Browse views: by Year, by Function, by GLF, by Subfunction, by Conference, by Journal

Novel Trends in High-Throughput Screening

Mayr, Lorenz and Bojanic, Dejan (2009) Novel Trends in High-Throughput Screening. Current Opinion in Pharmacology, 9 (5). pp. 580-588. ISSN 1471-4892


High-throughput screening (HTS) is a well established process for lead discovery in Pharma and Biotech companies and is now also being used for basic and applied research in academia. .It comprises the screening of large chemical libraries for activity against biological targets via the use of automation, miniaturized assays and large-scale data analysis. Since its first advent in the early to mid 90’s, the field of HTS has seen not only a continuous change in technology and processes, but also an adaptation to various needs in lead discovery. HTS has now evolved into a mature discipline that is a critical source of chemical starting points for drug discovery.
Whereas in previous years much emphasis has been put on a steady increase in screening capacity (“quantitative increase”) via automation and miniaturization, the last years have seen a much greater emphasis on content and quality (“quality increase”). Today, many experts in the field see HTS at a crossroad with the need to decide on either higher throughput/more experimentation, or a greater focus on assays of greater physiological relevance, both of which may lead to higher productivity in pharmaceutical R&D.
In this paper, we describe the development of HTS over the last decade and point out our own ideas for future directions of HTS in biomedical research. We predict that the trend towards further miniaturization will slow down with the balanced implementation of 384-well, 1536-well and 384 low-volume-well plates. Furthermore, we envisage that there will be much more emphasis on rigorous assay and chemical characterization, particularly considering that novel and more difficult target classes will be pursued. In recent years we have witnessed a clear trend in the drug discovery community towards rigid hit validation by the use of orthogonal readout technologies, label-free and biophysical methodologies. We also see a trend towards a more flexible use of the various screening approaches in lead discovery, i.e. the use of both full deck compound screening as well as the use of focused screening and iterative screening approaches. Moreover, we expect greater usage of target identification strategies downstream of phenotypic screening and the more effective implementation of affinity selection technologies as a result of advances in chemical diversity methodologies. We predict that, ultimately, each hit finding strategy will be much more project-related, tailor-made and better integrated into the broader drug discovery efforts.

Item Type: Article
Related URLs:
Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: High-throughput screening; lead finding; hit finding; drug discovery; assay miniaturization; automation; molecular targets; process optimization; orthogonal assays; label-free detection; biophysical methods; focused screening; iterative screening
Related URLs:
Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17


Email Alerts

Register with OAK to receive email alerts for saved searches.