Preferred Label : CoREST Inhibitor TNG260;
NCIt synonyms : CoreDAC Inhibitor TNG260; CoREST-selective Deacetylase Inhibitor TNG260;
NCIt definition : An orally bioavailable small molecule inhibitor of the histone deacetylase 1 (HDAC1)-containing
co-repressor of repressor element-1 silencing transcription (CoREST) complex, with
potential immunomodulating activity. Upon oral administration, CoREST inhibitor TNG260
binds to CoREST complex and inhibits the catalytic activity of HDAC1, which results
in an accumulation of highly acetylated chromatin histones, the induction of chromatin
remodeling and an altered pattern of gene expression. This may reverse immune evasion
and resistance to immune checkpoint inhibitors caused by serine-threonine kinase 11
(STK11) mutations. Loss-of-function mutations in STK11 is associated with immune checkpoint
inhibitor resistance.;
Molecule name : TNG 260; TNG-260;
NCI Metathesaurus CUI : CL1907079;
Origin ID : C200247;
concept_is_in_subset
- has_target
