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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

LSD1

Lysin (K)-specific demethylase 1 inhibition enhances proteasome inhibitor response and overcomes drug resistance in multiple myeloma

97 views | Nov 20 2023

The study demonstrates that inhibiting lysine-specific demethylase 1 (LSD1) synergizes with proteasome inhibitors, such as carfilzomib, overcoming drug resistance in multiple myeloma and other B-cell malignancies, offering a promising therapeutic strategy. [Read the Full Post]

Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection

149 views | Nov 16 2023

ML324, a specific inhibitor of JMJD2 histone demethylase, has demonstrated promising potential as a treatment against CyHV-3 infection in koi fish, effectively inhibiting viral replication both in vitro and in vivo. [Read the Full Post]

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

0 views | Jun 29 2023

This review summarizes the structure and functions of LSD1, its role in cancer and non-cancer diseases, and the potential of covalent and non-covalent LSD1 inhibitors, including those in clinical trials, as potent and selective anticancer agents. [Read the Full Post]

The pattern of histone H3 epigenetic posttranslational modifications is regulated by the VRK1 chromatin kinase

208 views | Jun 29 2023

The chromatin kinase VRK1 regulates the epigenetic patterns of histone H3 acetylation and methylation, particularly at lysines 4, 9, and 27, and is essential for coordinating chromatin organization and nuclear functions. [Read the Full Post]

JAK/BCL2 inhibition acts synergistically with LSD1 inhibitors to selectively target ETP-ALL

0 views | Jun 22 2023

The combination of a LSD1 inhibitor with a JAK/STAT pathway inhibitor or a BCL2 inhibitor reverses resistance and efficiently inhibits the growth of ETP-ALL cells, suggesting a potential novel combination therapy for ETP-ALL patients. [Read the Full Post]

Comparison of pharmacological inhibitors of lysine-specific demethylase 1 in glioblastoma stem cells reveals inhibitor-specific efficacy profiles

126 views | Jun 16 2023

This study demonstrates the cytotoxic effects of LSD1 inhibitors in patient-derived glioblastoma models and identifies potential resistance-associated genes, providing valuable insights for the development of future combination therapies. [Read the Full Post]

Recent advances of LSD1/KDM1A inhibitors for disease therapy

69 views | May 13 2023

The review highlights recent advances and challenges in LSD1-targeted drug discovery for the treatment of various diseases, including hematologic malignancies. [Read the Full Post]

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

86 views | May 13 2023

LSD1 is an epigenetic enzyme overexpressed in many types of cancers, and its inhibitors have emerged as a promising therapeutic strategy for selectively targeting cancer cells while sparing normal cells. [Read the Full Post]

JAK/BCL2 inhibition acts synergistically with LSD1 inhibitors to selectively target ETP-ALL

206 views | Nov 28 2022

Aissa Benyoucef et al. revealed the novel involvement of ZEB2/LSD1 complexes in repressing the intrinsic apoptosis pathway by inhibiting the expression of several pro-apoptotic proteins such as BIM (BCL2L11) as a major driver for ETP-ALL survival. [Read the Full Post]

Comprehensive in Vitro Characterization of the LSD1 Small Molecule Inhibitor Class in Oncology

323 views | Jan 05 2022

Natalia Sacilotto et al. highlighted significant differences in potency and selectivity among the clinical compounds with iadademstat being the most potent and revealed that most of the tool compounds had very low activity and selectivity. [Read the Full Post]