Identification of genes that are modulated by BET inhibitors in cancer cells to identify robust pharmacodynamic marker for monitoring target engagement of BET family bromodomain inhibitors in tumors and surrogate tissue

Competitive inhibitors of acetyl-lysine binding to the bromodomains of the BET (bromodomain and extra terminal) family are being developed for the treatment of solid and heme malignancies. BET family member BRD4 function at enhancers/super-enhancers has been shown to sustain signal-dependent or pathogenic gene expression programs.

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Lin X, Huang X, Uziel T, Hessler P, Albert DH, Roberts-Rapp LA, McDaniel KF, Kati WM, Shen Y