<i>In vitro</i> and <i>in vivo</i> activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphoma

In vitro and in vivo activity of a new small-molecule inhibitor of HDAC6 in mantle cell lymphomaCancer origin and development is associated not only with genetic alterations, but also with the disturbance of epigenetic profiles. 1In this regard, the tumoral epigenome is characterized by both specific and general shifts in the DNA methylation and histone-modification landscapes. 1 However, in contrast to genetic disruption, the effect of epigenetic modifications or marks may potentially be reversed by the use of drugs that target enzymes involved in adding, removing or signaling DNA methylation and histone modifications. 1 This basic knowledge has been adopted into clinical practice, and inhibitors of histone deacetylases and DNA demethylating agents have been approved for use in the therapy of hematologic malignancies, such as cutaneous T-cell lymphoma and myelodysplastic syndrome, respectively. 2Other promising epigenetic drugs include inhibitors of histone methyltransferases, 2 histone demethylases, 2 histone kinases, 3 and bromodomain proteins that interfere with the 'reading' of acetylated histone residues. 4,5istone deacetylase 6 (HDAC6) is a protein modifier that is an increasingly attractive pharmacological target.It is a member of class IIb of the histone deacetylase family, together with HDAC10. 6Unlike most HDACs,