A proteolysis targeting chimera (PROTAC) [2] is a molecule that can remove specific unwanted proteins. Rather than acting as a conventional enzyme inhibitor , a PROTAC works by inducing selective intracellular proteolysis .

Dec 22, 2022 · PROTACs are heterobifunctional molecules that degrade target proteins by hijacking the ubiquitin–proteasome system. Currently, about 20–25% of all protein targets are being studied, and most works focus on their enzymatic functions.

Jan 18, 2022 · With clinical proof-of-concept for PROTAC molecules against two well-established cancer targets provided in 2020, the field is poised to pursue targets that were previously considered...

Apr 4, 2022 · In recent years, PROteolysis TArgeting Chimeras (PROTAC) technology has emerged as one of the most promising approaches to remove specific disease-associated proteins by exploiting cells’ own...

Apr 2, 2024 · Proteolysis targeting chimeras (PROTAC) are an emerging precision medicine strategy, which targets key proteins for proteolytic degradation to ultimately induce cancer cell killing.

Oct 7, 2024 · Sometimes known as PROTAC protein degraders (PROTAC is an acronym of ‘proteolysis targeting chimera’ and has been trademarked by Arvinas), these new drugs are now entering late-stage clinical...

Nov 15, 2024 · Researchers are exploring how PRO teolysis TA rgeting C himeras (PROTACs) can potentially treat cancer, neurodegenerative diseases, and other difficult-to-treat conditions.

4 days ago · If a PROTAC candidate shows sufficient promise, it advances to human trials under regulatory oversight. Phase I trials focus on safety, dose escalation, and pharmacokinetics in a small cohort of patients, often those with advanced …

Jan 15, 2021 · Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3 ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug discovery paradigm which has been widely used as biological tools and medicinal molecules with the potential of clinical a …

By utilizing an event-driven MOA, the proteolysis-targeting chimeras (PROTACs) technology introduces a revolutionary tactic. Small-molecule-based heterobifunctional PROTACs hijack the ubiquitin–proteasome system to trigger the degradation of the target protein.