Definition

A ruthenium-based, small molecule that selectively inhibits stress-induced upregulation of GRP78, with potential antineoplastic activity. Although the exact mechanisms(s) through which this agent exerts its effects have yet to be fully elucidated, upon administration, BOLD-100 may selectively inhibit stress-induced upregulation of GRP78, thereby preventing the activation of multiple GRP78-mediated pathways and blocking GRP78-induced suppression of apoptotic pathways. This may lead to the induction of tumor cell apoptosis and slow tumor cell proliferation. GRP78, the endoplasmic reticulum (ER) chaperone and unfolded protein response (UPR) regulator, is overexpressed on the surface of a variety of cancer cell types. Its expression is associated with increased tumor cell survival and proliferation, as well as angiogenesis and resistance to chemotherapy.