European ScreeningPort

Hamburg, Germany

European ScreeningPort

Hamburg, Germany

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Prokofjeva M.M.,RAS Engelhardt Institute of Molecular Biology | Riecken K.,University of Hamburg | Spirin P.V.,RAS Engelhardt Institute of Molecular Biology | Yanvarev D.V.,RAS Engelhardt Institute of Molecular Biology | And 6 more authors.
AIDS Research and Therapy | Year: 2013

Background: Despite progress in the development of combined antiretroviral therapies (cART), HIV infection remains a significant challenge for human health. Current problems of cART include multi-drug-resistant virus variants, long-term toxicity and enormous treatment costs. Therefore, the identification of novel effective drugs is urgently needed.Methods: We developed a straightforward screening approach for simultaneously evaluating the sensitivity of multiple HIV gag-pol mutants to antiviral drugs in one assay. Our technique is based on multi-colour lentiviral self-inactivating (SIN) LeGO vector technology.Results: We demonstrated the successful use of this approach for screening compounds against up to four HIV gag-pol variants (wild-type and three mutants) simultaneously. Importantly, the technique was adapted to Biosafety Level 1 conditions by utilising ecotropic pseudotypes. This allowed upscaling to a large-scale screening protocol exploited by pharmaceutical companies in a successful proof-of-concept experiment.Conclusions: The technology developed here facilitates fast screening for anti-HIV activity of individual agents from large compound libraries. Although drugs targeting gag-pol variants were used here, our approach permits screening compounds that target several different, key cellular and viral functions of the HIV life-cycle. The modular principle of the method also allows the easy exchange of various mutations in HIV sequences. In conclusion, the methodology presented here provides a valuable new approach for the identification of novel anti-HIV drugs. © 2013 Prokofjeva et al.; licensee BioMed Central Ltd.


Gul S.,European ScreeningPort
European Pharmaceutical Review | Year: 2014

Recent years have witnessed an expansion in the disciplines encompassing drug discovery outside the pharmaceutical industry. This is most notable with a significant number of universities worldwide now that host infrastructure such as compound libraries and automated screening centres. An archetypal small molecule drug discovery project will aim to identify chemical starting points that modify the functions of genes, cells, or biochemical pathways. In some but not all instances, these functions may be linked to disease processes, and an opportunity will exist to further develop the chemical starting points into novel therapeutic agents. In small molecule drug discovery, the ultimate aim is to identify new therapeutics, an activity that for reasons of high risk and cost has historically been conducted within the commercial sectors.


Gul S.,European ScreeningPort
European Pharmaceutical Review | Year: 2013

The emergence of chemical biology has coincided with increasing numbers of exploratory molecular targets and mechanisms, both therapeutic and non-therapeutic in origin. Screening using miniaturised microtitre plate format based assays remains the most widely utilised methodology for identifying novel chemical matter capable of modulating target function in a meaningful, biologically relevant manner.


Gul S.,European ScreeningPort
European Pharmaceutical Review | Year: 2010

In this article, an overview regarding advances in assay formats for specific target classes and options that should be considered when considering hardware will be given. There has been a significant growth in the assay and automation technologies that are available for compound screening activities and it is essential to evaluate a variety of these before beginning a drug discovery program, the aims of these being to ensure the most relevant assay formats that are available are adopted.

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