MALVERN, Pa.--(BUSINESS WIRE)--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.”
About USP7 and P5091. The DUB USP7 is a well validated target for the treatment of neoplastic disease. USP7 stabilizes oncogenic proteins and promotes the degradation of tumor suppressors such as p53. Due to its broad range of oncogenic protein substrates, USP7 inhibition is predicted to be efficacious for the treatment of both p53 wild type and p53 mutant tumors. P5091 is an early scaffold in Progenra’s USP7 program that has been used to demonstrate proof of concept in animal tumor models. Progenra is committed to moving this and alternative novel compounds toward the clinic with the hope of bringing patients new treatments.
About Dana-Farber Cancer Institute. (www.dana-farber.org) Since its founding in 1947, Dana-Farber has been committed to providing adults and children with cancer with the best treatment available today while developing tomorrow's cures through cutting-edge research.
About Progenra, Inc. Founded in 2002, Progenra (www.progenra.com) seeks to discover and develop high value medicines exploiting ubiquitin pathways. Utilizing its world-class UbiPro™ Drug Discovery Platform, Progenra identifies novel modulators of ubiquitin targets as potential drugs that act therapeutically via the various documented roles of ubiquitin pathway components in disease.