verticillins and Neoplasms

Increasing studies show that methylation of histone lysine residues is implicated in the development and progression of varying disease states such as schizophrenia, diabetes, and multiple human cancers. Targeting the specific enzymes responsible for these processes has fueled global investigation into the understanding and correction of epigenetic pathology. This review aims to assemble a timely account of the current progress against chromatin-modifying histone lysine methyltransferases (KMTs) and demethylases (KDMs) to inform ongoing and future efforts into this promising field. In particular, we report on their role in tumor growth and progression and the development of small molecules that modulate these enzymes.

Topics: Animals; Epigenomics; Histone Demethylases; Histone-Lysine N-Methyltransferase; Histones; Humans; Lysine; Methylation; Neoplasms

The aim is to reveal the role of PFKFB3 in 11'-deoxyverticillin A (C42)-induced autophagy and apoptosis.. Electron and fluorescence microscopy, immunoblotting, MTS assay, siRNA interference and real time PCR were used.. C42 could induce multiple cell death in HeLa cells. Knockdown of either Beclin 1 or LC3, two important autophagic genes, increased both PARP-1 cleavage and cell viability loss. Although high dose of C42 triggered more cell viability loss, yet, it failed to augment autophagic flux. While PFKFB3 inhibitors attenuated C42-induced autophagy, the overexpression of PFKFB3 increased the induced autophagic flux.. PFKFB3 is involved in C42 induced-autophagy, which blunts the caspase-dependent apoptotic process.

Topics: Apoptosis; Autophagy; Disulfides; HeLa Cells; Humans; Neoplasms; Phosphofructokinase-2; Piperazines