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Epigenetic Reader Domain

CBP Bromodomain Inhibition Rescues Mice From Lethal Sepsis Through Blocking HMGB1-Mediated Inflammatory Responses

1 views | Mar 02 2021

Xiaowen Bi et al. suggested that CBP bromodomain could serve as a candidate therapeutic target for the treatment of lethal sepsis via inhibiting LPS-induced expression and release of HMGB1 and suppressing the pro-inflammatory activity of HMGB1. [Read the Full Post]

Pan- and Isoform-specific Inhibition of the Bromodomain and Extra-terminal Proteins and Evaluation of Synergistic Potential With Entospletinib in Canine Lymphoma

11 views | Dec 27 2020

Weibo Kong et al. showed that Entospletinib did not enhance the inhibitory effects of the pan- or isoform-specific BET. [Read the Full Post]

Small molecular compounds efficiently convert human fibroblasts directly into neurons

0 views | Dec 26 2020

Jijuan Yang et al. found that a novel combination of existing small molecular compounds that efficiently reprogramed human fibroblasts into neurons. [Read the Full Post]

Targeted therapy of TERT-rearranged neuroblastoma with BET bromodomain inhibitor and proteasome inhibitor combination therapy

12 views | Dec 24 2020

Jingwei Chen et al. showed that OTX015 and carfilzomib combination therapy was likely to be translated into the first clinical trial of a targeted therapy in TERT-rearranged neuroblastoma patients. [Read the Full Post]

Piceatannol reduces resistance to statins in hypercholesterolemia by reducing PCSK9 expression through p300 acetyltransferase inhibition

28 views | Oct 25 2020

Hyo-Jin Kim et al. indicated that PT was a new nutraceutical candidate to reduce the statin resistance and tolerance that occured in patients with hypercholesterolemia. [Read the Full Post]

Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors

27 views | Sep 29 2020

Qifei Li et al. supported that this novel compound 13f provided a perspective for developing effective BRD4 inhibitors. [Read the Full Post]

Combined treatment with CBP and BET inhibitors reverses inadvertent activation of detrimental super enhancer programs in DIPG cells

54 views | Aug 30 2020

Maria Wiese et al. found that combinatorial treatment with CBP and BET inhibitors was highly efficient in H3K27M-mutant DIPG due to reversal of inadvertent activation of detrimental SE programs in comparison with monotherapy. [Read the Full Post]

Antiviral activity of PLK1-targeting siRNA delivered by lipid nanoparticles in HBV-infected hepatocytes

83 views | Aug 10 2020

Adrien Foca et al. emphasized that a specific PLK1 inhibition could help in achieving an improved HBsAg loss in CHB patients, likely in combination with other HBsAg-targeting strategies. [Read the Full Post]

Small Molecule JQ1 Promotes Prostate Cancer Invasion via BET-independent Inactivation of FOXA1

141 views | May 31 2020

Leiming Wang et al. indicated that JQ1 has an unexpected effect of promoting invasion in prostate cancer. [Read the Full Post]

Targeting Bromodomain and Extra-Terminal (BET) Family Proteins in Castration-Resistant Prostate Cancer (CRPC

133 views | Apr 15 2020

Jonathan Welti et al. showed that BETi merit clinical evaluation as inhibitors of AR splicing and function, with trials demonstrating their blockade in proof-of-mechanism pharmacodynamic studies. [Read the Full Post]