1355356-58-9Relevant articles and documents
Perfluorinated hydroxamic acids are potent and selective inhibitors of HDAC-like enzymes from Pseudomonas aeruginosa
Meyners, Christian,Wolff, Benjamin,Kleinschek, Alexander,Kr?mer, Andreas,Meyer-Almes, Franz-Josef
supporting information, p. 1508 - 1512 (2017/03/16)
A series of perfluorinated SAHA (PFSAHA) was prepared and profiled against a panel of human and bacterial members of the Histone deacetylase (HDAC) family. Some of the active substances show nanomolar inhibitory activity and several hundred fold selectivity for the HDAC like enzyme PA3774 from P. aeruginosa. The extraordinary selectivity against human HDACs results from the distinct oligomeric state of PA3774 which consists of two head-to-head dimers. The binding pocket is defined by the surface of both opposite monomers confining the access of ligands to the active site. In addition, the aromatic cap group of PFSAHA undergoes an edge-to-face aromatic interaction with phenylalanine from the opposite monomer.
HISTONE DEACETYLASE (HDAC) INHIBITING COMPOUNDS AND METHOD OF MAKING SAME
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Page/Page column 14-15, (2012/08/28)
The invention relates to novel HDAC inhibitors and a method of making such HDAC inhibitors. The present invention provides novel HDAC inhibitors having a perfluorinated linker between the metal-binding group and the cap group.