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A Linker for the Solid-Phase Synthesis of Hydroxamic Acids and Identification of HDAC6 Inhibitors.

Claus G BangJakob F JensenEmil O'Hanlon CohrtLasse B OlsenSaba G SiyumKim T MortensenTine SkovgaardJens BerthelsenLiang YangMichael GivskovKatrine M QvortrupThomas Eiland Nielsen
Published in: ACS combinatorial science (2017)
We herein present broadly useful, readily available and nonintegral hydroxylamine linkers for the routine solid-phase synthesis of hydroxamic acids. The developed protocols enable the efficient synthesis and release of a wide range of hydroxamic acids from various resins, relying on high control and flexibility with respect to reagents and synthetic processes. A trityl-based hydroxylamine linker was used to synthesize a library of peptide hydroxamic acids. The inhibitory effects of the compounds were examined for seven HDAC enzyme subtypes using a chemiluminescence-based assay.
Keyphrases
  • histone deacetylase
  • clinical practice
  • sensitive detection
  • mass spectrometry
  • high resolution
  • bioinformatics analysis