KAT2A/KAT2B Degrader AUTX-703

**Semantic type:** Pharmacologic Substance

**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.

**Synonyms:** - AUTX 703 - AUTX-703 - AUTX703 - KAT2A/B Protein Degrader AUTX-703 - KAT2A/KAT2B Protein Degrader AUTX-703