Vepdegestrant showed a benefit for patients with ER-positive, HER2-negative, ESR1-mutated breast cancer who had previously received endocrine-based therapy.

Vepdegestrant significantly improved outcomes for certain patients with ER-positive, HER2-negative advanced breast cancer ...

Using a cell-based BRET assay, we identified 12 PROTAC analogs that significantly enhanced Nef ubiquitylation, all of which were coupled to ligands for the Cereblon (CRBN) E3 ubiquitin ligase. Six of ...

“Our team’s research experimentally demonstrated anticancer synergy between two PROTACS using different E3 ligases to target the same oncogene ... we recognized with Dr. Busino early on, that the ...

The E3 ligase ligand links the PROTAC to an E3 ligase, an enzyme that facilitates the attachment of ubiquitin molecules to proteins. Once the PROTAC simultaneously binds to the POI and the E3 ...

Targeted Protein Degradation (TPD) leverages this principle through Proteolysis Targeting Chimera (PROTAC®) technology, which selectively degrades pathological proteins by linking them to E3 ubiquitin ...

Furthermore, the ability to diversify E3 ligase ligands offers researchers the flexibility to design PROTACs tailored to specific cancer types, enhancing the specificity and potency of treatments. The ...

Therefore, in the next stage the project will focus on assessing if the selected E3 ligase is able to degrade different targets following recruitment with a PROTAC. The experiments will require ...

Upon introduction to the cells, PROTACs capture the activity of the E3 ubiquitin ligases for ubiquitination of the targeted protein, leading to its subsequent degradation by the proteasome. The main ...