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  • Celebrating success: 2011 announced as the International Year of Chemistry
    The United Nations Educational, Scientific and Cultural Organization (UNESCO) and International Union of Pure and Applied Chemistry (IUPAC) announced in 2008 that The International Year of Chemistry (IYC) would be celebrated in 2011. This exciting initiative celebrates success in chemistry hopefully to spark renewed excitement for the future of discovery in chemistry. IYC 2011 is an opportunity to encourage young, enthusiastic scientists, to celebrate the contribution of advancements in chemistry within our society and promote appreciation for women in science. By Ellen Smyth
  • Leeds Scientists Develop Potential New Multiple Myeloma Therapy
    A treatment for the incurable blood cancer Multiple Myeloma could be developed in the future if a groundbreaking scientific discovery is applied to new Leeds-based research into the disease.
  • The BIG retreat
    Some of pharmaceutical’s big boys, for example Pfizer, have faced well-documented challenges over the last 12 months. The industry is only too aware of this and understands that now is the time to look at new processes and a change in the way they have traditionally done business.
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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

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Downloads

  • Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity
    Here, we review the performance of chromatographic hydrophobicity measurements in a data set of 100 000 GlaxoSmithKline compounds, demonstrating the advantages of the method over octanol–water partitioning and highlighting new insights for drug discovery. The value of chromatographic measurements, versus other hydrophobicity estimates, was supported by improved relationships with solubility, permeation, cytochrome P450s, intrinsic clearance, hERG binding and promiscuity. We also observed marked differentiation of the relative influence of intrinsic and effective hydrophobicity. The summing of hydrophobicity values plus aromatic ring count [log DpH7.4 (or log P) + #Ar], indicated a wide relevance for simplistic ‘property forecast indices’ in developability assays, clearly enhanced by chromatographic values; therefore establishing new foundations for enriching property-based drug design.
  • The graphical representation of ADME-related molecule properties for medicinal chemists
    Timothy J. Ritchie, Peter Ertl and Richard Lewis review various approaches that have been used to represent molecule properties graphically in the context of oral ‘drug likeness’, with the goal of improving the decision making of medicinal chemists during the drug discovery process.
  • ROCK: the Roche medicinal chemistry knowledge application – design, use and impact
    Alexander Maywe et al. discuss ROCK (Roche medicinal chemistry knowledge), an internal user-friendly and peer-reviewed Wiki-like application to capture, browse and search tacit knowledge, key discoveries and property effects related to chemical structure, which is used as a primary source for addressing challenges faced in drug design.
  • The future of discovery chemistry: quo vadis? Academic to industrial – the maturation of medicinal chemistry to chemical biology
    In this article, Torsten Hoffmann and Cheryl Bishop outline a chain of thoughts that concludes that chemistry has a wider part to play in innovative drug discovery than it is currently permitted by industry to have.
  • How well do medicinal chemists learn from experience?
    David R. Cheshire provides evidence that suggests that modern medicinal chemists are overproductive in that they synthesise many more compounds than are required to achieve the objectives of the project.
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