Carfilzomib CAS# 868540-17-4 卡非佐米
Carfilzomib, also known as PR-171, is a tetrapeptide epoxyketone and an epoxomicin derivate with potential antineoplastic activity. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth. Carfilzomib was approved by the FDA for use in patients with relapsed and refractory multiple myeloma on 20 July 2012.
📌 参考资料/链接：
Screen, Michael; Britton, Matthew; Downey, Sondra L.; Verdoes, Martijn; Voges, Mathias J.; Blom, Annet E. M.; Geurink, Paul P.; Risseeuw, Martijn D. P.; Florea, Bogdan I.; van der Linden, Wouter A.; Pletnev, Alexandre A.; Overkleeft, Herman S.; Kisselev, Alexei F. Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors. Journal of Biological Chemistry. Volume 285. Issue 51. Pages 40125-40134. Journal. (2010).
Screen, Michael; Britton, Matthew; Downey, Sondra L.; Verdoes, Martijn; Voges, Mathias J.; Blom, Annet E. M.; Geurink, Paul P.; Risseeuw, Martijn D. P.; Florea, Bogdan I.; van der Linden, Wouter A.; Pletnev, Alexandre A.; Overkleeft, Herman S.; Kisselev, Alexei F. Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors. Journal of Biological Chemistry. Volume 285. Issue 51. Pages 40125-40134. Journal. (2010).
📄 详细内容
CAS No. 868540-17-4 卡非佐米Carfilzomib synthetic routes
Screen, Michael; Britton, Matthew; Downey, Sondra L.; Verdoes, Martijn; Voges, Mathias J.; Blom, Annet E. M.; Geurink, Paul P.; Risseeuw, Martijn D. P.; Florea, Bogdan I.; van der Linden, Wouter A.; Pletnev, Alexandre A.; Overkleeft, Herman S.; Kisselev, Alexei F. Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors. Journal of Biological Chemistry. Volume 285. Issue 51. Pages 40125-40134. Journal. (2010).
产品链接: CAS No. 868540-17-4 ››
Screen, Michael; Britton, Matthew; Downey, Sondra L.; Verdoes, Martijn; Voges, Mathias J.; Blom, Annet E. M.; Geurink, Paul P.; Risseeuw, Martijn D. P.; Florea, Bogdan I.; van der Linden, Wouter A.; Pletnev, Alexandre A.; Overkleeft, Herman S.; Kisselev, Alexei F. Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors. Journal of Biological Chemistry. Volume 285. Issue 51. Pages 40125-40134. Journal. (2010).
产品链接: CAS No. 868540-17-4 ››