PROteolysis TArgeting Chimeras (PROTACs) are small molecules, that regulate protein function by degrading target proteins instead of inhibiting them. They are used as a novel therapeutic method against diseases driven by the expression of a disease-causing protein and have been proven to show better selectivity compared to classic inhibitors.
Structure
PROTACs molecules consist of three crucial parts. They include an “anchor” to bind to an E3 ubiquitin ligase, a “warhead” to bind to a protein of interest, and a linker, which connects them (you can find the scheme on the illustration below)
Mode of action
PROTACs are used to connect the protein of interest (POI) with E3 ubiquitin ligase. By bringing them together in space, the ubiquitination of the POI is induced. After complex dissociation, the labeled protein is successfully degraded by a proteasome.
Chemspace PROTACs collection contains 2 parts: anchors for E3 ligases and linkers.
Besides that, you can order a custom library based on the protein of interest in your research.
This will help every scientist to find their unique combinations to work with PROTACs with no intellectual property loss.
Linkers for PROTACs could be PEGs, Alkyl-Chain, and Alkyl/Ether. However, the most common linkers are PEG fragments as they increase the water-solubility of the molecules. Therefore, our PROTACs Linkers collection was prepared based on bifunctional building blocks including PEG fragments.
As for anchors, modifications of E3 ligase are capable to participate in protein-targeted degradation. Their ligands including bestatin, thalidomide, kb02, lenalidomide, pomalidomide were used as references for anchors design for our set.
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