Discovery of a small-molecule bromodomain-containing protein 4 (BRD4) inhibitor that induces AMP-activated protein kinase-modulated autophagy-associated cell …
L Ouyang, L Zhang, J Liu, L Fu, D Yao… - Journal of medicinal …, 2017 - ACS Publications
… (29) Thus, induction of ACD is a possible strategy to … As mentioned above, we identified the
BRD4-AMPK interaction, … to design a small-molecule inhibitor of BRD4 that induces BRD4-…
BRD4-AMPK interaction, … to design a small-molecule inhibitor of BRD4 that induces BRD4-…
Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening
… be useful for other design approaches and scaffold hopping, and we report novel inhibitors
of BRD4 that have the potential to be developed into significantly more potent compounds. …
of BRD4 that have the potential to be developed into significantly more potent compounds. …
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular …
F Jiang, Q Wei, H Li, H Li, Y Cui, Y Ma, H Chen… - Bioorganic & medicinal …, 2020 - Elsevier
… Bromodomain-containing proteins contain domains that specifically recognize histone
acetylation, named “reader”. Among them, the bromodomain and extra-terminal domain (BET) …
acetylation, named “reader”. Among them, the bromodomain and extra-terminal domain (BET) …
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery
D Liang, Y Yu, Z Ma - European journal of medicinal chemistry, 2020 - Elsevier
… many small-molecule BRD4 inhibitors have been discovered… induction. These indicate that
PROTAC is a more efficient strategy for targeting BRD4 than current small molecule inhibitors…
PROTAC is a more efficient strategy for targeting BRD4 than current small molecule inhibitors…
Selective small molecule induced degradation of the BET bromodomain protein BRD4
… Our discovery opens up new opportunities to elucidate the cellular phenotypes … to induce
selective intracellular degradation of their respective target bromodomain-containing proteins. …
selective intracellular degradation of their respective target bromodomain-containing proteins. …
Dual-target inhibitors of bromodomain-containing protein 4 (BRD4) in cancer therapy: Current situation and future directions
W Jin, H Tan, J Wu, G He, B Liu - Drug discovery today, 2022 - Elsevier
… Bromodomain-containing protein 4 (BRD4) is emerging as a therapeutic target that acts
synergistically with other targets of small-molecule … conjugate, can induce BRD4 degradation in …
synergistically with other targets of small-molecule … conjugate, can induce BRD4 degradation in …
[HTML][HTML] Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1
M Jung, M Philpott, S Müller, J Schulze… - Journal of biological …, 2014 - ASBMB
… Bromodomain protein 4 (BRD4) is the best studied member of the BET family. It is a nuclear
protein that binds to acetylated histone 3 (H3) and histone 4 (H4) tails and plays an essential …
protein that binds to acetylated histone 3 (H3) and histone 4 (H4) tails and plays an essential …
Drug discovery targeting bromodomain-containing protein 4
… , the number of small-molecule BET inhibitors has expanded … BRD4 inhibitors can not
only abrogate cytokine-induced … carbon tetrachloride-induced fibrosis in mouse models. (78) …
only abrogate cytokine-induced … carbon tetrachloride-induced fibrosis in mouse models. (78) …
Discovery and characterization of small molecule inhibitors of the BET family bromodomains
C Chung, H Coste, JH White, O Mirguet… - Journal of medicinal …, 2011 - ACS Publications
… of many bromodomain containing proteins has advanced … bromodomains (Brd2, Brd3, and
Brd4). By using a combination … 1b), which shows potent induction of the ApoA1 reporter gene …
Brd4). By using a combination … 1b), which shows potent induction of the ApoA1 reporter gene …
An overview on small molecule inhibitors of BRD4
W Huang, X Zheng, Y Yang, X Wang… - Mini Reviews in …, 2016 - ingentaconnect.com
… are a total of 61 different bromodomain-containing proteins [3], … to discover the BRD4 inhibitors
by Chung [32]. By analysing … is a positive regulatory component of PTEFb and stimulates …
by Chung [32]. By analysing … is a positive regulatory component of PTEFb and stimulates …