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Drug Discovery

 

FIGURE 1 Schematic overview of a typical homology modelling procedure that is used to build threedimensional coordinates for a protein of unknown structure
FIGURE 1 Schematic overview of a typical homology modelling procedure that is used to build threedimensional coordinates for a protein of unknown structure
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Status and challenges in structure-based drug discovery for G protein-coupled receptors

13 December 2011 | By Henri Xhaard, Head of Computational Drug Discovery Group, Centre for Drug Research, University of Helsinki

The central location of G protein-coupled receptors (GPCRs) at the interface between the interior and exterior of cells, as well as their key role in signalling events, make GPCRs a prominent class of pharmaceutical targets. To date, approximately 40 per cent of known drugs are thought to act on GPCRs…

Drug discovery assays for the histone deacetylase class of enzymes
Drug discovery assays for the histone deacetylase class of enzymes
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Implementing electronic laboratory notebooks to improve the efficiency of pre-clinical drug discovery

13 December 2011 | By Sheraz Gul, Vice President and Head of Biology, European ScreeningPort GmbH

The pre-clinical phase of drug discovery spans a period in the region of five years and requires contributions from multi-disciplinary teams often working at different sites. These teams can generate significant amounts of data which are processed using standard as well as specialist software. The recording of a substantial amount…

FIGURE 1 The rapid evolution of sequencing technologies. A. First generation Sanger sequencing technology. B. Second ‘Next’ generation massively parallel sequencing technology (454 Sequencing © Roche Diagnostics) C. Third ‘Next-Next’ generation single molecule, real-time sequencing technology. In the coming years, second or third generation technologies may develop to an extent where a human genome can be sequenced for a USD 1,000 in a matter of hours
FIGURE 1 The rapid evolution of sequencing technologies. A. First generation Sanger sequencing technology. B. Second ‘Next’ generation massively parallel sequencing technology (454 Sequencing © Roche Diagnostics) C. Third ‘Next-Next’ generation single molecule, real-time sequencing technology. In the coming years, second or third generation technologies may develop to an extent where a human genome can be sequenced for a USD 1,000 in a matter of hours
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DNA sequencing technologies and emerging applications in drug discovery

13 December 2011 | By Nalini A.L. Mehta & David J. Dow, Molecular and Cellular Technologies, Platform Technology and Science, GlaxoSmithKline and Anthony M. Battram, Molecular and Cellular Technologies, Platform Technology and Science, GlaxoSmithKline & Department of Life Sciences, Imperial College London

In recent years, the development of Next Generation DNA Sequencing (NGS) technology has significantly impacted molecular biology research, resulting in many new insights and discoveries. NGS technology goes beyond traditional DNA sequencing with applications that reach across the central dogma of molecular biology from DNA to RNA and protein science.…

FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
FIGURE 1 Schematic overview of the MALDI-MSI process as applied to imaging compound and metabolite distributions in a whole body rat sample. From one section of an animal dosed with the unlabelled compound, the substance and metabolite distributions can be acquired
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MALDI-mass spectrometry imaging applied to drug discovery and development

19 October 2011 | By Brendan Prideaux, Dieter Staab, Gregory Morandi, Nicole Ehrhard and Markus Stoeckli, Novartis Institutes for BioMedical Research

Since its introduction in the field of biomedical imaging over 10 years ago1, matrixassisted laser desorption/ionisation mass spectrometry imaging (MALDI-MSI) has played an ever increasing role in drug discovery and development and is now utilised in laboratories of many leading pharmaceutical companies and collaborating academic institutions.

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Emergence and identification of new designer drug products from the internet

31 August 2011 | By S. Assi, S. Fergus, J.L. Stair, O. Corazza and F. Schifano, University of Hertfordshire

Designer drugs represent a rapidly expanding phenomenon particularly facilitated by their internet availability. These drugs are continuously emerging as analogues of controlled substances (amfetamine, aminoindane, cathinone, phencyclidine, etc) and once an analogue has been banned, another replacement analogue appears on the market. They are often made in unlicensed laboratories which…

Figure 1 Free energy diagram for a single step binding interaction between protein (P) and ligand (L). For a binding reaction of this type increasing affinity is achieved by lowering the free energy of the PL complex. Increasing residence (decreasing koff) time is achieved by lowering the free energy of the PL complex and/or destabilizing the transition state
Figure 1 Free energy diagram for a single step binding interaction between protein (P) and ligand (L). For a binding reaction of this type increasing affinity is achieved by lowering the free energy of the PL complex. Increasing residence (decreasing koff) time is achieved by lowering the free energy of the PL complex and/or destabilizing the transition state
article

Thermodynamics and kinetics driving quality in drug discovery

31 August 2011 | By Geoff Holdgate, AstraZeneca

Recently, there has been renewed interest in using thermodynamic and kinetic data, alongside empirical rules (particularly focused upon cLogP and molecular weight) and guiding metrics such as ligand efficiency and lipophilic ligand efficiency developed for fragments, leads and drugs in order to facilitate the design of compounds with a greater…

