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  • MRC Technology and EMBLEM Collaborate to Streamline Drug Development
    Initiative strengthens drug development and commercialization network
  • Medical Research Council Technology and MS Society Launch Joint ‘Call for Targets’
    MRC Technology, a technology transfer organisation with its own drug discovery laboratories, and the MS Society, a charity providing support and research funding for people affected by MS, today announced a joint ‘call for targets’ in order to fast-track the discovery and development of novel drugs to slow, stop or reverse progression in MS or treat MS symptoms. The call to academic researchers seeks to fund further validation of small molecule and antibody targets prior to initiating a full scale drug discovery project to produce ‘drug-like’ molecules or therapeutic antibodies that have the potential to become therapies.
  • Launch of trial of ‘master switch’ drug to treat several cancer types
    Cancer Research UK and its commercial arm Cancer Research Technology (CRT) are launching a trial of an experimental drug shown to simultaneously block many enzymes that control cancer cell growth and death. The ‘master-switch’ experimental drug, owned by Astex Pharmaceuticals, could potentially treat a range of cancer types.
  • Smallest and fastest-known RNA switches provide new drug targets
    A University of Michigan biophysical chemist and his colleagues have discovered the smallest and fastest-known molecular switches made of RNA, the chemical cousin of DNA. The researchers say these rare, fleeting structures are prime targets for the development of new antiviral and antibiotic drugs.
  • Scientists use worms to unearth cancer drug targets
    Through novel experiments involving small nematode worms, scientists from University of Wyoming have discovered several genes that may be potential targets for drug development in the ongoing war against cancer. Specifically, researchers hypothesize that inhibiting these genes could reverse certain key traits associated with cancer cells. This discovery is published in the August 2012 issue of the Genetics Society of America’s journal Genetics.
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Podcasts

  • Evotec strengthens and expands its Alliance Business
    Dr Mark Ashton is Executive Vice President, Business Development of Evotec and is responsible for Evotec's commercial and partnering activities. Prior to assuming responsibility for Business Development in 2005, Dr Ashton held a number of positions within Operations at Evotec: He joined the Company in 1995 as one of the initial employees of the Discovery Division, becoming Department Manager in 2001, Director of Chemistry Services in 2002 and taking over responsibility for Evotec's Discovery Services Division in 2004, where he had responsibility for Evotec's screening, parallel synthesis and medicinal chemistry operations. During his time at Evotec, Dr Ashton has managed a wide range of pharmaceutical and biotechnology related projects, including medicinal chemistry projects, design and synthesis of screening libraries and technology transfer projects and has been involved in the progression of a number of drug candidates into the clinic in numerous therapeutic areas. Dr Ashton has authored and co-authored a number of peer reviewed papers, articles and book chapters in addition to being named on a number of pharmaceutical patents. He is trained as a medicinal chemist. Prior to joining Evotec, Dr Ashton also had spells at ICI Pharmaceuticals and Organon Laboratories. Mark Whittaker is Senior Vice President Drug Discovery at Evotec where he manages a large drug discovery collaboration and the groups of computational chemistry and structural biology. Before joining Evotec in 2001, Mark spent 13 years at British Biotech Pharmaceuticals where he led a number of medicinal chemistry programmes and was latterly Director of Chemistry. At British Biotech, Mark contributed to the discovery and development of six compounds that have progressed into human clinical trials. Before his career at British Biotech, Mark carried out post-doctoral research at the University of Oxford and at York University, Toronto and obtained a D. Phil in Chemistry from the University of York.
  • The Ubiquitin Story
    In this podcast interview with Drug Discovery Today, Nobel Prize winner Professor Aaron Ciechanover will talk about his career, his Nobel Prize-winning discovery of the UPS, and the extraordinary opportunities and challenges for drug discovery in this area.
  • Califf, Behrman and Kramer discuss the Clinical Trials Transformation Initiative.
    Download the Califf, Behrman and Kramer podcast as an mp3 file
  • Dr Brent Vose outlines AstraZeneca's oncology pipeline.
    Download the Dr. Brent Vose podcast as an mp3 file
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Webinars

