KAT6/KAT7

Class

small molecule

Notes

original target text: KAT6/KAT7 inhibitor

KAT6 (comprising KAT6A/MOZ and KAT6B/MORF) and KAT7 (HBO1) are enzymes belonging to the MYST family of lysine acetyltransferases. These enzymes add acetyl groups to specific lysine residues on histone proteins, particularly histone H3, a chemical modification that loosens chromatin structure and promotes the transcription of genes needed for cell division and self-renewal. Cancer cells frequently exploit this activity, either through direct amplification of the KAT6 gene or through dependence on the transcriptional programs these enzymes sustain, to maintain uncontrolled proliferation and evade normal growth-arrest signals such as cellular senescence. Small-molecule inhibitors of KAT6/KAT7 aim to block this acetyltransferase activity, reducing transcription of proliferation-associated genes and, in some contexts, reactivating senescence pathways that constrain tumor growth. Because KAT6 and KAT7 can have overlapping and partially redundant functions within chromatin-regulatory complexes, an agent that inhibits both may achieve a more complete disruption of the relevant transcriptional program than one targeting a single paralog. This mechanism is being explored primarily in oncology, particularly in cancers where these acetyltransferases or their associated chromatin complexes are amplified or otherwise implicated in sustaining malignant growth.