Repurposing E3 ubiquitin ligases for targeted protein degradation via customized molecular
glues or proteolysis-targeting chimeras (PROTACs) is an increasingly important therapeutic …

Inducing macromolecular interactions with small molecules to activate cellular signaling is a
challenging goal. PROTACs (proteolysis-targeting chimeras) are bifunctional molecules that …

Protein misfolding is an emerging field that crosses multiple therapeutic areas and causes
many serious diseases. As the biological pathways of protein misfolding become more …

Conspectus One of the biggest bottlenecks in modern drug discovery efforts is in tackling the
undruggable proteome. Currently, over 85% of the proteome is still considered undruggable …

Targeted protein degradation is a drug modality represented by compounds that recruit a
target to an E3 ubiquitin ligase to promote target ubiquitination and proteasomal …

Targeted protein degradation (TPD) has emerged as a powerful tool in drug discovery for
the perturbation of protein levels using heterobifunctional small molecules. E3 ligase …

Heterobifunctional proteolysis-targeting chimeric compounds leverage the activity of E3
ligases to induce degradation of target oncoproteins and exhibit potent preclinical antitumor …

Targeted protein degradation is a promising strategy for drug design and functional
assessment. Several small molecule approaches have been developed that localize target …

Protein misfolding is involved in a large number of diseases, among which cystic fibrosis.
Complex intra-and inter-domain folding defects associated with mutations in the cystic …

E3 ligases are typically classified by hallmark domains such as RING and RBR, which are
thought to specify unique catalytic mechanisms of ubiquitin transfer to recruited substrates …