Ontology highlight
ABSTRACT:
SUBMITTER: Methot JL
PROVIDER: S-EPMC4027730 | biostudies-literature | 2014 Apr
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20140102 4
The identification and in vitro and in vivo characterization of a potent SHI-1:2 are described. Kinetic analysis indicated that biaryl inhibitors exhibit slow binding kinetics in isolated HDAC1 and HDAC2 preparations. Delayed histone hyperacetylation and gene expression changes were also observed in cell culture, and histone acetylation was observed in vivo beyond disappearance of drug from plasma. In vivo studies further demonstrated that continuous target inhibition was well tolerated and effi ...[more]