Search results for " Screening"

Histologie in vivo avec endomicroscopie confocale dans le diagnostic des cancers colorectaux

2005

L’endomicroscopie confocale constitue un nouvel outil diagnostique destine au diagnostic in vivo des modifications epitheliales constatees en cours de coloscopie. Apres l’application d’agents fluorescents, la technique permet d’obtenir en temps reel, une imagerie de la surface muqueuse et de la couche sous-muqueuse sous microscopie a haute resolution.

CHA on CDK2: a way to identify the best pharmacophore model for the virtual screening of new inhibitors

2018

Cyclin-dependent kinase-2 (CDK2) is a member of serine/threonine protein kinases family. It plays an important role in the regulation events of the eukaryotic cell division cycle, especially during the G1 to S phase transition. Experimental evidences indicate that excessive expression of CDK2 should cause abnormal cell cycle regulation. Therefore, CDK2 has been considered a potential therapeutic target for cancer therapy. In this work, we used a modelling approach that incorporates flexibility based on extensive MD simulations of protein−ligand complexes into structure-based pharmacophore modeling and virtual screening to identify new CDK2 inhibitors. One-hundred and forty-nine CDK2-inhibit…

Retracted Article: Differential detection and quantification of cyclic AMP and other adenosine phosphates in live cells

2017

A new naphthol-based rhodamine derivative (NpRD) has been developed for the selective and differential detection of adenosine 3′,5′-cyclic monophosphate (cAMP) and adenosine phosphates (APs) (ATP, ADP, and AMP) from other nucleotides. The simple detection and quantification of cAMP in human blood cells and in other samples based on the ‘turn on’ fluorescence properties of this chemosensor through colorimetry or fluorometry makes it unique for probable application in high throughput screening.

Design, Synthesis, and Evaluation of New Tripeptides as COX-2 Inhibitors

2013

Cyclooxygenase (COX) is a key enzyme in the biosynthetic pathway leading to the formation of prostaglandins, which are mediators of inflammation. It exists mainly in two isoforms COX-1 and COX-2. The conventional nonsteroidal anti-inflammatory drugs (NSAIDs) have gastrointestinal side effects because they inhibit both isoforms. Recent data demonstrate that the overexpression of these enzymes, and in particular of cyclooxygenases-2, promotes multiple events involved in tumorigenesis; in addition, numerous studies show that the inhibition of cyclooxygenases-2 can delay or prevent certain forms of cancer. Agents that inhibit COX-2 while sparing COX-1 represent a new attractive therapeutic deve…

Application of Molecular Topology to the Prediction of the Reaction Yield and Anticancer Activity of Imidazole and Guanidine Derivatives

2013

In this study molecular topology based QSAR has been applied to predict the reaction yield and anticancer activity of 18 imidazole and guanidine derivatives. Four properties were evaluated, namely reaction yield, anti prostatic-cancer activity, anti breast-cancer activity and anti lung-cancer activity. The four models have been validated by both internal and cross validation, and also by randomness tests. The results obtained are in full agreement with the experimental results and confirm the precision, accuracy and robustness of the method followed. After carrying out a virtual screening upon such models, new imidazole and guanidine derivatives with potential anticancer activity are propos…

Compliance with the clinical practice guidelines for the management of hepatitis B and C virus-related chronic liver disease: a survey based on hospi…

2013

Current development of CFTR potentiators in the last decade

2020

Cystic fibrosis (CF) is a genetic disorder produced by the loss of function of CFTR, a main chloride channel involved in transepithelial salt and water transport. CFTR function can be rescued by small molecules called "potentiators" which increase gating activity of CFTR on epithelial surfaces. High throughput screening (HTS) assays allowed the identification of new chemical entities endowed with potentiator properties, further improved through medicinal chemistry optimization. In this review, the most relevant classes of CFTR potentiators developed in the last decade were explored, focusing on structure-activity relationships (SAR) of the different chemical entities, as a useful tool for t…

Coronary artery disease screening

2008

Cancer colorectal : du diagnostic au dépistage

2009

Colorectal cancer fulfils the conditions required for mass screening. Data from controlled studies indicate that it is possible to reduce colorectal cancer mortality at a population level using faecal occult blood testing. Screenings rely on biennial testing in between 50 and 74average risk subjects. Compliance must be over 50%. Colorectal cancer mortality decrease in this case between 15 and 18% in the general population, 33 and 39% among participants to screening. The European Commission, on the basis of available data recommended to organise colorectal cancer screening in the European Union. Generalisation of screening has become a reality in France. Epidemiological studies allow us to d…

Universal method to determine acidic licit and illicit drugs and personal care products in water by liquid chromatography quadrupole time-of-flight

2016

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