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HTS (High Throughput Screening) - Articles and news items

Empower your research with Tecan’s Spark® 20M multimode reader

Empower your research with Tecan’s Spark® 20M multimode reader

Supplier news / 25 January 2016 / Tecan

Tecan has launched the Spark® 20M multimode microplate reader, offering tailor-made solutions to suit virtually any drug discovery or advanced life science research application…

MALDI High-Throughput Screening beyond 100,000 Samples per Day in Drug Discovery

Poster note: MALDI high-throughput screening beyond 100,000 samples per day in drug discovery

Whitepapers / 17 November 2015 / Bruker and Novartis

This work focuses on the improvement of MALDI-TOF automation parameters to further increase sample analysis speed in HTS assays to more than 100,000 samples per day…

Bruker app note September 2015

Application note: High-throughput Screening of Deubiquitylase enzyme (DUB) activity/specificity and inhibitor screening by MALDI-TOF mass spectrometry

Whitepapers / 1 September 2015 / Bruker Daltonik

In biopharmaceutical laboratories, there is a growing need for high-throughput, yet sensitive methodologies to characterize deubiquitylase enzymes (DUBs) and DUB inhibitors…


SLAS2015 : Promises Information, Innovation and Connections

Issue 6 2014 / 23 December 2014 / The Society for Laboratory Automation & Screening (SLAS)

The Society for Laboratory Automation and Screening (SLAS) is proud to present SLAS2015, the Fourth Annual Conference and Exhibition of the Society…

Pharmaceutical Salts

Pharmaceutical salts of small molecule drugs: opportunities and challenges

Issue 5 2014, Screening / 28 October 2014 / Axel Becker, Scientist, Merck KGaA

Over the past decades, pharmaceutical drug development has undergone some significant changes, a prominent example for this being the emergence of biomolecular drugs (New Biological Entities, NBEs) such as antibodies and peptides. However, classical small molecule drugs (New Chemical Entities, NCEs) are far from being a dying species, and in fact the number of NCE drugs approved by the US Food and Drug Administration (FDA) in the past few years has been higher with increasing trend compared to NBE drugs, which appear to stagnate at lower level in terms of new drug approvals…

EPR Screening Supplement 2013 - 100

Screening: In-depth focus 2013

Issue 6 2013, Screening, Supplements / 16 December 2013 / Roger Clark, Paul Harper and Mark Wigglesworth (AstraZeneca Global High Throughput Centre), Rob Jepras and Steve Ludbrook (GlaxoSmithKline)

Technological and sociological advances in HTS: evolution and revolution?
Flow cytometry as a drug screening platform
Show Preview: High-Content Analysis 2014

Sergio Chai

Laboratory Automation: Liquid handling devices in drug discovery: when, what, why?

Drug Discovery, Issue 6 2013 / 15 December 2013 / Sergio C. Chai, Asli N. Goktug and Taosheng Chen, High Throughput Screening Center, Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital

Liquid handlers are ubiquitous and essential tools in every aspect of the drug discovery arena. Innovations in the past few decades resulted in a sizeable array of devices. With so many choices, it is important to identify appropriate instrumentation for a particular screening strategy, which should be based on unique capabilities and limitations. Intense advances in the design of liquid handling devices have broadened the capabilities to screen larger collections of compounds at a faster pace with increased reliability and efficiency. These innovations drift towards miniaturisation, in large part to reduce cost and increase throughput. A wide selection of fluid handlers has been developed for every aspect of drug discovery, which incorporate different technologies for discrete functions. Although this segment focuses on instrumentation relevant to the screening of small organic molecules, the perspectives presented herein can be valuable in the handling of oligonucleotides or biologics…

Figure 1The autophagy pathway. Autophagy proceeds in three steps: initiation by protein kinase complexes

Molecular drug targets in autophagy

Issue 2 2011, Screening / 19 April 2011 / Robin Ketteler, MRC LMCB, University College London

