Tag: Ubiquitination

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,...

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,...