[HTML][HTML] The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone …

J Kikuchi, S Yamada, D Koyama, T Wada… - Journal of Biological …, 2013 - ASBMB
Bortezomib therapy is now indispensable for multiple myeloma, but is associated with
patient inconvenience due to intravenous injection and emerging drug resistance. The
development of orally active proteasome inhibitors with distinct mechanisms of action is
therefore eagerly awaited. Previously, we identified homopiperazine derivatives as a novel
class of proteasome inhibitors with a different mode of proteasome binding from bortezomib.
In this study, we show that K-7174, one of proteasome inhibitory homopiperazine …