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Drug Discovery

 

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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
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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…

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Automated workflow optimisation and assay development strategies for High Content Research Facility, Trinity College Dublin

23 November 2007 | By

High Content Screening (HCS) is becoming increasingly utilised as an early drug-discovery and basic research tool for defining the functions of genes, proteins and other biomolecules in normal and abnormal cellular functions. HCS involves the integration of a number of preparation steps which include; cell-sample preparation, fluorescent labelling, image acquisition,…

New trends in intelligent robotics in the laboratory
New trends in intelligent robotics in the laboratory
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Protein crystallography in drug design: current bottlenecks

21 September 2007 | By Timothy Allison & Sanjeev Munshi, Department of Structural Biology, Merck, Westpoint, PA

Protein crystallography is an integral component of the structure-guided drug discovery process. Rapid access to structural information about drug targets as well as bound ligands has been pivotal in accelerating lead identification and optimisation processes...

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A new era for microcalorimetry in drug development

21 September 2007 | By Dr Ernesto Freire, Faculty Professor, Johns Hopkins University, Baltimore

Drug development involves the identification and subsequent optimisation of low molecular weight compounds with a desired biological activity. Often, the initial binding affinity of those compounds towards their intended target needs to be improved by five or more orders of magnitude before they become viable drug candidates; a process that…

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How will MicroRNAs affect the drug discovery landscape?

21 July 2007 | By Dr. Neil Clarke and Dr. Mark Edbrooke, GlaxoSmithKline Research and Development, Hertfordshire, UK

The archetypal microRNAs, lin-4 and let-7, were discovered in the nematode worm Caenorhabditis elegans over a decade ago and, at that time, no one would have predicted that they would be anything other than an interesting feature of worm developmental biology. However, in recent years there has been an explosion…

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The impact of automation on drug discovery

21 July 2007 | By William P. Janzen, President and COO, Amphora Discovery

Automated systems and modern pharmaceuticals have both had a hugely positive impact on human life. While these technologies developed in parallel with one another during roughly the same time period in the early 20th century, they didn’t interact until automation found its way into the laboratory in the 1970s.