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Bead-based screening in chemical biology and drug discovery

Komnatnyy, Vitaly V ; Nielsen, Thomas E ; Qvortrup, Katrine

Chemical communications (Cambridge, England), 2018-06, Vol.54 (5), p.6759-6771 [Periódico revisado por pares]

England: Royal Society of Chemistry

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  • Título:
    Bead-based screening in chemical biology and drug discovery
  • Autor: Komnatnyy, Vitaly V ; Nielsen, Thomas E ; Qvortrup, Katrine
  • Assuntos: Combinatorial analysis ; Combinatorial chemistry ; Combinatorial Chemistry Techniques - methods ; Drug delivery systems ; Drug Discovery ; High-Throughput Screening Assays - methods ; Libraries ; Organic chemistry ; Peptide Library ; Screening ; Small Molecule Libraries - chemistry
  • É parte de: Chemical communications (Cambridge, England), 2018-06, Vol.54 (5), p.6759-6771
  • Notas: Dr Vitaly Komnatnyy obtained his PhD in 2012 from the Technical University of Denmark (DTU) under the supervision of Professor Thomas E. Nielsen. His doctoral work was dedicated to development of synthetic methods for creating molecular libraries on solid supports. In 2013-2014 he continued his stay as a researcher in Professor Nielsen's group, before joining Professor Stephan Pless's group at the University of Copenhagen in 2015 for a short postdoctoral stay. Since 2016 Dr Komnatnyy has been employed as Development Scientist at Novo Nordisk A/S. His scientific interests comprise chemical biology, in particular synthesis of peptides and peptidomimetics for probing biological targets.
    Dr Katrine Qvortrup obtained her PhD from the University of Copenhagen under the supervision of Prof. Mogens Brøndsted, before doing postdoctoral work at Princeton University (with Prof. David MacMillan) and the Technical University of Denmark, DTU (with Prof. Thomas Nielsen). In July 2017 Katrine Qvortrup was appointed as Assistant Professor at DTU, Chemistry Department, where she is leading a dynamic research group that aims to develop new approaches to address long-standing problems in Chemical Biology. Her research efforts aim at developing screening technologies and lead compounds for drug discovery. Her current focus is directed towards inflammatory diseases, cancer and drug delivery.
    Professor Thomas E. Nielsen started his independent career in 2008 at the Technical University of Denmark (DTU), heading the development of new synthesis methodology, bioactive materials, and assay technologies. In 2014, he became director of Protein & Peptide Chemistry, Novo Nordisk A/S, and affiliated as a professor at the University of Copenhagen. A central theme in his research is the chemical synthesis of small molecules, peptides, and modified proteins to probe biological phenomena and ultimately provide the basis for the development of new medicines. Thomas E. Nielsen has received several scientific awards and co-authored more than 90 journal publications.
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  • Descrição: High-throughput screening is an important component of the drug discovery process. The screening of libraries containing hundreds of thousands of compounds requires assays amenable to miniaturisation and automization. Combinatorial chemistry holds a unique promise to deliver structurally diverse libraries for early drug discovery. Among the various library forms, the one-bead-one-compound (OBOC) library, where each bead carries many copies of a single compound, holds the greatest potential for the rapid identification of novel hits against emerging drug targets. However, this potential has not yet been fully realized due to a number of technical obstacles. In this feature article, we review the progress that has been made in bead-based library screening and its application to the discovery of bioactive compounds. We identify the key challenges of this approach and highlight key steps needed for making a greater impact in the field. High-throughput screening is an important component of the drug discovery process.
  • Editor: England: Royal Society of Chemistry
  • Idioma: Inglês
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