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GSK2820151 is an orally bioavailable small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, developed by GSK. It acts by inhibiting BET proteins, which are epigenetic readers involved in regulating gene expression through recognition of acetylated lysine residues on histone tails. By blocking these proteins, particularly BRD2, BRD3, and BRD4, GSK2820151 disrupts transcriptional programs that drive tumor growth and survival. The drug was investigated for its antineoplastic activity in advanced or recurrent solid tumors but development has been discontinued[1][2][3][4].
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