1.Development of hedgehog pathway inhibitors by epigenetically targeting GLI through BET bromodomain for the treatment of medulloblastoma.
Xiaohua LIU ; Yu ZHANG ; Yalei LI ; Juan WANG ; Huaqian DING ; Wenjing HUANG ; Chunyong DING ; Hongchun LIU ; Wenfu TAN ; Ao ZHANG
Acta Pharmaceutica Sinica B 2021;11(2):488-504
Medulloblastoma (MB) is a common yet highly heterogeneous childhood malignant brain tumor, however, clinically effective molecular targeted therapy is lacking. Modulation of hedgehog (HH) signaling by epigenetically targeting the transcriptional factors GLI through bromodomain-containing protein 4 (BRD4) has recently spurred new interest as potential treatment of HH-driven MB. Through screening of current clinical BRD4 inhibitors for their inhibitory potency against glioma-associated oncogene homolog (GLI) protein, the BRD4 inhibitor
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