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HTS (High Throughput Screening)

 

lab-automation
lab-automation
article

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

15 December 2013 | By 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…

LC-MSMS IVD kits
LC-MSMS IVD kits
article

Pharmaceutical proteomics: a journey from discovery and characterisation of targets to development of high-throughput assays

15 December 2013 | By Joerg Reinders, Institute of Functional Genomics, University of Regensburg

Proteomics has evolved during the last few years from a time-intensive, cost-intensive and hard-to-reproduce technique in basic research to a versatile and reliable tool in various areas of pharmaceutical research. The exploding progress in mass-spectrometry-compatible protein and peptide-separation methods led to the development of new approaches particularly suited for monitoring…

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

Molecular drug targets in autophagy

19 April 2011 | By 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…

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.
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.
article

Establishing assays and small molecule screening facilities for Drug discovery programs

16 February 2011 | By 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…

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

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

16 December 2010 | By 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…

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.
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.
article

Polymorph screening in pharmaceutical development

19 August 2010 | By 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), is of considerable importance when trying to achieve consistent product quality during the manufacture of pharmaceutical solids and solid dosage…

Figure 1 ASSET™ plan and detail Copyright: The Automation Partnership
Figure 1 ASSET™ plan and detail Copyright: The Automation Partnership
article

High content cell based primary screening for oncology targets – a perspective

25 June 2010 | By Peter Alcock, Colin Bath, Carolyn Blackett & Peter B. Simpson, Screening & Assay Sciences, Cancer Bioscience, AstraZeneca Alderley Park

Over the last 15 years, vendors have offered microscope-based instruments capable of producing images of fluorescent labelled components of cells grown in microtitre plates. These instruments are typically bundled with analysis software capable of defining the relative distribution of several fluorescent markers on a cell by cell basis1,2. As the…

Automation in the Pharmaceutical Industry
Automation in the Pharmaceutical Industry
article

Trends in laboratory automation: From speed and simplicity to flexibility and information content

24 June 2010 | By Fernando A. Ramon Olayo, Manager, GlaxoSmithKline

The pharmaceutical industry has significantly influenced laboratory automation trends in the past two decades. The need to screen large collections of chemical entities in a short time with minimised consumption of reagents has driven a strong demand of parallelisation, automation, simplification and miniaturisation solutions from the suppliers of instruments, labware…

article

Launching an HTS campaign to discover new antivirals

23 May 2007 | By Colleen B. Jonsson, Ph.D., Program Leader, Emerging Infectious Disease Research and E. Lucile White, Manager, High-Throughput Screening Center and Enzymology Laboratory, Southern Research Institute, Birmingham, AL, United States

There are over 300 human viruses that have no treatment, vaccine or antiviral. Unfortunately, only sixty-two drugs are approved by the US Food and Drug Administration (FDA) for the treatment of six different viral illnesses. Of these, 45% are for the treatment of HIV/AIDS. The remaining drugs offer treatments that…

article

HTS technologies to facilitate chemical genomics

27 March 2007 | By Douglas S. Auld, James Inglese, Ajit Jadhav and Christopher P. Austin, NIH Chemical Genomics Center, National Institutes of Health, Bethesda, G.Sitta Sittampalam, Chahrzad Montrose-Rafizadeh and James E. Mcgee, Lead Generation & Lead Optimization Biology, Discovery Chemistry Research & Technology and Philip W. Iversen, Global Discovery & Development Statistics, Eli Lilly & Company

Industrial scale technologies developed and applied within the pharmaceutical industry for the purpose of drug discovery have recently been adopted by many research laboratories for the purpose of facilitating chemical genomics. Taking full advantage of these technologies will require education in high-throughput screening assay systems as well as new methods…

article

Pursuing hot targets in drug discovery

28 November 2006 | By Colleen B. Jonsson, Program Leader, Emerging Infectious Diseases Research, Southern Research Institute

Over the past few decades we have experienced a dramatic increase in the rate of emergence and re-emergence of infectious diseases1,2. Many of these diseases, such as SARS, resulted in fewer than 1,000 deaths, but caused an estimated 2 per cent decline gross domestic product in East Asia. The economic…

article

The role of HTS in eADMET profiling

28 September 2006 | By Werner Stuermer, Altana Pharma

Historically (until the late 1980s), compounds discovered by phenotypical in vivo screens were at least characterised with implicit ADMET data. An attractive compound in these test systems was available at the (usually unknown) target; had a minimal toxicological profile (the animal did not die immediately) and gave phenotypical (High-Content) information…

article

Affinity-based screening

20 July 2006 | By Dr Lorenz M. Mayr, Executive Director & Head Biochemical Screening and Dr Hartmut Zehender, Labhead SpeedScreen, Biochemical Screening, Novartis Institute for Biomedical Research

Drug (lead) discovery relies on massive screening of chemical libraries against various extra- and intracellular molecular targets to find compounds with the desired mode of action. Sequencing of the human genome1 has generated a large number (>40 per cent) of new molecular targets with unknown function (‘orphan targets’), as well…