bortezomib-ps-341

Description: Bortezomib (foremrly also known as PS-341; trade names name Velcade among others), a dipeptide boronic acid derivative, is cell-permeable, reversible, potent and highly selective inhibitor of 20S proteasome with potential antitumor activity. It inhibits 20S proteasome with a Ki of 0.6 nM in a cell-free assay. The ubiquitin-proteasome pathway plays a critical role in the regulated degradation of proteins involved in cell cycle control and tumor growth. Dysregulating the degradation of such proteins should have profound effects on tumor growth and cause cells to undergo apoptosis. As a potent 20S proteasome inhibitor, bortezomib has potential antineoplastic activity and was approved in 2003 in the U.S. and Europe for the treatment relapsed multiple myeloma and mantle cell lymphoma. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy.

References: Cancer Res. 1999; 59(11):2615-22; Cancer Cell Int. 2005; 5(1):18; Cancer Res. 2002; 62(17):4996-5000.

Related CAS: 205393-22-2 (Bortezomib-pinanediol)