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Showing 1–25 of 25 results
Advanced filters: Author: John P Overington Clear advanced filters
  • For the past decade, the number of molecular targets for approved drugs has been debated. In this article and the accompanying poster, Overington and colleagues provide a comprehensive survey of current drug targets and a wealth of associated information on the characteristics of target families and the drugs that modulate them.

    • John P. Overington
    • Bissan Al-Lazikani
    • Andrew L. Hopkins
    Reviews
    Nature Reviews Drug Discovery
    Volume: 5, P: 993-996
  • Nicole Soranzo, Tim Spector, Gabi Kastenmüller and colleagues report a large-scale analysis of genetic variants influencing human blood metabolite levels. They identify genome-wide significant associations at 145 loci, providing a framework for exploring relationships between genetic variation, metabolism and complex disease.

    • So-Youn Shin
    • Eric B Fauman
    • Nicole Soranzo
    Research
    Nature Genetics
    Volume: 46, P: 543-550
  • The success of mechanism-based drug discovery depends on the definition of the drug target, but targets are often poorly defined in the literature. Here, Overington and colleagues present a comprehensive map of the molecular targets of approved drugs, and explore aspects including the footprint of target classes across disease areas, the success of privileged target families and drug target orthologues across standard model organisms.

    • Rita Santos
    • Oleg Ursu
    • John P. Overington
    Research
    Nature Reviews Drug Discovery
    Volume: 16, P: 19-34
  • Schistosoma mansoni and Schistosoma japonicum are the pathogenic agents that cause the tropical disease schistosomiasis. Here, and in an accompanying paper, the genomes of these two flatworms are sequenced and analysed. The results provide insights into the molecular architecture and host interactions of the flatworms, as well as avenues for future development of targeted interventions for schistosomiasis.

    • Matthew Berriman
    • Brian J. Haas
    • Najib M. El-Sayed
    ResearchOpen Access
    Nature
    Volume: 460, P: 352-358
  • Classification of proteins by ligand binding similarity offers an alternative approach to evolutionary methods for organizing and understanding biology, allowing new insights into protein function and physiological signal transduction.

    • Gerard J P van Westen
    • John P Overington
    News & Views
    Nature Methods
    Volume: 10, P: 116-117
  • Genome sequences of human-infective tapeworm species reveal extreme losses of genes and pathways that are ubiquitous in other animals, species-specific expansions of non-canonical heat shock proteins and families of known antigens, specialized detoxification pathways, and metabolism that relies on host nutrients; this information is used to identify new potential drug targets.

    • Isheng J. Tsai
    • Magdalena Zarowiecki
    • Matthew Berriman
    ResearchOpen Access
    Nature
    Volume: 496, P: 57-63
  • The wealth of genomic data for pathogens that cause tropical diseases hold considerable promise for the discovery of novel drugs. An international consortium describes how the TDR Targets database integrates this data with related biochemical and pharmacological data to facilitate the identification and prioritization of drug targets.

    • Fernán Agüero
    • Bissan Al-Lazikani
    • Christophe L. M. J. Verlinde
    Reviews
    Nature Reviews Drug Discovery
    Volume: 7, P: 900-907
  • A common assumption in current drug discovery strategies is that compounds with highin vitro potency at their target(s) have a greater potential to translate into successful, low-dose therapeutics, which is reflected in screening cascades with in vitro potency embedded as an early filter. This analysis of the publicly available ChEMBL database, which includes more than 500,000 drug discovery and marketed oral drug compounds, suggests that the perceived benefit of high in vitropotency may be negated by poorer absorption, distribution, metabolism, elimination and toxicity (ADMET) properties.

    • M. Paul Gleeson
    • Anne Hersey
    • John Overington
    Research
    Nature Reviews Drug Discovery
    Volume: 10, P: 197-208
  • Drugs that are chemically quite similar often bind to biologically diverse protein targets, and it is unclear how selective many of these compounds are. Because many drug–target combinations exist, it would be useful to explore possible interactions computationally. Here, 3,665 drugs are tested against hundreds of targets; chemical similarities between drugs and ligand sets are found to predict thousands of unanticipated associations.

    • Michael J. Keiser
    • Vincent Setola
    • Bryan L. Roth
    Research
    Nature
    Volume: 462, P: 175-181
  • Can traditional computational analysis and machine learning help compensate for inadequate peer review of drug-repurposing papers in the context of an infodemic?

    • Jeremy M. Levin
    • Tudor I. Oprea
    • Alex Zhavoronkov
    Comments & Opinion
    Nature Biotechnology
    Volume: 38, P: 1127-1131
  • In 2014, the Illuminating the Druggable Genome programme was launched to promote the exploration of currently understudied but potentially druggable proteins. This article discusses how the systematic collection and processing of a wide array of biological and chemical data as part of this programme has enabled the development of evidence-based criteria for tracking the target development level of human proteins, which indicates a substantial knowledge deficit for approximately one out of three proteins in the human proteome. It also highlights the nature of the unexplored therapeutic opportunities for major protein families.

    • Tudor I. Oprea
    • Cristian G. Bologa
    • Gergely Zahoránszky-Köhalmi
    Research
    Nature Reviews Drug Discovery
    Volume: 17, P: 317-332
  • Chemical probes are powerful reagents with increasing impacts on biomedical research. However, probes of poor quality or that are used incorrectly generate misleading results. To help address these shortcomings, we will create a community-driven wiki resource to improve quality and convey current best practice.

    • Cheryl H Arrowsmith
    • James E Audia
    • William J Zuercher
    Comments & Opinion
    Nature Chemical Biology
    Volume: 11, P: 536-541