Description
Apicidin is a cyclic tetrapeptide that inhibits histone deacetylase (HDAC) and exhibits anticancer benefit. In oral squamous cell carcinoma cells, it upregulates expression of p21, inducing G2/M phase cell cycle arrest, apoptosis, and autophagy. In non-small cell lung cancer (NSCLC) cells, it downregulates expression of checkpoint kinase (CHK) 1, decreases phosphorylation of cdc25C and cdc2, and upregulates expression of cdc25A, inducing apoptotic cell death. Additionally, apicidin increases apoptosis in Brc-Abl positive leukemia cells through disruption of the mitochondrial membrane potential, activation of caspases 3, 8, and 9, cleavage of poly(ADP)-ribose polymerase (PARP), and release of cytochrome c. It also induces apoptosis in eosinophils and neutrophils.