Fibroblast growth factor receptor 2 (FGFR2) is a transmembrane tyrosine kinase that regulates signaling pathways controlling cell survival and proliferation. Dysregulation of FGFR2, through amplification or activating mutations, contributes to tumor development, making it an attractive target for therapeutic intervention in oncology.
Researchers from Fudan University reported the development of CZL-077, a p300/CBP bromodomain inhibitor. p300 and CREB-binding protein (CBP) are closely related histone acetyltransferases that play central roles in regulating gene expression. Dysregulation of these proteins has been implicated in tumorigenesis and the development of therapy resistance.
Triple-negative breast cancer (TNBC) cells depend on the transcriptional kinases CDK12 and CDK13 to maintain DNA damage response gene expression and manage replication stress. Due to their functional overlap, inhibition of a single kinase may permit compensatory activity.
