|Publication Type||Journal Article|
|Year of Publication||2013|
|Authors||Olson, DE, Wagner, FF, Kaya, T, Gale, JP, Aidoud, N, Davoine, EL, Lazzaro, F, Weïwer, M, Zhang, Y-L, Holson, EB|
|Journal||J Med Chem|
|Date Published||2013 Jun 13|
|Keywords||Antineoplastic Agents, HeLa Cells, Histone Deacetylase Inhibitors, Histone Deacetylases, Humans, Hydroxamic Acids, Molecular Docking Simulation, Phthalic Acids, Protein Binding, Repressor Proteins, Structure-Activity Relationship|
We disclose the first small molecule histone deacetylase (HDAC) inhibitor (3, BRD73954) capable of potently and selectively inhibiting both HDAC6 and HDAC8 despite the fact that these isoforms belong to distinct phylogenetic classes within the HDAC family of enzymes. Our data demonstrate that meta substituents of phenyl hydroxamic acids are readily accommodated upon binding to HDAC6 and, furthermore, are necessary for the potent inhibition of HDAC8.
|Alternate Journal||J. Med. Chem.|