepared. This mixed-valent compound containing CoII and CoIII centers is formed in the reaction of a dinuclear cobalt pivalate species with the polydentate 2,3-dicarboxypyrazine ligand. In terms of magnetic properties it behaves as a {Co16-Co16} supramolecular dimer in which the S = A spin ground states of each monomer do not interact. Fil: Alborés, Pablo. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Ciudad Universitaria. Instituto de Química, Física de los Materiales, Medioambiente y Energía. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales. Instituto de Química, Física de los Materiales, M…
Paracentrin 1, a synthetic antimicrobial peptide from the sea-urchin Paracentrotus lividus, interferes with staphylococcal and Pseudomonas aeruginosa…
2014
The rise of antibiotic-resistance as well as the reduction of investments by pharmaceutical companies in the development of new antibiotics have stimulated the investigation for alternative strategies to conventional antibiotics. Many antimicrobial peptides show a high specificity for prokaryotes and a low toxicity for eukaryotic cells and, due to their mode of action the development of resistance is considered unlikely. We recently characterized an antimicrobial peptide that was called Paracentrin 1 from the 5-kDa peptide fraction from the coelomocyte cytosol of the Paracentrotus lividus. In this study, the chemically synthesized Paracentrin 1, was tested for its antimicrobial and antibiof…
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors
2020
[Image: see text] Breast cancer (BC) is the most diffused cancer type in women and the second leading cause of death among the female population. Effective strategies to fight estrogen responsive (ER+) BC, which represents 70% of all BC cases, rely on estrogen deprivation, via the inhibition of the aromatase enzyme, or the modulation of its cognate estrogen receptor. Current clinical therapies significantly increased patient survival time. Nevertheless, the onset of resistance in metastatic BC patients undergoing prolonged treatments is becoming a current clinical challenge, urgently demanding to devise innovative strategies. In this context, here we designed, synthesized, and performed in …
Mesoporous Silica-Based Materials with Bactericidal Properties
2019
[EN] Bacterial infections are the main cause of chronic infections and even mortality. In fact, due to extensive use of antibiotics and, then, emergence of antibiotic resistance, treatment of such infections by conventional antibiotics has become a major concern worldwide. One of the promising strategies to treat infection diseases is the use of nanomaterials. Among them, mesoporous silica materials (MSMs) have attracted burgeoning attention due to high surface area, tunable pore/particle size, and easy surface functionalization. This review discusses how one can exploit capacities of MSMs to design and fabricate multifunctional/controllable drug delivery systems (DDSs) to combat bacterial …
Targeting a Targeted Drug: An Approach Toward Hypoxia-Activatable Tyrosine Kinase Inhibitor Prodrugs
2016
Tyrosine kinase inhibitors (TKIs), which have revolutionized cancer therapy over the past 15 years, are limited in their clinical application due to serious side effects. Therefore, we converted two approved TKIs (sunitinib and erlotinib) into 2-nitroimidazole-based hypoxia-activatable prodrugs. Kinetics studies showed very different stabilities over 24 h; however, fast reductive activation via E. coli nitroreductase could be confirmed for both panels. The anticancer activity and signaling inhibition of the compounds against various human cancer cell lines were evaluated in cell culture. These data, together with molecular docking simulations, revealed distinct differences in the impact of …
Development and biological investigations of hypoxia-sensitive prodrugs of the tyrosine kinase inhibitor crizotinib
2019
Despite the huge success of tyrosine kinase inhibitors as anticancer agents, severe side effects are a major problem. In order to overcome this drawback, the first hypoxia-activatable 2-nitroimidazole-based prodrugs of the clinically approved ALK and c-MET inhibitor crizotinib were developed. The 2-aminopyridine functionality of crizotinib (essential for target kinase binding) was considered as ideal position for prodrug derivatization. Consequently, two different prodrugs were synthesized with the nitroimidazole unit attached to crizotinib either via carbamoylation (A) or alkylation (B) of the 2-aminopyridine moiety. The successful prodrug design could be proven by docking studies and a dr…
Psychological Factors in Childhood Asthma
1994
The influence of the personality of asthmatic children and their mothers on the course of their illness is analysed, taking as a basis a sample of 48 asthmatic children. This is done through the assessment of the role of personality in the change that takes place, after the application of various psychological treatments (relaxation, systematic desensitization and stress inoculation) in three variables: number of days of illness, symptomatic relief drug use and school absences. The results obtained highlight the influence of personality on therapeutic success. Consequently, this study shows the importance of tending to personality traits in order to forecast and improve the effectiveness of…
Cytoskeleton mediates negative inotropism and lusitropism of chromogranin A-derived peptides (human vasostatin1-78 and rat CgA(1-64)) in the rat heart
2010
Cytoskeleton scaffold in cardiac myocytes provides structural support and compartmentalization of intracellular components. It is implicated in cardiac pathologies including hypertrophy and failure, playing a key role in the determinism of contractile and diastolic dysfunctions. Chromogranin A (CgA) and its derived peptides have revealed themselves as novel cardiovascular modulators. In humans, normal CgA levels considerably increase in several pathologies, including heart failure. Recent data have shown on the unstimulated rat heart that human recombinant Vasostatin-1 (hrVS-1) and rat chromogranin A 1-64 (rCgA(1-64)) induce negative inotropic and lusitropic effects counteracting the beta-a…
Pharmacokinetic evaluation of mycophenolate mofetil for pemphigus.
2011
Introduction: Pemphigus is an autoimmune blistering disease of the skin and mucous membranes characterized by the development of autoantibodies against the desmosomal proteins, desmoglein-1 and -3. Before the advent of corticosteroids, therapy was almost fatal. The introduction of high-dose corticosteroid therapy has reduced mortality rates to similar to 10%, but long-term use of steroids can lead to side effects, many of which are severe and associated with significant morbidity. Thus, the major goal of pemphigus therapy has been to reduce the patient's cumulative exposure to systemic corticosteroids. Over the last 2 decades, a range of corticosteroid-sparing immunosuppressive agents have …
Nanocomposites híbridos preparados a partir de soportes silíceos mesoporosos
2015
Esta tesis se ha desarrollado en el marco de la búsqueda de aplicaciones de Materiales Mesoporosos, como son los sólidos de sílice pura: MCM-41, UVM-7 y UVM-11 (xerogel). Estos tres materiales han sido sintetizados mediante el denominado Método de los Atranos. De forma independiente, estos materiales han sido sintetizados, y posteriormente caracterizados, para ser utilizados en tres áreas científicas diferentes, como son: - Como soporte como sistema de almacenamiento y liberación de fármacos (concretamente el Ibuprofeno). - Como soporte de composite de materiales magnéticos (complejo magnético de Niquel). - Como reactivo para la síntesis (junto con moléculas del disacárido sacarosa) de un m…