Unknown

Dataset Information

0

Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.


ABSTRACT: Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell lines, the hybrid 5 impaired cell viability at low micromolar level and in leukemia U937 and rhabdomyosarcoma RH4 cells provided G1 arrest, apoptotic induction, and increased differentiation, associated with an increase of acetyl-H3 and acetyl-α-tubulin and a decrease of H3K27me3 levels. In glioblastoma U87 cells, 5 hampered epithelial to mesenchymal transition by increasing the E-cadherin expression, thus proposing itself as a useful candidate for anticancer therapy.

SUBMITTER: Romanelli A 

PROVIDER: S-EPMC7236245 | biostudies-literature |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC6651501 | biostudies-literature
2024-09-10 | GSE264565 | GEO
| S-EPMC5554914 | biostudies-literature
| S-EPMC7238858 | biostudies-literature
| S-EPMC6466523 | biostudies-literature
| S-EPMC8876975 | biostudies-literature
| S-EPMC8658794 | biostudies-literature
| S-EPMC4399029 | biostudies-literature
| S-EPMC6249066 | biostudies-literature
| S-EPMC4230991 | biostudies-literature