Figure 1 High Content Imaging Technology. The leading fluorescent high content imaging platforms established within the pharmaceutical and biotechnology industry. Represented are; A. Fully automated high throughput high content imaging systems (ImageXpress, InCell, BD Pathway, ScanR, Opera and the Arrayscan). B. Live cell kinetic imaging systems (IncuCyteFLR and Cell-IQ) and C. Fluorescent tissue slide imaging platform (Scanscope FL)
Figure 1 High Content Imaging Technology. The leading fluorescent high content imaging platforms established within the pharmaceutical and biotechnology industry. Represented are; A. Fully automated high throughput high content imaging systems (ImageXpress, InCell, BD Pathway, ScanR, Opera and the Arrayscan). B. Live cell kinetic imaging systems (IncuCyteFLR and Cell-IQ) and C. Fluorescent tissue slide imaging platform (Scanscope FL)
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Advancing high content analysis towards improving clinical efficacy

16 February 2011 | By Neil Carragher, Edinburgh Cancer Research UK Centre, Institute of Genetics and Molecular Medicine, University of Edinburgh

High-content analysis is primed to play a prominent role in a new era of drug discovery research that places greater emphasis on clinical translation at all stages of the discovery process from target identification to proof-of-concept testing. High content analysis provides a technical bridge between reductionist targetdirected drug discovery approaches…

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.
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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 Cardiac safety schematic integrating indirect ion channel modulation analysis
Figure 1 Cardiac safety schematic integrating indirect ion channel modulation analysis
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Indirect modulation of cardiac ion channels and implications for preclinical safety assessment

19 August 2010 | By Gül Erdemli & Dmitri Mikhailov, Center for Proteomic Chemistry, Novartis Institutes for BioMedical Sciences and Albert M Kim, Translational Medicine, Novartis Institutes for BioMedical Sciences

The preclinical assessment of a small molecule’s liability for QT interval prolongation is an essential part of the drug discovery process. Patch clamp assays for heterologously expressed recombinant cardiac ion channels are widely used in the pharmaceutical industry to evaluate potential drug-channel interactions. These assays are generally acute assessments and…

Figure 1 Overview of DILI-sim A. Schematic overview of the key biological processes represented in DILI-sim B. Overview of different modules within DILI-sim. Each module is itself a model that captures a specific area of relevant biology, pharmacology and metabolism. This modular approach to DILI-sim allows the overall model to be built in manageable, testable pieces C. Knowledge management aspects of DILI-sim. Under each of the models, the supporting evidence is explicitly captured and hence the model acts as a highly structured knowledge repository
Figure 1 Overview of DILI-sim A. Schematic overview of the key biological processes represented in DILI-sim B. Overview of different modules within DILI-sim. Each module is itself a model that captures a specific area of relevant biology, pharmacology and metabolism. This modular approach to DILI-sim allows the overall model to be built in manageable, testable pieces C. Knowledge management aspects of DILI-sim. Under each of the models, the supporting evidence is explicitly captured and hence the model acts as a highly structured knowledge repository
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Applying systems biology and computer simulations to predicting idiosyncratic DILI

19 August 2010 | By David Cook, Associate Director, Global Safety Assessment, AstraZeneca

Idiosyncratic drug-induced liver injury (DILI) is a rare adverse drug reaction which accounts for a significant amount of patient suffering, including death. Currently, idiosyncratic DILI is unpredictable and as a result arises late in the drug development process or even post-marketing. The prediction of idiosyncratic DILI based on preclinical or…

Sheraz Gul, Head of Assay Development & Screening at the Fraunhofer Institute for Molecular Biology and Applied Ecology.
Sheraz Gul, Head of Assay Development & Screening at the Fraunhofer Institute for Molecular Biology and Applied Ecology.
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Applying automation in early drug discovery: lessons learnt and future perspectives

29 September 2008 | By

An issue that the drug discovery industry has faced over the past several years has been that whilst the number of targets in their portfolios has increased and the level of investment across all Research & Development functions has risen, the likelihood of discovering suitable chemical starting points for medicinal…

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Europe’s premier event for Drug Discovery

29 September 2008 | By

This year's Leading European Event for Drug Discovery – MipTec 2008 – moves from spring to autumn and will be held on the 14-16 October 2008 at the Congress Centre Basel, Switzerland.

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High throughput materials discovery “reducing product time to market”

23 January 2008 | By Dr. Neil Campbell, Senior Experimental Officer, Automation and Process Development Specialist, Centre for Materials Discovery, University of Liverpool

With ever mounting market pressure on industries, from increasing global competition, along with consumer desire for value for money and improved performance results there is a greater driving force to stay one step ahead by reducing product time to market. This enforced impetus has many companies having to continually improve…

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Driving lab automation forward

23 November 2007 | By

A round table discussion covering the driving forces behind the integration of automated technology within the pharmaceutical industry, the procedures that are followed when implementing new automated techniques, current areas of drug discovery most benefiting from lab automation, how lab automation advanced the drug discovery marketplace over the last five…