Search results for "complex"
showing 10 items of 5889 documents
Development of peptidomimetic boronates as proteasome inhibitors.
2013
Abstract Proteasome inhibition has emerged over the past decade as an effective therapeutic approach for the treatment of hematologic malignancies. It is a multicatalytic complex, whose proteolytic activity relies in three types of subunits: chymotrypsin-like (β5), trypsin-like (β2) and caspase-like (β1). Most important for the development of effective antitumor agents is the inhibition of the β5 subunits. In this context, the dipeptide boronate bortezomib (Velcade ® ) represents the first proteasome inhibitor approved by the FDA and the lead compound in drug discovery. This paper describes the synthesis and biological evaluation of a series of conformationally constrained pseudopeptide bor…
First bodipy–DOTA derivatives as probes for bimodal imaging
2010
The synthesis and the photophysical studies of the first bodipy-DOTA and its In(III), Ga(III) and Cu(II) complexes are reported. The introduction of an isothiocyanate handle generates a new bimodal imaging agent capable of both optical and nuclear imaging.
Chromo-fluorogenic BODIPY-complexes for selective detection of V-type nerve agent surrogates
2014
Two new Eu3+ and Au3+ BODIPY-complexes capable of chromofluorogenically detecting micromolar concentrations of V-type nerve agent surrogates by a simple displacement assay are described
Near-infrared emitting fluorescent homobimetallic gold(I) complexes displaying promising in vitro and in vivo therapeutic properties
2021
International audience; Boron neutron capture therapy (BNCT) has the potential to specifically destroy tumor cells without damaging the tissues infiltrated by the tumor. BNCT is a binary treatment method based on the combination of two agents that have no effect when applied individually: 10B and thermal neutrons. Exclusively, the combination of both produces an effect, whose extent depends on the amount of 10B in the tumor but also on the organs at risk. It is not yet possible to determine the 10B concentration in a specific tissue using non-invasive methods. At present, it is only possible to measure the 10B concentration in blood and to estimate the boron concentration in tissues based o…
BODIPY-phosphane as a versatile tool for easy access to new metal-based theranostics
2012
A new BODIPY-phosphane was synthesized and proved to be a versatile tool for imaging organometallic complexes. It also led to easy access to a new family of theranostics, featuring gold, ruthenium and osmium complexes. The compounds' cytotoxicity was tested on cancer cells, and their cell uptake was followed by fluorescence microscopy in vitro.
Gold( i )–BODIPY–imidazole bimetallic complexes as new potential anti-inflammatory and anticancer trackable agents
2017
International audience; Two new gold(I)–BODIPY–imidazole based trackable therapeutic bimetallic complexes have been synthesized and fully characterized. They display strong antiproliferative properties on several types of cancers including colon, breast, and prostate and one of them presents a significant anti-inflammatory effect. Additionally, the two compounds could be visualised in vitro by confocal microscopy in the submicromolar range.
Unsteady Separation and Navier-Stokes Solutions at High Reynolds Numbers
2010
We compute the numerical solutions for Navier-Stokes and Prandtl’s equations in the case of a uniform bidimensional flow past an impulsively started disk. The numerical approx- imation is based on a spectral methods imple- mented in a Grid environment. We investigate the relationship between the phenomena of unsteady separation of the flow and the exponential decay of the Fourier spectrum of the solutions. We show that Prandtl’s solution develops a separation singularity in a finite time. Navier-Stokes solutions are computed over a range of Reynolds numbers from 3000 to 50000. We show that the appearance of large gradients of the pressure in the stream- wise direction, reveals that the visc…
Boundary angles, cusps and conformal mappings
1986
Let f be a conformal mapping of a bounded Jordan domain D in the complex plane onto the unit disk . This paper examines the consequences for the local geometry of D near a boundary point z 0 of the mapping f-or, to be more precise, of the homeomorphic extension of this mapping to the closure of D—satisfying a Holder condition at z 0 or, alternatively, of its inverse satisfying a Holder condition at the point f(z 0). In particular, the compatibility of Holder conditions with the presence of cusps in the boundary of D is investigated.
Measuring High-Order Interactions in Rhythmic Processes Through Multivariate Spectral Information Decomposition
2021
Many complex systems in physics, biology and engineering are modeled as dynamical networks and described using multivariate time series analysis. Recent developments have shown that the emergent dynamics of a network system are significantly affected by interactions involving multiple network nodes which cannot be described using pairwise links. While these higher-order interactions can be probed using information-theoretic measures, a rigorous framework to describe them in the frequency domain is still lacking. This work presents an approach for the spectral decomposition of multivariate information measures, capable of identifying higher-order synergistic and redundant interactions betwee…
Effects of cadmium chloride on some mitochondria-related activity and gene expression of human MDA-MB231 breast tumor cells.
2007
It was reported that cadmium is able to exert a cytotoxic effect on tumor MDA-MB231 cells, which shows signs of "non-classical" apoptosis and is characterized by drastic changes in gene expression pattern. In this study, we have extended our knowledge of metal-breast cancer cell interactions by analyzing some mitochondria-related aspects of the stress response to CdCl(2) at either 5 or 50 microM 24- or 96-h exposure, by cytochemical, conventional PCR and Northern/Western blot techniques. We demonstrated that (i) no modification of the mitochondrial mass was detectable due to CdCl(2) exposure; (ii) the respiration activity appeared to be increased after 96-h exposures, while the production o…