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Potent and Selective Inhibition of Histone Deacetylase 6 (HDAC6) Does Not Require a Surface-Binding Motif.
|Publication Type||Journal Article|
|Authors||Wagner, FF, Olson DE, Gale JP, Kaya T., Weïwer M., Aidoud N., Thomas M., Davoine EL, Lemercier BC, Zhang YL, and Holson EB|
|Abstract||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.|
|Year of Publication||2013|
|Journal||Journal of medicinal chemistry|
|Date Published (YYYY/MM/DD)||2013/02/18|