Search results for " Screening"

Advanced Drug Screening platforms by Inkjet printing

2011

In this work, we show a low-cost, speed, microarray-based drug screening platform that employs inkjet printing drug dispensing on an enzymatic-rich surface. Mixtures of a model substrate (Dglucose)/ inhibitor (D-glucal) couple have been inkjet printed on a target enzymatic monolayer (glucose oxidase) linked to a functionalized silicon oxide solid surface [1]. It has been possible to fabricate microarrays with quality factors as high as those of conventional pin printing spotting. By a simple horseradish-based colorimetric enzymatic assay, the detection of biological activity at the single spot has been proved. The figure shows a scheme of the platform: molecular inks of the enzymatic substr…

Cationic Supramolecular Vesicular Aggregates for Pulmonary Tissue Selective Delivery in Anticancer Therapy

2016

The biopharmaceutical properties of supramolecular vesicular aggregates (SVAs) were characterized with regard to their physicochemical features and compared with cationic liposomes (CLs). Neutral and cationic SVAs were synthesized using two different copolymers of poly(aspartyl hydrazide) by thin-layer evaporation and extrusion techniques. Both copolymers were self-assembled in pre-formulated liposomes and formed neutral and cationic SVAs. Gemcitabine hydrochloride (GEM) was used as an anticancer drug and loaded by a pH gradient remote loading procedure, which significantly increased drug loading inside the SVAs. The resulting average size of the SVAs was 100 nm. The anticancer activity of …

Inkjet printing methodologies for drug screening

2010

We show for the first time a contactless, low-cost, and rapid drug screening methodology by employing inkjet printing for molecular dispensing in a microarray format. Picoliter drops containing a model substrate (D-glucose)/ inhibitor (D-glucal) couple were accurately dispensed on a single layer consisting of the enzymatic target (glucose oxidase) covalently linked to a functionalized silicon oxide support. A simple colorimetric detection method allowed one to prove the screening capability of the microarray with the possibility to assay with high reproducibility at the single spot level. Measurements of the optical signal as a function of concentration and of time verified the occurrence a…

Identification <i>In Silico</i> and <i>In Vitro</i> of Novel Trypanosomicidal Drug-like Compounds

2012

Atom-based bilinear indices and linear discriminant analysis are used to discover novel trypanosomicidal compounds. The obtained linear discriminant analysis-based quantitative structure–activity relationship models, using non-stochastic and stochastic indices, provide accuracies of 89.02% (85.11%) and 89.60% (88.30%) of the chemicals in the training (test) sets, respectively. Later, both models were applied to the virtual screening of 18 in-house synthesized compounds to find new pro-lead antitrypanosomal agents. The in vitro antitrypanosomal activity of this set against epimastigote forms of Trypanosoma cruzi is assayed. Predictions agree with experimental results to a great extent (16/18…

Lung tumorspheres as a drug screening platform against cancer stem cells.

2019

Treatment resistance and metastasis are linked to cancer stem cells (CSCs). This population represents a promising target, but remains unexplored in lung cancer. The main objective of this study was to characterize lung CSCs and discover new therapeutic strategies.

Development of a Multiparametric Cell-based Protocol to Screen and Classify the Hepatotoxicity Potential of Drugs

2012

Hepatotoxicity is a major reason for drug nonapprovals and withdrawals. The multiparametric analysis of xenobiotic toxicity at the single cells level using flow cytometry and cellular imaging-based approaches, such as high-content screening (HCS) technology, could play a key role in the detection of toxicity and the classification of compounds based on patterns of cellular injury. This study aimed to develop and validate a practical, reproducible, in vitro multiparametric cell-based protocol to assess those drugs that are potentially hepatotoxic to humans and to suggest their mechanisms of action. The assay was applied to HepG2 human cell line cultured in 96-well plates and exposed to 78 di…

Intracellular retention of ABL kinase inhibitors determines commitment to apoptosis in CML cells

2012

PLoS one 7(7), e40853 (2012). doi:10.1371/journal.pone.0040853

Deep neural networks leveraging different arrangements of molecular fingerprints to define a novel embedding for virtual screening procedure

2022

A proposal for an evidence-based model of the screening for the colorectal carcinoma in an Italian setting

2011

Introduction. The aim of this paper is to improve the feasibility perception of policymakers, health care workers and target population about the cost-effectiveness of the implementation of colorectal screening as Public Health strategy. Methods. Retrospective study by application of a three-step model designed for a local setting in Sicily (Palermo and its Province) in order to distribute Fecal Occult Blood Tests (FOBTs), offer colonoscopy and surgery, by district allocation of pharmacies, public digestive endoscopic centres and oncologic and general surgery units. Mean adherence to consolidated colorectal screening programs in Italy was applied in order to evaluate the feasibility of an o…

The role of «perceived loss» aversion on credit screening: an experiment

2013

A major characteristic of credit markets is information asymmetry.To combat its problems, as credit rationing, principals can use a menu of contracts to screen clients with different risk level. We conduct a laboratory experiment to address an important question for such settings —does the framing of the offered menu of contracts interfere with the self-selection mechanism? The answer is yes. We find subjects' choices shift when the same (positive) outcomes of the same menu of contracts are presented in two different frames. Subjects exhibit loss aversion in their perception of the positive outcomes below the reference point, and self-selection fails to occur. Uno de los mayores problemas a…