Search results for "44"

In Silico Design, Synthesis and Biological Evaluation of Anticancer Arylsulfonamide Endowed with Anti-Telomerase Activity

2022

Telomerase, a reverse transcriptase enzyme involved in DNA synthesis, has a tangible role in tumor progression. Several studies have evidenced telomerase as a promising target for developing cancer therapeutics. The main reason is due to the overexpression of telomerase in cancer cells (85–90%) compared with normal cells where it is almost unexpressed. In this paper, we used a structure-based approach to design potential inhibitors of the telomerase active site. The MYSHAPE (Molecular dYnamics SHared PharmacophorE) approach and docking were used to screen an in-house library of 126 arylsulfonamide derivatives. Promising compounds were synthesized using classical and green methods. Com…

Binding abilities of a chiral calix[4]resorcinarene: a polarimetric investigation on a complex case of study

2017

Polarimetry was used to investigate the binding abilities of a chiral calix[4]resorcinarene derivative, bearing L-proline subunits, towards a set of suitably selected organic guests. The simultaneous formation of 1:1 and 2:1 host–guest inclusion complexes was observed in several cases, depending on both the charge status of the host and the structure of the guest. Thus, the use of the polarimetric method was thoroughly revisited, in order to keep into account the occurrence of multiple equilibria. Our data indicate that the stability of the host–guest complexes is affected by an interplay between Coulomb interactions, π–π interactions, desolvation effects and entropy-unfavorable conformatio…

New insights into the surface functionalities and adsorption evolution of water molecules on silica gel surface: A study by second derivative near in…

2010

Accepted version of an article in the journal: Vibrational Spectroscopy. Published version available on Science Direct: http://dx.doi.org/10.1016/j.vibspec.2010.06.003 Surface functionalities and adsorption evolution of water molecules on silica gel samples were studied by second derivative near infrared spectroscopy. Four different silica gel samples with varying surface area were used in this experiment. Each of the dry samples was allowed to equilibrate with surrounding air and the near infrared spectra were accumulated at different time intervals using reflectance technique. The evolved spectra were analysed using second derivative technique to study the adsorption evolution of water mo…

Sustainable development as a challenge for a society and an economy

2017

During the political process leading up to the Earth Summit in Rio de Janeiro in 1992 it was decided that the concept which will be used to coordinate spontaneous development processes will be the concept of sustainable development. Since that time, efforts are made to implement this concept through inclusion in the legal regulations and by modelling the development objectives of societies. This process should be accompanied by: 1) a reflection over a direction in which we should go and 2) a question whether actions, carried out in the spirit of sustainable development, really bring us closer to the realisation of this concept. The proposed paper will develop these last two questions focusi…

Syntaxe adjectivale et syntaxe verbale. Un cas d'étude en grec ancien

2013

Synthesis and biological evaluation of a novel MUC1 glycopeptide conjugate vaccine candidate comprising a 4’-deoxy-4’-fluoro-Thomsen–Friedenreich epi…

2015

The development of selective anticancer vaccines that provide enhanced protection against tumor recurrence and metastasis has been the subject of intense research in the scientific community. The tumor-associated glycoprotein MUC1 represents a well-established target for cancer immunotherapy and has been used for the construction of various synthetic vaccine candidates. However, many of these vaccine prototypes suffer from an inherent low immunogenicity and are susceptible to rapid in vivo degradation. To overcome these drawbacks, novel fluorinated MUC1 glycopeptide-BSA/TTox conjugate vaccines have been prepared. Immunization of mice with the 4’F-TF-MUC1-TTox conjugate resulted in strong im…

Note sur le mot « Fantastique » (rubrique du Dr. Néophobus)

2020

Le "Scarabée des hiéroglyphes" est la gazette annuelle publiée par l'Association des Amis de Charles Nodier. La présente référence est une notice de vulgarisation linguistique. Il s'agit d'une étude d'étymologie et de sémantique historique sur le mot « Fantastique », en particulier sur l'usage qu'en fait Charles Nodier, théoricien du genre dans "Du fantastique en littérature" et écrivain romantique à l'origine de la veine du conte fantastique français.; International audience; Notice étymologique et de sémantique historique sur le mot « Fantastique », en particulier sur l'usage qu'en fait Charles Nodier, théoricien du genre dans "Du fantastique en littérature" et écrivain romantique à l'ori…

Inefficient Termination of Antigen Responses in NF-ATp-Deficient Mice

1998

In order to elucidate the role of NF-ATp, one of the most prominent members of family of NF-AT transcription factors in peripheral T lymphocytes, in T cell activation and differentiation we created NF-ATp-deficient mice by gene targeting. Such NF-ATp-/- mice are born and appear to develop a normal immune system. Apart from clear-cut defects in the synthesis of mRNAs for Th2-type lymphokines, such as IL-4, IL-5, IL-10 and IL-13, in primary and secondary stimulations of spleen cells in vitro, of a distinct impaired deletion of V beta 11+/CD4+ T lymphocytes from these mice was detected after superantigen injection. Moreover, NF-ATp-/- mice older than 6 weeks show an 2-5 fold increase in number…

Study of the Ti-44(alpha, p)V-47 reaction and implications for core collapse supernovae

2014

The underlying physics triggering core collapse supernovae is not fully understood but observations of material ejected during such events helps to solve this puzzle. In particular, several satellite based γ -ray observations of the isotope 44Ti have been reported recently. Conveniently, the amount of this isotope in stellar ejecta is thought to depend critically on the explosion mechanism. The most influential reaction to the amount of 44Ti in supernovae is 44Ti(α, p)47V. Here we report on a direct study of this reaction conducted at the REX-ISOLDE facility, CERN. The experiment was performed with a 44Ti beam at Elab = 2.16 MeV/u, corresponding to an energy distribution, for reacting α-par…

Strategies to Target ADAM17 in Disease: From Its Discovery to the iRhom Revolution

2021

For decades, disintegrin and metalloproteinase 17 (ADAM17) has been the object of deep investigation. Since its discovery as the tumor necrosis factor convertase, it has been considered a major drug target, especially in the context of inflammatory diseases and cancer. Nevertheless, the development of drugs targeting ADAM17 has been harder than expected. This has generally been due to its multifunctionality, with over 80 different transmembrane proteins other than tumor necrosis factor α (TNF) being released by ADAM17, and its structural similarity to other metalloproteinases. This review provides an overview of the different roles of ADAM17 in disease and the effects of its ablation in a n…