Published on September 17, 2012 at 1:17 AM
Researchers at the Dana-Farber Cancer Institute and Progenra, Inc.
announce the publication of a research article entitled "A Small
Molecule Inhibitor of Ubiquitin-Specific Protease-7 Induces Apoptosis in
Multiple Myeloma Cells and Overcomes Bortezomib Resistance" (Chauhan et
al, Cancer Cell).
Data presented in this study include a comprehensive in vitro and in
vivo analysis of the novel small molecule USP7 inhibitor P5091,
discovered by Progenra. This selective inhibitor of USP7 induces
anti-multiple myeloma activity alone and in combination with approved
chemotherapeutic agents in cultured cells. Further, P5091 inhibits the
growth of bortezomib resistant multiple myeloma tumor cells and
suppresses tumor burden in distinct animal tumor models. In particular,
when tested at their respective maximum tolerated doses, P5091 and
VELCADE® repressed myeloma xenograft growth with equivalent efficacies.
The lead author of the study Dr. Dharminder Chauhan stated, "Targeting
the ubiquitin proteasome system upstream of the proteasome, as
exemplified by these studies with Progenra's USP7 inhibitor P5091,
offers a novel opportunity for new treatments for multiple myeloma and
other refractory cancers."
Source: Dana-Farber Cancer Institute