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- Title
In-Bead Screening of Hydroxamic Acids for the Identification of HDAC Inhibitors.
- Authors
Qvortrup, Katrine; Nielsen, Thomas E.
- 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.
- Subjects
COMBINATORIAL chemistry; HISTONE deacetylase inhibitors; PHOTOLABILE compounds; HYDROXAMIC acids; SOLID-phase synthesis
- Publication
Angewandte Chemie, 2016, Vol 128, Issue 14, p4548
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201511308