sAJM-589 is a Myc Inhibitor by Disrupts the Myc-Max Heterodimer
The proto-oncogene Myc belongs to the basic helix-loop-helix leucine zipper (B-HLH-LZ) transcription factor family. It plays a key role in cellular proliferation, differentiation, and apoptosis. Myc expression is normally under tight control. Its expression is transient and responsive to mitogen stimulation. Indeed, in more than 70% of human malignancies,...
GNA002, a Specific EZH2 Inhibitor, Suppresses H3K27Me3 and Effectively Reactivates PRC2-Silenced Tumor Suppressor Genes
Enhancer of zeste homolog 2 (EZH2) is a critical oncogene. Meanwhile, it is a promising drug target in human malignant tumors. H3K27Me3 functions as a suppressive marker of gene transcription. Previous studies have revealed that EZH2 are largely due to its ability to suppress the expression of a cohort...
GSK2643943A is a Novel DUB Inhibitor
The ubiquitin proteasome system participates in a variety of biological functions including cell cycle progression, intracellular signaling and protein degradation. Therefore, it is not surprising to find many misregulation of this system in cancer. Fortunately, the first-generation deubiquitylating enzyme (DUB) inhibitors are now approaching clinical trials. For instance, the...
BI8622 is a HUWE1 Ubiquitin Ligase Inhibitor for Colorectal Cancer
HUWE1 is a colonic tumor suppressor. Especially, HUWE1 is a critical colonic tumour suppressor gene that prevents MYC signalling, DNA damage accumulation and tumor initiation.HUWE1 is a pleiotropic E3 ubiquitin ligase that modulates the function of several proteins involved in oncogenesis and DNA damage response including MYC, MYCN, MCL1...