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Drug Discovery

 

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Imaging for decision-making in drug discovery and early development

23 December 2014 | By Paul McCracken & Stephen Krause

The cost of drug discovery and development, depending upon the size of a given company, has been estimated upwards of $5 billion. Hay et al. recently published a review of clinical development success rates showing only a 10.4% likelihood of regulatory approval of all drugs entering Phase I, 64.5% of…

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A history of recombinant protein technology in small molecule drug discovery

28 October 2014 | By Rick Davies, Associate Director, AstraZeneca / Ian Hardern, Senior Research Scientist, AstraZeneca / Ross Overman, Associate Principal Scientist, AstraZeneca

Recombinant protein production is a prerequisite and essential component of most modern small molecule drug discovery programs. Target proteins are required to underpin screening, structural and mechanistic studies providing data that drives chemical design. From the initial establishment of recombinant protein production in the pharmaceutical industry in the 1980s, systems…

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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…

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Proteases: How naturally occurring inhibitors can facilitate small molecule drug discovery for cysteine proteases

20 August 2013 | By Sheraz Gul, Vice President and Head of Biology, European ScreeningPort GmbH

Cysteine proteases are expressed ubiquitously in the animal and plant kingdom and are thought to play key roles in maintaining homeostasis. The aberrant function of cysteine proteases in humans are known to lead to a variety of epidermal disease states such as inflammatory skin disease1. In marked contrast, the serine…

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Raman spectroscopy: an enabling tool for accelerating pharmaceutical discovery to development

20 August 2013 | By Chanda R. Yonzon, Atul Karande, Sai P. Chamarthy and Brent A. Donovan (Merck & Co. Inc)

Raman spectroscopy has emerged as the preeminent analytical tool for a number of applications within drug discovery and development. Advances in the instrumentation, sensor fabrication and data analysis have enabled the wider acceptance of Raman spectroscopy1,2. In discovery, Raman spectroscopy is used to elucidate structural activity relationships3 and to optimise…

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GPCRs: Cell based label-free assays in GPCR drug discovery

20 August 2013 | By Niklas Larsson, Linda Sundström, Erik Ryberg and Lovisa Frostne (AstraZeneca)

G protein-coupled receptors are one of the major classes of therapeutic targets for a broad range of diseases. The most commonly used assays in GPCR drug discovery measure production of second messengers such as cAMP or IP3 that are the result of activation of individual signalling pathways. Such specific assays…

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Gene to drugs: can expression be the key to new discoveries?

25 February 2013 | By Esther P. Black, College of Pharmacy and Markey Cancer Center, University of Kentucky

Cancer treatment faces a conundrum: a growing lack of therapeutics with lasting effects. The low hanging fruit of the medicinal chemistry orchard seems to have been picked, and modification of existing anti-cancer therapeutics has produced only incremental rewards[1]. Thus, both pharmaceutical companies and academic researchers are left searching for new…

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Future trends in drug discovery technology

18 December 2012 | By Terry McCann, TJM Consultancy

The average cost to a major pharmaceutical company of developing a new drug is over USD 6 billion1. Herper1 observes that the pharmaceutical industry is gripped by rising failure rates and costs, and suggests that the cost of new drugs will be reduced by new technologies and deeper understanding of…

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A new vision of drug discovery and development

18 December 2012 | By D. Lansing Taylor, Director, University of Pittsburgh Drug Discovery Institute and Allegheny Foundation Professor of Computational and Systems Biology, University of Pittsburgh School of Medicine

The pharmaceutical industry has experienced a decade of turbulence driven by the ‘patent cliff’ as major revenue generators are lost to generic status, coupled to the absence of a sustainable pipeline of drug candidates in development that have a good chance of being approved and launched. It is generally agreed…

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What is label-free screening and why use it in drug discovery?

18 December 2012 | By Matthew A. Cooper and Reena Halai, Institute for Molecular Bioscience, the University of Queensland

In the journey of a molecule from its origins in a compound library to candidate drug status, a large variety of profiling must occur to define activity, selectivity, potency, adverse effects, pharmacology and in vivo efficacy. Advances in biophysical methods that can analyse drug interactions with a molecular target, a…

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Drug discovery assays for the histone deacetylase class of enzymes

18 December 2012 | By Sheraz Gul and Gesa Witt, European ScreeningPort GmbH

The histone deacetylase (HDAC) class of enzyme are a group of conserved enzymes known for their ability to remove acetyl groups from lysine residues on histone tails. Since aberrant HDAC enzyme expression is observed in various diseases, there is increasing interest in finding small molecules which function as HDAC enzyme…