KDM (lysine demethylase)阻害剤

Histone lysine demethylases (KDMs) are a group of enzymes that play a pivotal role in epigenetic regulation by removing methyl groups from lysine residues on histone proteins. This demethylation process is crucial for the modulation of chromatin structure, which in turn regulates gene transcription. KDMs are involved in various cellular processes, including cell differentiation, proliferation, and DNA repair, by influencing the expression of genes associated with these pathways. These enzymes are categorized into two main families based on their mechanism of action: the LSD (Lysine Specific Demethylase) family, particularly LSD1, and the Jumonji C-domain-containing family, which includes multiple members. Dysregulation of KDM activity is implicated in several diseases, including cancer, neurological disorders, and developmental abnormalities, as it can lead to aberrant gene expression patterns. KDMs function within a complex network of histone modifications and interact with other epigenetic regulators, highlighting their importance in the broader context of chromatin dynamics and gene regulation.

Targeting KDM histone lysine demethylases with small molecules for disruption or inhibition offers a powerful tool for understanding their biological functions and the consequences of their dysregulation. By selectively inhibiting specific KDMs, researchers can observe changes in histone methylation patterns and subsequent effects on gene expression. This approach allows for the dissection of the roles of individual KDMs in various cellular processes and their contribution to the maintenance of epigenetic landscapes. Inhibiting KDMs can shed light on the mechanistic pathways involved in diseases where these enzymes are dysregulated, providing insights into potential targets.