GNE-987

BRD4 inhibitor

Also Known As:

GNE987; N-(11-((7-(3,5-difluoropyridin-2-yl)-2-methyl-10-((methylsulfonyl)methyl)-3-oxo-3,4,6,7-tetrahydro-2H-2,4,7-triazadibenzo(cd,f)azulene-9-carbonyl)amino)undecanoyl)-3-methyl-L-valyl-(4R)-4-hydroxy-N-((4-(4-methyl-1,3-thiazol-5-yl)phenyl)methyl)-L-prol

Networked: 3 relevant articles (0 outcomes, 1 trials/studies)

Bio-Agent Context: Research Results

Organic Chemicals: 133
- Amides: 2428
  - GNE-987: 3

Experts

1.	Cao, Hai-Bo: 1 article (03/2022)
2.	Chen, Yan-Ling: 1 article (03/2022)
3.	Fang, Fang: 1 article (03/2022)
4.	Fei, Xiao-Dong: 1 article (03/2022)
5.	Feng, Chen-Xi: 1 article (03/2022)
6.	Jia, Si-Qi: 1 article (03/2022)
7.	Jiao, Wan-Yan: 1 article (03/2022)
8.	Li, Gen: 1 article (03/2022)
9.	Li, Xiao-Lu: 1 article (03/2022)
10.	Li, Zhi-Heng: 1 article (03/2022)

Related Diseases

1.	Neoplasms (Cancer) 03/18/2022 - "Consistent with in vitro results, GNE987 administration (0.25 mg/kg) markedly decreased the tumor size in the xenograft model, with less toxicity, and induced similar BRD4 protein degradation to that observed in vitro. " 03/18/2022 - "BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting super-enhancers in neuroblastoma." 01/01/2022 - "Recent studies have shown that as a novel BRD4 (bromodomain containing 4) PROTACs (proteolysis targeting chimeras) degrader, GNE-987 can slow down the growth of various tumors and increase apoptosis, with promising clinical prospects. " 12/01/2022 - "We evaluated the anti-tumor effect of GNE987 in vitro and in vivo by Western blot, CCK8, flow cytometry detection, clone formation, the size of xenografts, and Ki67 immunohistochemical staining, and combined ChIP-seq with RNA-seq techniques to find its anti-tumor mechanism. "
2.	Precursor Cell Lymphoblastic Leukemia-Lymphoma (Acute Lymphoblastic Leukemia) 01/01/2022 - "Based on analysis of RNA-seq and ChIP-seq analyses, GNE-987 could target multiple SE- (super-enhancer-) related genes, including LYL1 (lymphoblastic leukemia 1), to inhibit AML. "
3.	Acute Myeloid Leukemia (Acute Myelogenous Leukemia) 01/01/2022 - "BRD4 Inhibitor GNE-987 Exerts Anticancer Effects by Targeting Super-Enhancer-Related Gene LYL1 in Acute Myeloid Leukemia."
4.	Neuroblastoma 03/18/2022 - "BRD4 inhibitor GNE987 exerts anti-cancer effects by targeting super-enhancers in neuroblastoma."
5.	Leukemia 01/01/2022 - "In an AML xenograft model, GNE-987 significantly reduced the hepatosplenic infiltration of leukemia cells and increased the mouse survival time. "

Related Drugs and Biologics

1.	Proteolysis Targeting Chimera
2.	RNA (Ribonucleic Acid)