Autophagy is a cellular stress response to diverse stimuli such as starvation, infection and DNA damage. Autophagy plays important roles in the progression of various diseases including cancer, neurodegenerative diseases and Crohn’s disease. Despite recent advances in our understanding of the autophagy machinery, surprisingly little effort has been undertaken towards utilising this knowledge in drug discovery processes. Several phenotypic screens have been undertaken to identify drug candidates that modulate this process. Current highthroughput screening approaches assay the formation of the autophagosome and very little effort is made towards the identification of compounds that inhibit specific autophagy components. Here, I give an overview about potential molecular drug targets in the autophagy pathway and review the current status of targeted drug discovery towards identifying autophagy gene-specific drugs.

Figure 1 Typical critical path for small molecule Drug Discovery programs. Drug Discovery involves identification of a Target of interest for which an assay is developed. This assay is then adapted for screening purposes and utilised in a High Throughput Screening campaign against small molecule libraries. The High Throughput Screening campaign will usually yield many Hit molecules. Confirmation, Counter and Selectivity Screening will provide a final list of Validated Hits.

Establishing assays and small molecule screening facilities for Drug discovery programs

Issue 1 2011, Screening / 16 February 2011 / Sheraz Gul, Vice President & Head of Biology, European ScreeningPort GmbH

Although many of the marketed small molecule drugs have been discovered by research and development efforts within the pharmaceutical industry, there has been a paradigm shift with external sources increasingly being relied upon to fill their pipelines. This trend is likely to increase and the key pre-clinical activities carried out by organisations outside the pharmaceutical industry include target validation, assay development and their use in High Throughput Screening campaigns, validation of the Hit molecules, Hit-to-Lead and Lead-to-Candidate screening/chemistry. In order to perform these activities, adequate know-how and technical expertise is essential so that the processes meet appropriate industry standards. This article discusses some of the challenges associated with assay development and the automation of High Throughput Screening.

Figure 1 Schematic illustration of the recombinant antibody microarray set-up

Developing and applying recombinant antibody microarrays for high-throughput disease proteomics

Issue 6 2010, Screening / 16 December 2010 / Carl A.K. Borrebaeck and Christer Wingren, Department of Immunotechnology and CREATE Health, Lund University

Deciphering crude proteomes in the quest for candidate biomarker signatures for disease diagnostics, prognostics and classifications has proven to be challenging using conventional proteomic technologies. In this context, affinity protein microarrays, and in particular recombinant antibody microarrays, have recently been established as a promising approach within high-throughput (disease) proteomics1-3. The technology will provide miniaturised set-ups capable of profiling numerous protein analytes in a sensitive, selective and multiplexed manner.

Figure 1 Packing diagrams showing the different molecular arrangements in polymorphs A (left) and B (right) of the antipsychotic drug risperidone (centre). Unit cell parameters for each polymorph are shown.

Polymorph screening in pharmaceutical development

Issue 4 2010, Screening / 19 August 2010 / Professor Alastair J. Florence, Solid-State Research Group, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde

The majority of active pharmaceutical ingredients (APIs) are produced by crystallisation and so the phenomenon of polymorphism, whereby an organic molecule can adopt more than one crystalline form (Figure 1 opposite), is of considerable importance when trying to achieve consistent product quality during the manufacture of pharmaceutical solids and solid dosage forms. Although morphology and particle size-distribution are important solid-state characteristics, the uncontrolled occurrence of multiple physical forms (polymorphs, solvates, salts, co-crystals or amorphous) of an API can have significant effects on the performance of the material during processing, manufacture, storage and administration. For example, the solubility difference between some polymorphs has been shown to be over four times that of the least soluble form1 and can vary by significantly more for amorphous forms2.

Pharma ‘HTS’ the Mark with Screening

Industry news, News / 21 July 2010 / NG Online News

Back in May, it was announced that new stem cell research would reduce the need for animal testing…


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