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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…

Bottlenecks and potential improvements

28 September 2006 | By Carlo E.A. Jochems and Stefan Herzig, Department of Pharmacology, Faculty of Medicine, University of Köln

Ion channels are membrane proteins that regulate the entrance and departure of specific ions from cells, thus influencing the physiology of all cells. These ion flows also underlie electrical impulses required for sensory and motor functions of the brain, control of contraction of heart, skeletal, smooth and vascular muscle, as…

Wyeth forges ahead

28 September 2006 | By Graham Cook Ph.D., Director Technology and External Supply, EMEA, Wyeth

Is the pharmaceutical manufacturing environment of today becoming more challenging? There is increasing pressure to control or reduce costs because of the limitations on healthcare budgets. Asset utilisation, operating efficiencies and cycle times in the pharmaceutical industry generally compare unfavourably with other high technology industries. Despite the resources invested in…

Streamlining with automation and robotics

28 September 2006 | By Bart Hazes, Dept. of Medical Microbiology & Immunology, University of Alberta and Bernhard Rupp, q.e.d. life science discoveries, inc.

Protein crystallography has been embraced by the pharmaceutical industry to accelerate and rationalise the drug development process. In this role, success rates, throughput and turnaround times have become key competitive factors, and nearly every stage in the protein crystallography process has been targeted for automation using robotics and advanced software.…

Cell-based imaging

28 September 2006 | By Jinghai J. Xu, Ph.D., Margaret C. Dunn, Arthur R. Smith, Pfizer Global Research and Development

Traditionally, in vivo histopathological findings have been used as part of standard readouts for safety assessment of new chemical entities (NCEs). The process typically involves dosing animals with NCEs for varying amounts of time, harvesting their major organs at the end of the study, preparing tissue sections and slides and…

The right technology, at the right time

28 September 2006 | By EPR

The growing popularity of Electronic Data Capture (EDC) is indicative of a broad recognition that EDC as a method of data capture offers significant realisable benefits. Developers of drugs that use EDC within their clinical research processes will have a significant competitive advantage, bringing new drugs and therapies to market…

The current market and future trends for RMM

28 September 2006 | By Tony Cundell, Director, Pharmaceutical Sciences – Microbiology, Schering Plough Research Institute

Following on from our latest report in Issue 4 in which we outlined independent views on ‘solutions for the next stage’ in Rapid Microbiological Methods (RMM) from some of the industry’s leading names, Tony Cundell follows up with his own thoughts on this exciting field.

Essential techniques for development

28 September 2006 | By Dr Danielle Giron, President, Swiss Society for Thermal Analysis & Calorimetry

Thermal analysis methods and coupled techniques are well established procedures in material science. Due to the different information delivered, thermal analysis methods are concurrent or complementary to other analytical techniques such as spectroscopy, chromatography, melting point determination, loss on drying, assay, for identification, purity and quantitation. They are basic methods…

Quantitative PCR assays in clinical drug development

28 September 2006 | By Michael E. Burczynski, Ph.D. and Ole E. Vesterqvist, Ph.D. Biomarker Laboratory, Clinical Translational Medicine, Wyeth Research

Biomarkers (biological markers) have become an integral part of both drug discovery and drug development and play an important role in the transition of potential new drugs from discovery into clinical drug development. In the past, most biomarkers were proteins/peptides and metabolites measured by technologies such as immunoassays, enzymatic assays,…

MitoCheck: checking mitosis

20 July 2006 | By Dr Yan Sun, MitoCheck Project Manager, Institute of Molecular Pathology

MitoCheck is a multi-national, multi-disciplinary research project on cell cycle control. It is funded by the European Union within its 6th framework program (FP6). Leading scientists from 11 research institutes, universities and industry in Austria, Germany, UK, Italy and France with a wide range of expertise in molecular and cell…

Novel antisense drugs for micro-RNA therapeutics

20 July 2006 | By Sakari Kauppinen, Joacim Elmen and Phil Kearney, Santaris Pharma

MicroRNAs (miRNAs) are an abundant class of short endogenous RNAs that act as important post-transcriptional regulators of gene expression.

A showcase project for EU research

20 July 2006 | By Dr Anne Katrin Werenskiold, Project Manager, Interaction Proteome

The investigation of functional protein-protein interactions has been gaining momentum with recent technological innovations. The high-throughput era in genomics and proteomics research is essentially dependent on technological advancements to drastically increase capacities in both large-scale gathering of data; their interpretation and functional validation, as well as the compilation and storage…

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…

Identifying human toxicity potential

20 July 2006 | By Dolores Diaz, CEREP and Peter J. O’Brien, Safety Sciences Europe, Pfizer Global R&D

The statins (3-hydroxy-3-methylglutaryl coenzyme A [HMG-CoA] reductase inhibitors) are drugs that inhibit cholesterol biosynthesis by blocking the formation of the cholesterol precursor mevalonate. Statins are the most effective cholesterol-lowering agents available and are considered the first line of treatment for most patients with high serum cholesterol levels1.

Four years and counting for automation

20 July 2006 | By Claire Townsend, Ph.D., Investigator, GlaxoSmithKline

As a classically trained electrophysiologist, I shall always remember my first encounter with automated patch clamp at Essen Instruments in June 2002. Essen Instruments had just developed the IonWorks HT, an instrument that can record currents from 48 cells simultaneously and perform up to 384 recordings with a drug addition…