In-Bead Screening of Hydroxamic Acids for the Identification of HDAC Inhibitors

Katrine Qvortrup, Thomas Eiland Nielsen

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

A one bead–one compound screening format is presented. Following solid-phase synthesis on a photolabile linker, library compounds were readily released and screened inside polymer beads. The release of screening compounds was readily controlled by varying photolysis time and light intensity. Dose-response experiments were carried out to effectively distinguish high- and low-affinity ligands. A library containing 55 800 compounds was synthesized and screened in a fluorometric assay, thereby identifying potent HDAC inhibitors with IC50 values in the nanomolar range.
Original languageEnglish
JournalAngewandte Chemie
Volume128
Issue number14
Pages (from-to)4548-4551
Number of pages4
ISSN0044-8249
DOIs
Publication statusPublished - 2016

Keywords

  • HDAC-Inhibitoren
  • Kombinatorische Bibliotheken
  • Photolabile Linker
  • Screening in Kügelchen

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