Oprozomib [ONX 0912]

Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047): H.J. Zhou, et al.; J. Med. Chem. 52, 3028 (2009) | A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma: D. Chauhan, et al.; Blood 116, 4906 (2010) | The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects: M.A. Hurchla, et al.; Leukemia 27, 430 (2013) | Carfilzomib and ONX 0912 inhibit cell survival and tumor growth of head and neck cancer and their activities are enhanced by suppression of Mcl-1 or autophagy: Y. Zang, et al.; Clin. Cancer Res. 18, 5639 (2012) | The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4: Y. Zang, et al.; Autophagy 8, 1873 (2012) | Effect of novel proteasome and immunoproteasome inhibitors on dendritic cell maturation, function, and expression of IkappaB and NFkappaB: A.S. Al-Homsi, et al.; Transpl. Immunol. 29, 1 (2013) | Overview of proteasome inhibitor-based anti-cancer therapies: Perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system: Q.P. Dou & J.A. Zonder; Curr. Cancer Drug Targets 14, 517 (2014) | Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma: L. Kubiczkova, et al.; J. Cell. Mol. Med. 18, 947 (2014) | Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma: Y.P. Vandewynckel, et al.; Oncotarget 7, 34988 (2016) | Second Generation Proteasome Inhibitors in Multiple Myeloma: A. Gozzetti, et al.; Anticancer Agents Med. Chem. 17, 920 (2017) | Anti-angiogenic and anti-multiple myeloma effects of oprozomib (OPZ) alone and in combination with pomalidomide (Pom) and/or dexamethasone (Dex): E. Sanchez, et al.; Leuk. Res. 57, 45 (2017) (Review)