Targeted protein degradation has emerged as a new paradigm to manipulate cellular
proteostasis. Proteolysis-targeting chimeras (PROTACs) are bifunctional small molecules …

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

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 …

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

Ubiquitination is initiated by transfer of ubiquitin (Ub) from a ubiquitin-activating enzyme (E1)
to a ubiquitin-conjugating enzyme (E2), producing a covalently linked intermediate (E2–Ub) …

Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

Targeted protein degradation has arisen as a powerful therapeutic modality for degrading
disease targets. While proteolysis-targeting chimera (PROTAC) design is more modular, the …

Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …

Bivalent chemical degraders provide a catalytic route to selectively degrade disease-
associated proteins. By linking target-specific ligands with E3 ubiquitin ligase recruiting …

Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs),
function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary …