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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Epigenetic Reader Domain

Long Noncoding RNA MALAT1 Promotes Laryngocarcinoma Development by Targeting miR-708-5p/BRD4 Axis to Regulate YAP1-Mediated Epithelial-Mesenchymal Transition

48 views | May 25 2022

Xiaoqin Wu et al. thought that targeting MALAT1/miR-708-5p/BRD4 axis might provide a promising therapeutic strategy for laryngocarcinoma. [Read the Full Post]

Degradation and inhibition of epigenetic regulatory protein BRD4 exacerbate Alzheimer's disease-related neuropathology in cell models

61 views | Apr 12 2022

Siyi Zhang et al. not only showed that BRD4 was a novel epigenetic component that regulated BACE1 and Aβ levels, but also provided novel and translational insighted into the targeting of BRD4 for potential clinical applications. [Read the Full Post]

Inhibition of Bromodomain and Extra Terminal (BET) Domain Activity Modulates the IL-23R/IL-17 Axis and Suppresses Acute Graft- Versus-Host Disease

47 views | Apr 08 2022

Katiri J Snyder et al. identified a role for BET proteins in regulating the IL-23R/STAT3/IL-17 pathway. [Read the Full Post]

The p300 inhibitor A-485 exerts antitumor activity in growth hormone pituitary adenoma

78 views | Apr 07 2022

Chenxing Ji et al. found that inhibition of HAT p300 by its selective inhibitor A-485 was a promising therapy for GHPA. [Read the Full Post]

AZD5153 reverses palbociclib resistance in ovarian cancer by inhibiting cell cycle-related proteins and the MAPK/PI3K-AKT pathway

140 views | Mar 22 2022

Chen Liu et al. revealed that it was anticipated that this class of drugs, including AZD5153, which inhibited the cell cycle-related protein and MAPK/PI3K-AKT pathway, would exhibit synergistic effects with palbociclib in OC. [Read the Full Post]

XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer

95 views | Feb 20 2022

Daniel R Principe et al. suggested that XP-524 might benefit PDAC patients and warrant further exploration, particularly in combination with immune checkpoint inhibition. [Read the Full Post]

High-Throughput Screening for CEBPD-Modulating Compounds in THP-1-Derived Reporter Macrophages Identifies Anti-Inflammatory HDAC and BET Inhibitors

100 views | Dec 16 2021

Tatjana Ullmann et al. found that I-BET151 and HDAC inhibitors simultaneously upregulated the mRNA expression of pro-inflammatory IL-1ß. [Read the Full Post]

Anticancer Effects of I-BET151, an Inhibitor of Bromodomain and Extra-Terminal Domain Proteins

114 views | Dec 15 2021

Jiacheng Lai et al. showed that the research on the anticancer mechanism of I-BET151 would lead to new treatment strategies for clinical cancer. [Read the Full Post]

Biological Effects of BET Inhibition by OTX015 (MK-8628) and JQ1 in NPM1-Mutated (NPM1c) Acute Myeloid Leukemia (AML)

247 views | Dec 13 2021

Hanane Djamai et al. found that BETi, similar to ATO + ATRA, induced differentiation and apoptosis which was TP53 independent in the NPM1c cell line OCI-AML3 and primary cells. [Read the Full Post]

C646 Protects Against DSS-Induced Colitis Model by Targeting NLRP3 Inflammasome

355 views | Oct 20 2021

Xueming Xu et al. demonstrated the ability of C646 to suppress the NLRP3 inflammasome activity and its potential application in the treatment of inflammatory bowel disease. [Read the Full Post]