Elucidation of the working principle of a gene-directed caged HDAC inhibitor with cell-type selectivity.

Kotoko SakamotoAyumi HiranoRika HidakaAkinobu Z SuzukiTaro Ueno Toshiaki Furuta

Published in: Chemical communications (Cambridge, England) (2022)

Histone deacetylases (HDACs) play crucial roles in the epigenetic regulation of gene expression. Here, we report CM-Bhc-SAHA, a novel caged HDAC inhibitor, genetically targeting cells of interest. Mammalian cells expressing porcine liver esterase led to the optochemical inhibition of endogenous HDAC activity when treated with CM-Bhc-SAHA and irradiated with 405 nm light.

Keyphrases

histone deacetylase
gene expression
dna methylation
induced apoptosis
cell cycle arrest
genome wide
photodynamic therapy
cancer therapy
cell death
signaling pathway
newly diagnosed
structural basis