Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous BET inhibitors, and show that it suppresses BRD4 and targets tumour associated …

These results show that BRD4 inhibition affects both cancer cells and their microenvironment and support further development of BRD4 inhibitors for treatment of solid tumors in the...

Feb 1, 2021 · Treatment with BRD4 inhibitors has multiple effects on tumor cells as well as their microenvironments by affecting PD-L1 expression and VEGF secretion and by blocking the …

Inhibitors of the BET family proteins are limited by their potency and oral bio-availability. Here, the authors report a new BET inhibitor, NHWD-870, with improved potency compared to previous …

Targeted inhibition of BRD4 using BET inhibitors blocks the expression of SASP factors and induces senescence in cancer cells, resulting in enhanced recognition and phagocytosis of …

Dec 22, 2023 · Small molecule compound BRD4 BD1 and BD2 bromodomain inhibitors block BRD4 binding to super-enhancers, suppress oncogene transcription and expression, reduce …

D4, CSF1, and TAMs were negatively associated with patient outcome. To investigate whether BRD4 activation in ovarian cancer cells correlates with CSF1 expression, the number of TAMs …

Apr 14, 2020 · Here we report the development and characterization of a potent BRD4 inhibitor NHWD-870. We show that NHWD-870 depletes phosphorylated BRD4 and c-MYC, and …

Here we report the discovery and characterization of NHWD-870, a BET inhibitor that is more potent than three major clinical stage BET inhibitors BMS-986158, OTX-015, and GSK …

This review provides a comprehensive summary of the functions and underlying mechanisms of BRD4 in oncogenesis. It further highlights the recent progress in the development of BRD4 …