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Scientific Data - PROTAC-PatentDB: A PROTAC Patent Compound Dataset

Momentum is building for PROTAC treatments that eliminate disease-causing proteins, including those responsible for difficult-to-treat childhood cancers.

Momentum is building for PROTAC treatments that eliminate disease-causing proteins, including those responsible for difficult-to-treat childhood cancers.

The authors show that DCAF1, a substrate receptor of CUL4 and EDVP E3 ligases, can be recruited by PROTACs to degrade the cancer drug target, WDR5. They also report the crystal structures of PROTAC te...

STAT3 is an attractive therapeutic target for cancer and other human diseases. We have previously reported the discovery of potent, selective, and efficacious PROTAC STAT3 degraders SD-36 and SD-91. I...

Pharmaceutical companies are investing in therapies that target proteins for degradation, with trials ongoing for cancer, autoimmune diseases and neurological disorders.

Scientific Reports - PRosettaC outperforms AlphaFold3 for modeling PROTAC ternary complexes

Pharmaceutical companies are investing in therapies that target proteins for degradation, with trials ongoing for cancer, autoimmune diseases and neurological disorders.

Proteolysis Targeting Chimeras (PROTACs) are bifunctional molecules that induce ubiquitination and degradation of a target protein via recruitment to an E3 ligase. The linker influences many steps of ...

Momentum is building for PROTAC treatments that eliminate disease-causing proteins, including those responsible for difficult-to-treat childhood cancers.

Ultra high-throughput chemistry carried out in 1536-well plates is increasingly utilized for reaction optimization protocols and direct-to-biology (D2B) platforms, where nanomolar quantities of the fi...

The biotech company Arvinas was originally founded based on pioneering research from Yale chemist Craig Crews into PROTAC protein degraders.

The tedious synthesis and limited throughput biological evaluation remain a great challenge for discovering new proteolysis targeting chimera (PROTAC). To rapidly identify potential PROTAC lead compounds, we report a platform named Auto-RapTAC. Based on the modular characteristic of the PROTAC molecule, a streamlined workflow that integrates lab automation with “click chemistry” joint building-block libraries was constructed. This facilitates the autonomous generation of a variety of PROTACs, each with distinct linkers and E3 ligase ligands, all stored in biocompatible solutions. The ready-for-screening (R4S) approach, when paired with fluorescence-based assays, enables the efficient assessment of the PROTAC degradation activity in a high-throughput manner. To further test the capability of the platform, we identify six new PROTACs that target CDK2, CDK12, and BCL6 within a mere 8-day time frame for each target. In all, this platform could find broad application not only in discovering new PROTACs but also in the rapid development of novel heterobifunctional modalities.

Proteins lacking defined ligandable pockets remain challenging drug targets. Here, we develop a molecular glue-based PROTAC (MGPROTACs) approach that chemically conjugates a molecular glue stabilizer ...

Proximity-dependent biotinylation coupled with ubiquitin remnant enrichment identifies PROTAC-induced ubiquitylation sites and E3 ligase substrates.

COMPASS enables structure-based screening of PROTAC linker libraries by jointly evaluating ternary complex formation and ubiquitination competence. The pipeline accurately recovers experimentally obs...