Proteolysis-targeting chimaeras (PROTACs) are molecules that combine a target-binding
warhead with an E3 ligase-recruiting moiety; by drawing the target protein into a ternary …

The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …

Targeted protein degradation (TPD) with proteolysis targeting chimeras (PROTACs),
heterobifunctional compounds consisting of protein targeting ligands linked to recruiters of …

Inducing biomolecular interactions with synthetic molecules to impact biological function is a
concept of enormous appeal. Recent years have seen a resurgence of interest in designing …

Natural products continue to be an unparalleled source of pharmacologically active lead
compounds because of their unprecedented structures and unique biological activities …

Ubiquitination is a key post-translational modification of proteins, affecting the regulation of
multiple cellular processes. Cells are equipped with over 600 ubiquitin orchestrators, called …

Targeting the “undruggable” proteome remains one of the big challenges in drug discovery.
Recent innovations in the field of targeted protein degradation and manipulation of the …

Targeted protein degradation offers several advantages over direct inhibition of protein
activity and is gaining increasing interest in chemical biology and drug discovery …

The key proteins involved in transcriptional regulation play convergent roles in cellular
homeostasis, and their dysfunction mediates aberrant gene expressions that underline the …

Targeted protein degradation (TPD) and proteolysis-targeting chimeras (PROTACs) have
arisen as powerful therapeutic modalities for degrading specific proteins in a proteasome …