  • The Promise of Epigenetics in Early Stage Drug Discovery
    Epigenetic targets are exciting to drug discovery scientists because they hold great potential across a wide spectrum of therapeutic areas. The field of epigenetics focuses on the investigation of enzymes that alter gene expression through modification of their target substrates, usually through the addition or removal of methyl or acetyl groups. High-throughput assays to identify agents capable of modifying the action of such enzyme targets has, in the past, proven to be challenging due to the relatively small molecular alterations in addition to the possibility of sequential modifications, leading to multiple end products. As such, high-throughput bioassays that allow the direct, concurrent quantification of multiple modification states are attractive. The RapidFire platform enables high-throughput mass spectrometric analysis of native molecules from in vitro reactions by performing on-line desalting in seconds, as opposed to HPLC, which requires minutes. Moreover, the RapidFire system can be connected to any mass spectrometer providing unparalleled versatility in reaction detection.
  • Integrated Quant / Qual for In-vivo Discovery Bioanalysis using Hybrid Quadrupole-Time-of-Flight Mass Spectrometry
    Ultra high performance liquid chromatography (UHPLC) coupled with orthogonal acceleration hybrid quadrupole-time-of-flight (QqTOF) mass spectrometry is an emerging technique offering new strategies for the efficient screening of new chemical entities (NCE) and related molecules at the early discovery stage within the pharmaceutical industry.
  • Drug Delivery: enabling technology for discovery and development
    The integration of pharmacodynamic and pharmacokinetic parameters in non clinical pharmacology studies is a key aspect in drug discovery for efficacy and safety assessment, in the particular for the translation from the non clinical to the clinical field. Modeling the profile of plasma exposure achieved with the intended therapeutic route often requires the use of intravenous infusion. In addition, in most cases infusion parameters (infusion rate, volume, duration and sequences) need to be customized to achieve the appropriate pattern of plasma drug exposure. When pharmacodynamic parameters are recorded by telemetry, the use of implantable pumps rather than external pumps is necessary to preserve the improvement in physiological data recording offered by telemetry.
  • Part 2: How has HR-MS technology fundamentally changed the way we study drug biotransformation and disposition?
    AB SCIEX is proud to present the 2nd installment of a Global 4-Part Live Webinar Series exploring novel and dynamic workflows for Metabolite Identification & Drug Metabolism solutions as it pertains to the 4 main stages of the drug discovery and development paradigm, Lead Discovery, Late Stage Discovery, Early Development and Late Stage Development. Part 2 of this webinar series will focus on how HRMS technology has fundamentally changed the way metabolite biotransformations are investigated in Lead Discovery.
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Features

  • Most downloaded review Q1 2009: Target discovery from data mining approaches
    The most downloaded review article from Drug Discovery Today from the first quarter of 2009 deals with the topic of target discovery from the informatics perspective. It would be difficult to overstate the value to Pharma of identifying and validating the most relevant therapeutic targets. In this article, Yang, Adelstein and Kassis outline text mining, its value and limitations and application to target discovery. In addition, they cover the field of emerging and integrated data mining approaches.
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Downloads

  • Fragment screening to predict druggability (ligandability) and lead discovery success
    In this article Fredrik N.B. Edfeldt et al. discuss using an initial fragment screen to determine the ligandability of new targets. An insightful analysis of the ligandability score, the success of HTS and entry into hit-to-lead is presented for 36 targets.
  • Ligand efficiency as a guide in fragment hit selection and optimization
    Fragment-based screening (FBS) has become an established approach for hit identification. Starting points identified by FBS, are small fragments that require substantial modification to become leads. As fragments are different from classical hits a process tailored for fragment evolution is required. Scores for ligand efficiency have been proposed as guides for this process. In this article the Sabine Schultes et al. review how these have been applied to guide the selection and optimization of fragment hits.
  • Fragments: past, present and future
    In this article Mark Whittaker et al. review the origin of the fragment-based drug discovery approach, discuss how it is being applied and the prospects for future development. Futhermore, they illustrate this with examples from their own projects where they have found that information from fragments can inform the optimisation of hits identified by other means (e.g. HTS and/or virtual screening) and vice versa.
  • Disease-specific target selection: a critical first step down the right road
    Relevance of a drug target for a disease is often inferred with strong belief but fragile evidence. Here, a program for early identification of human diseasespecific drug targets using high-throughput genetic associations is described
  • Identifying and validating novel targets with in vivo disease models: Guidelines for study design
    In vivo studies are an important tool for the identification and validation of novel drug targets in medicine; however, the interpretation of submitted and published data is often compromised by inadequate study design.
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