Preferred Label : KAT2A/KAT2B Degrader AUTX-703;
NCIt synonyms : KAT2A/B Protein Degrader AUTX-703; KAT2A/KAT2B Protein Degrader AUTX-703;
NCIt definition : An orally bioavailable, small molecule degrader of the histone acetyltransferases
and transcriptional activators lysine acetyltransferase 2A (KAT2A) and its paralog
lysine acetyltransferase 2B (KAT2B), with potential antineoplastic activity. Upon
oral administration, KAT2A/KAT2B degrader AUTX-703 targets, binds to and selectively
degrades KAT2A and KAT2B. This prevents the acetylation of non-histone substrates
and transcription of certain genes, such as MYC. KAT2A/KAT2B degradation by AUTX-703
reverses the block in differentiation of certain cancer cells, promotes epithelial
cell state differentiation towards a more terminally differentiated state, and inhibits
proliferation in susceptible tumor cells. In addition, epithelial differentiation
induced by AUTX-703 enhances expression of antigen presenting genes in certain tumor
cells. KAT2A and KAT2B, epigenetic enzymes involved in normal human development, play
a key role in tumor cell plasticity and in creating an altered, de-differentiated,
and more proliferative cellular state in certain tumors.;
Molecule name : AUTX 703; AUTX-703;
Origin ID : C215445;
concept_is_in_subset
- has_target
