149648-29-3Relevant academic research and scientific papers
Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif
Wagner, Florence F.,Olson, David E.,Gale, Jennifer P.,Kaya, Taner,We?wer, Michel,Aidoud, Nadia,Thomas, Méryl,Davoine, Emeline L.,Lemercier, Bérénice C.,Zhang, Yan-Ling,Holson, Edward B.
, p. 1772 - 1776 (2013/04/10)
Hydroxamic acids were designed, synthesized, and evaluated for their ability to selectively inhibit human histone deacetylase 6 (HDAC6). Several inhibitors, including compound 14 (BRD9757), exhibited excellent potency and selectivity despite the absence of a surface-binding motif. The binding of these highly efficient ligands for HDAC6 is rationalized via structure-activity relationships. These results demonstrate that high selectivity and potent inhibition of HDAC6 can be achieved through careful choice of linker element only.
