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 International Edition
Volume55
Issue number14
Pages (from-to)4472-4475
Number of pages4
ISSN1433-7851
DOIs
Publication statusPublished - 2016

Keywords

  • Combinatorial libraries
  • HDAC inhibitors
  • In-bead screening
  • Photolabile linker

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