A5038371282- Ubiquitin and proteasome pathways
- Biochemical and Molecular Research
- Endoplasmic Reticulum Stress and Disease
- Protein Degradation and Inhibitors
- Click Chemistry and Applications
Vanderbilt University
2019-2020
The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to a tumorigenic state. Indeed, is overexpressed in up ∼50% human cancers considered highly validated anticancer target. Recently, we discovered that WD repeat-containing protein 5 (WDR5) binds critical cofactor required for the recruitment target genes reported first small molecule inhibitors WDR5–MYC interaction using structure-based design. These compounds display high binding affinity, but...
The treatment of tumors driven by overexpression or amplification MYC oncogenes remains a significant challenge in drug discovery. Here, we present new strategy toward the inhibition via disruption protein–protein interaction between and its chromatin cofactor WD Repeat-Containing Protein 5. Blocking association these proteins is hypothesized to disrupt localization chromatin, thus disrupting ability sustain tumorigenesis. Utilizing high-throughput screening campaign subsequent...