Use of inhibitors in elucidating the mechanism of an enzyme

HDACs are tightly involved in cell cycle regulation, cell proliferation, and in the development of human diseases including cancer, cardiovascular and pulmonary diseases, and neurological diseases.The detection of activity and inhibition of HDACs is important in elucidating mechanisms of epigenetic regulation of gene activation and silencing, as well as benefiting cancer diagnostics and therapeutics.BRDs bind selectively to acetylated lysines, acting as “readers” of the histone code, and have recently been shown to regulate transcription activity; they also contain a druggable binding pocket.Proteins that contain BRD2 have been implicated in the development of a large variety of diseases and inhibitors that target BRDs of the BET (Bromodomains and extra-terminal), which inhibit BRD-mediated protein-protein interaction and have the potential to modulate multiple diseases including inflammation and cancer.

The comprehensive panel of enzymes in this system have important biological and therapeutic relevance.

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Continued development of these inhibitors, especially isoform-selective inhibitors, would further improve cancer treatment and lead to the possibility of successful cancer treatment drugs.

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