Targeting Chromatin Complexes in Myeloid Malignancies and Beyond: From Basic Mechanisms to Clinical Innovation.

摘要: The aberrant function of chromatin regulatory networks (epigenetics) is a hallmark cancer promoting oncogenic gene expression. A growing body evidence suggests that the disruption specific chromatin-associated protein complexes has therapeutic potential in malignant conditions, particularly those are driven by modifiers. Of note, number enzymatic inhibitors block catalytic histone modifying enzymes have been established and entered clinical trials. Unfortunately, many these molecules do not potent single-agent activity. One explanation for this phenomenon fact drugs profoundly disrupt integrity network multiprotein on chromatin. Recent advances drug development led to establishment novel protein-protein interactions as well targeted degraders may provide inroads longstanding effort physically In review, we summarize some current concepts role epigenetic modifiers states with focus myeloid malignancies recent early-phase