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Showing 1–5 of 5 results
Advanced filters: Author: Jörg Eder Clear advanced filters

  • Previous analyses of new drug approvals have suggested that phenotypic screening strategies have been more productive than target-based approaches in the discovery of first-in-class small-molecule drugs. Eder and colleagues analysed the origins of the first-in-class drugs approved by the US Food and Drug Administration from 1999 to 2013, and found that target-based approaches have had a substantial impact in more recent years. They discuss the implications for drug discovery strategies, including viewing phenotypic screening as a novel discipline rather than as a neoclassical approach.

    • Jörg Eder
    • Richard Sedrani
    • Christian Wiesmann
    Research
    Nature Reviews Drug Discovery
    Volume: 13, P: 577-587

  • There has been a resurgence in interest in phenotypic drug discovery (PDD) approaches in recent years based on their potential to address the incompletely understood complexity of diseases and their promise of delivering first-in-class drugs. However, PDD approaches can also present considerable challenges, and this article focuses on the lessons learned by researchers engaged in PDD in the pharmaceutical industry, and discusses how PDD can best deliver value to drug discovery portfolios.

    • John G. Moffat
    • Fabien Vincent
    • Marco Prunotto
    Reviews
    Nature Reviews Drug Discovery
    Volume: 16, P: 531-543

  • Dysregulation of protein degradation by the ubiquitin-proteasome system is a feature commonly associated with cancer. Here, the authors develop an orally available small molecule that inhibits CSN5, the proteolytic subunit of the COP9 signalosome, and blocks tumour growth in a xenograft model.

    • Anita Schlierf
    • Eva Altmann
    • Bruno Martoglio
    ResearchOpen Access
    Nature Communications
    Volume: 7, P: 1-10

  • A fragment-based design approach identifies reversible inhibitors targeting human protease complement factor D (FD), which is required for amplification of complement C3 signaling. FD inhibitors act as systemic regulators of complement activation in vivo.

    • Jürgen Maibaum
    • Sha-Mei Liao
    • Karen Anderson
    Research
    Nature Chemical Biology
    Volume: 12, P: 1105-1110