Description
Staurosporine is an alkaloid initially produced by Streptomyces that inhibits PKC and other protein kinases. Staurosporine is a precursor in the synthesis of kinase inhibitors K252c and PKC412. This compound exhibits anticancer, anti-parasitic, and anti-protozoan activities. Staurosporine induces apoptosis in hepatocarcinoma cells by decreasing levels of p38 MAPK, pERK, and DNA methyltransferase 3B (DNMT 3B) and increasing levels of pJNK. Staurosporine also causes cell death in Trypanosoma. This compound also inhibits mammalian RNA splicing.
References
Zhao C, Yin P, Mei C, et al. Down-regulation of DNA methyltransferase 3B in staurosporine-induced apoptosis and its mechanism in human hepatocarcinoma cell lines. Mol Cell Biochem. 2013 Apr;376(1-2):111-9. PMID: 23397112.
Bruges G, Betancourt M, March M, et al. Apoptotic-like activity of staurosporine in axenic cultures of Trypanosoma evansi. Rev Inst Med Trop Sao Paulo. 2012 Mar-Apr;54(2):103-8. PMID: 22499424.
Aukema KG, Chohan KK, Plourde GL, et al. Small molecule inhibitors of yeast pre-mRNA splicing. ACS Chem Biol. 2009 Sep 18;4(9):759-68. PMID: 19634919.
Tanramluk D, Schreyer A, Pitt WR, et al. On the origins of enzyme inhibitor selectivity and promiscuity: a case study of protein kinase binding to staurosporine. Chem Biol Drug Des. 2009 Jul;74(1):16-24. PMID: 19519740.
