Search results for "Moi"
showing 10 items of 2109 documents
Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives
2018
A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-b-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced 62% HSD1 inhibition at 5 mM and, furthermore, three of them produced 68% inhibition at 1 mM. A docking-based structure-activity relationship analysis was done to determine the molecular basis of the inhibition and the cross-reactivity of the analogues was tested against oestrogen receptor, aromatase, cytochrome P450 1A2, and monoamine oxidases. Most of the analogues are only modestly active with 17-b-hydroxysteroid dehydrogenase 2 – a requirement for lowe…
Effect of Manganese Chloride and of Cotreatment with Cadmium Chloride on the In Vitro Proliferative, Motile, and Invasive Behavior of MDA-MB231 Breas…
2019
We examined the dose&ndash
Fluorouracil and bevacizumab plus anakinra for patients with metastatic colorectal cancer refractory to standard therapies (IRAFU): a single-arm phas…
2018
IF 5.503 (2017); International audience; In preclinical models, IL-1β inhibition could enhance the efficacy of fluorouracil (5-FU). In this phase 2 study, we assessed the activity and safety of 5-FU plus bevacizumab and anakinra (an IL-1β and α inhibitor) in patients with metastatic colorectal (mCRC) refractory to chemotherapy and anti-angiogenic therapy. Eligible patients had unresectable mCRC; were refractory or intolerant to fluoropyrimidine, irinotecan, oxaliplatin, anti-VEGF therapy, and anti-EGFR therapy (for tumors with wild-type KRAS). Patients were treated with a simplified acid folinic plus 5-FU regimen and bevacizumab (5 mg/kg) both administered by intravenous infusion for 30 min…
Antiviral Properties of Chemical Inhibitors of Cellular Anti-Apoptotic Bcl-2 Proteins
2017
Viral diseases remain serious threats to public health because of the shortage of effective means of control. To combat the surge of viral diseases, new treatments are urgently needed. Here we show that small-molecules, which inhibit cellular anti-apoptotic Bcl-2 proteins (Bcl-2i), induced the premature death of cells infected with different RNA or DNA viruses, whereas, at the same concentrations, no toxicity was observed in mock-infected cells. Moreover, these compounds limited viral replication and spread. Surprisingly, Bcl-2i also induced the premature apoptosis of cells transfected with viral RNA or plasmid DNA but not of mock-transfected cells. These results suggest that Bcl-2i sensiti…
Influence of the metaphysis positioning in a new reverse shoulder prosthesis
2016
Aim of this work is to investigate the behaviour of a new reverse shoulder prosthesis, characterized by a humeral metaphysis with a variable offset, designed to increase the range of movements and to reduce the impingement. In particular, by means of virtual prototypes of the prosthesis, different offset values of the humeral metaphysis have been analysed in order to find the best positioning able to maximize the range of movements of the shoulder joint. The abduction force of the deltoid, at different offset values, has been also estimated. The study has been organized as follows. In the first step, the point clouds of the surfaces of the different components of the prosthesis have been ac…
Edible films/coating with tailored properties for active packaging of meat, fish and derived products
2020
Abstract Background Meat, fish and derived products are perishable food items with quick deterioration under improper storage. Edible films and/or coatings present an interesting approach to preserve and package these foods. These are composed of biopolymers generated from food industry wastes or underutilized sources of proteins, lipids, or polysaccharides that are biodegradable, edible and can act as carriers with active agents from natural sources. Scope and approach The protective effect of active films and coatings in meat, fish and derived products against quality decay during storage is described. This review reinforces the benefits of active films and coatings incorporated with natu…
An Interactive Framework for Offline Data-Driven Multiobjective Optimization
2020
We propose a framework for solving offline data-driven multiobjective optimization problems in an interactive manner. No new data becomes available when solving offline problems. We fit surrogate models to the data to enable optimization, which introduces uncertainty. The framework incorporates preference information from a decision maker in two aspects to direct the solution process. Firstly, the decision maker can guide the optimization by providing preferences for objectives. Secondly, the framework features a novel technique for the decision maker to also express preferences related to maximum acceptable uncertainty in the solutions as preferred ranges of uncertainty. In this way, the d…
A New Paradigm in Interactive Evolutionary Multiobjective Optimization
2020
Over the years, scalarization functions have been used to solve multiobjective optimization problems by converting them to one or more single objective optimization problem(s). This study proposes a novel idea of solving multiobjective optimization problems in an interactive manner by using multiple scalarization functions to map vectors in the objective space to a new, so-called preference incorporated space (PIS). In this way, the original problem is converted into a new multiobjective optimization problem with typically fewer objectives in the PIS. This mapping enables a modular incorporation of decision maker’s preferences to convert any evolutionary algorithm to an interactive one, whe…
Intrinsic adhesive and cohesive assessment of the moisture sensitivity of bio-rejuvenated recycled asphalt binders
2019
Alternative binders not derived from fossil fuels, known as biobinders, are opening new paths for multiple applications in road infrastructure. Biobinders, usually produced from bio-oils obtained from the processing of biomass and industry by-products, are tuneable materials whose properties can be adjusted to meet specific targets. For this reason, an interesting approach is to couple biobinders with Reclaimed Asphalt (RA) by taking advantage of their rejuvenating properties to design bio-asphalt mixtures with high-content RA and no additional virgin bitumen. Recent research has proven the feasibility of this approach through validation at full-scale (BioRePavation project). However certai…
Progress Checking for Dummies
2018
Verification of progress properties is both conceptually and technically significantly more difficult than verification of safety and deadlock properties. In this study we focus on the conceptual side. We make a simple modification to a well-known model to demonstrate that it passes progress verification although the resulting model is intuitively badly incorrect. Then we point out that the error can be caught easily by adding a termination branch to the system. We compare the use of termination branches to the established method of addressing the same need, that is, weak fairness. Then we discuss another problem that may cause failure of catching progress errors even with weak fairness. Fi…