TRRAP Inhibitors

The indirect inhibitors of TRRAP (Transformation/Transcription Domain-Associated Protein) primarily consist of compounds that influence chromatin remodeling and epigenetic regulation. TRRAP is a crucial cofactor in various histone acetyltransferase complexes, playing a significant role in modulating gene expression. Since direct chemical inhibitors for TRRAP are not well-established, the focus shifts to compounds that modulate the activity of histone acetyltransferases (HATs), histone deacetylases (HDACs), and other components of the chromatin remodeling machinery. Compounds like C646, Anacardic Acid, and Garcinol target HATs such as p300 and CBP. By inhibiting these enzymes, they can indirectly affect TRRAP's function in transcriptional regulation, as TRRAP is involved in recruiting these HATs to specific genomic loci. Inhibition of HATs leads to reduced histone acetylation, subsequently affecting gene expression patterns where TRRAP is involved.

HDAC inhibitors like Vorinostat, Trichostatin A, MGCD0103, Panobinostat, and Entinostat work by preventing the removal of acetyl groups from histone tails, leading to an open chromatin structure and potentially increased gene expression. These changes in the chromatin landscape can indirectly influence the activity and functional outcomes of TRRAP-associated complexes. BIX-01294 and 5-Azacytidine, targeting histone methyltransferase and DNA methyltransferase, respectively, represent another strategy to indirectly influence TRRAP activity. By altering methylation patterns on histones or DNA, these compounds can modify the overall epigenetic landscape, potentially impacting the gene regulatory functions where TRRAP is involved.