EZH1/2

Novel small molecule inhibitors of the transcription factor ETS-1 and their antitumor activity against hepatocellular carcinoma

19 views | Nov 08 2023

This study identified four novel small molecule inhibitors of the transcription factor ETS-1, demonstrating their potential to suppress HCC cell proliferation and invasion, offering safer and more effective therapeutic strategies for hepatocellular carcinoma. [Read the Full Post]

Dual inhibition of EZH1/2 induces cell cycle arrest of B cell acute lymphoblastic leukemia cells through upregulation of CDKN1C and TP53INP1

93 views | Sep 09 2023

The study demonstrates that the EZH1/2 dual inhibitor DS-3201 (valemetostat) shows significant antitumor effects against B cell acute lymphoblastic leukemia (B-ALL) by inhibiting cell growth, inducing cell cycle arrest and apoptosis, and upregulating CDKN1C and TP53INP1 expression, offering a potential treatment option for B-ALL. [Read the Full Post]

EZH2 presents a therapeutic target for neuroendocrine tumors of the small intestine

39 views | Jul 30 2023

The study suggests that targeting the EZH2 histone methyltransferase with inhibitors like CPI-1205 and utilizing metformin may hold promise as potential therapeutic options for patients with small intestinal neuroendocrine tumors (SI-NETs). [Read the Full Post]

Resistance to Pyrrolobenzodiazepine Dimers Is Associated with SLFN11 Downregulation and Can Be Reversed through Inhibition of ATR

66 views | Jun 30 2023

This study identified downregulation of Schlafen family member 11 (SLFN11) and its association with PBD resistance in cancer cells, highlighting the potential of targeting SLFN11 and combining ATR inhibitors to overcome resistance to PBD-conjugated ADCs. [Read the Full Post]

The role of EZH2 as a potential therapeutic target in retinoblastoma

94 views | Jun 30 2023

The study reveals that the high expression of EZH2 in retinoblastoma tissues is associated with poor overall survival, and inhibiting EZH2 with UNC1999 shows promising results in suppressing RB cell proliferation, metastasis, and tumor glycolysis, making it a potential target for anti-RB treatment. [Read the Full Post]

Alteration of the tumor microenvironment by pharmacological inhibition of EZH2 in hepatocellular carcinoma

31 views | May 26 2023

The study found that EZH2 inhibition with UNC1999 impaired HCC tumor growth but also altered the TME by decreasing interferon-γ+ CD8+ T cells and regulatory T cells and increasing myeloid-derived suppressor cells, and combination therapy with agents that reduce MDSCs may represent a potential novel therapeutic strategy for HCC. [Read the Full Post]

Dual inhibition of EZH2 and G9A/GLP histone methyltransferases by HKMTI-1-005 promotes differentiation of acute myeloid leukemia cells

98 views | May 26 2023

The study investigates the potential of using an EZH2 inhibitor, HKMTI-1-005, to improve the response of non-APL AML cells to ATRA-based therapy by inducing differentiation and upregulating the expression of differentiation pathway genes. [Read the Full Post]

A patent review of EZH2 inhibitors from 2017 and beyond

76 views | May 23 2023

EZH2 inhibitors are a promising class of drugs for the treatment of various diseases, particularly cancers, but further research is needed to optimize their efficacy and safety. [Read the Full Post]

The Effect of Direct and Indirect EZH2 Inhibition in Rhabdomyosarcoma Cell Lines

49 views | May 17 2023

The study found that direct and indirect inhibition of EZH2 affect cellular functions differently, and the alveolar cell line RH30 is more sensitive to epigenetic intervention than the embryonal cell line RD, suggesting EZH2 as a potential therapeutic target in RMS. [Read the Full Post]

HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia

0 views | Nov 17 2022

Zhengchang He et al. thought that HO-1 could influence MDS resistance and progression to AML. [Read the Full Post]