Controlled perturbation of protein activity is essential to study protein function in cells and
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …

Molecular glues (MGs) are monovalent small molecules that induce an interaction between
proteins (native or non-native partners) by altering the protein–protein interaction (PPI) …

Small-molecule antagonists disable discrete biochemical properties of protein targets. For
multi-domain protein targets, the pharmacologic consequence of drug action is limited by …

With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …

Highlights•E3 ligases recruit substrates for proteasomal degradation by recognition of
degrons.•Crystal structures reveal the structural basis and mechanism of degron …

Targeted protein degradation (TPD) uses small molecules to recruit E3 ubiquitin ligases into
the proximity of proteins of interest, inducing ubiquitination-dependent degradation. A major …

Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …

The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …