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Apicidin, a fungal metabolite, contains potent and broad antiprotozoal characteristics in vitro against Apicomplexan parasites. This compound has also been shown to be active in mice against Plasmodium berghei. Apicidin is an HDAC inhibitor. Mechanistic studies utilizing Apicidin inhibition in low nanomolar concentration has been shown to cause hyperacetylation of histones in the Apicomplexan HDAC (histone deacetylase), which causes hyperacetylation of histones within the parasite. It has been reported that Apicidin also contains a wide range of antiproliferative activity against various cancer cell lines in mice, again through HDAC inhibition. Apicidin has also been shown to stimulate apoptosis via induction of Fas/Fas ligand. Furthermore, it has been reported to dramatically decrease HIF-1α levels and therefore reduce transcriptional activity of HIF-1 in murine cell lines. Apicidin is an inhibitor of HDAC3 and N-CoR.
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2. Han, J W., et al., 2000. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer research. 60(21): 6068-74. PMID: 11085529
3. Colletti, S L., et al., 2001. Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1. Bioorganic & medicinal chemistry letters. 11(2): 107-11. PMID: 11206438
4. Singh, Sheo B., et al., 2002. Structure and chemistry of apicidins, a class of novel cyclic tetrapeptides without a terminal alpha-keto epoxide as inhibitors of histone deacetylase with potent antiprotozoal activities. The Journal of organic chemistry. 67(3): 815-25. PMID: 11856024
5. Hong, JangJa., et al., 2003. Apicidin, a histone deacetylase inhibitor, induces differentiation of HL-60 cells. Cancer letters. 189(2): 197-206. PMID: 12490313
6. Kim, Se-Hee., et al., 2007. Regulation of the HIF-1alpha stability by histone deacetylases. Oncology reports. 17(3): 647-51. PMID: 17273746
See how others have used Apicidin. Click on the entry to view the PubMed entry .
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