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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

NSD

Prototropic forms of hydroxy derivatives of naphthoic acid within deep eutectic solvents

154 views | Jul 29 2023

The prototropic behavior of probes in deep eutectic solvents (DESs) is strongly influenced by the varying hydrogen-bonding capabilities of the DES constituents, as observed through the presence or absence of specific prototropic forms of the probes in different DES compositions. [Read the Full Post]

In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer

364 views | Jul 11 2023

This study utilized epigenomic profiling and a computational pipeline to identify potential therapeutic candidates and enhance stratification for ovarian cancer, with a focus on high-grade serous carcinoma. [Read the Full Post]

A Phase I Study of Pelabresib (CPI-0610), a Small-Molecule Inhibitor of BET Proteins, in Patients with Relapsed or Refractory Lymphoma

125 views | Jul 02 2023

The first-in-human phase I study of pelabresib demonstrated its safety, pharmacokinetics, pharmacodynamics, and preliminary clinical activity, establishing a maximum tolerated dose of 225 mg once daily and supporting its potential as a therapeutic agent for relapsed/refractory lymphomas. [Read the Full Post]

Pelabresib (CPI-0610): An Exciting Novel Drug for the Treatment of Myelofibrosis

181 views | Jul 02 2023

Pelabresib (CPI-0610), an investigational BET inhibitor, shows promising potential as a novel treatment approach for myelofibrosis, based on preclinical and clinical data demonstrating its ability to target key oncogenic signaling pathways and provide favorable responses in symptom control and disease-related parameters. [Read the Full Post]

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors

283 views | Jun 04 2023

The passage describes the discovery of a potent BET inhibitor called 1q (SJ1461) through a CLICK chemistry-based approach, which shows improved profiles compared to existing BET inhibitors and has promising potential for further development as a cancer therapy. [Read the Full Post]

Binding of the SARS-CoV-2 envelope E protein to human BRD4 is essential for infection

165 views | Nov 06 2022

Kendra R Vann et al. provided insight into molecular mechanisms that contributed to SARS-CoV-2 pathogenesis and shed light on a new strategy to block SARS-CoV-2 infection. [Read the Full Post]

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

505 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]

A comprehensive study of epigenetic alterations in hepatocellular carcinoma identifies potential therapeutic targets

0 views | Mar 23 2022

Juan Bayo et al. thought that the epigenetic alterations identified in HCC could be used to predict prognosis and to define a subgroup of high-risk patients that would potentially benefit from JmjC inhibitor therapy. [Read the Full Post]

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

482 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]

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

508 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]