p300 HAT inhibitor

p300 HAT inhibitors are a class of small molecules designed to inhibit the histone acetyltransferase (HAT) activity of the p300 (EP300) protein and its closely related paralog, CBP (CREB-binding protein). These proteins function as transcriptional co-activators that modify chromatin structure by acetylating lysine residues on histones (notably H3K18 and H3K27) and various non-histone proteins, such as p53, GATA4, and NF-κB. By blocking this enzymatic activity, p300 HAT inhibitors can downregulate the expression of key oncogenic drivers like c-Myc and HIF-1α. This class of epigenetic modulators is being investigated for the treatment of various cancers, including multiple myeloma, prostate cancer, and glioblastoma, as well as for their potential to reverse chemoresistance and treat cardiovascular conditions like hypertension-induced cardiac hypertrophy.

Other names

p300 HAT inhibitorp-300 HAT inhibitorp 300 HAT inhibitorp300 inhibitorsp-300 inhibitorsp 300 inhibitorsEP300 inhibitorsEP-300 inhibitorsEP 300 inhibitorsp300/CBP HAT inhibitorsHistone acetyltransferase p300 inhibitors