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Building Blocks for Synthesis of Proteolysis Targeting Compounds

In recent years, research in medicinal chemistry has increasingly investigated the use of the ubiquitin-proteasome system (UPS) to combat diseases. As a result, a variety of chimera compounds have been synthesized consisting of a tag that can bind to ubiquitin ligase, a linker and another ligand that can bind to disease related proteins. This enables us to bring the disease related protein in proximity to an activated UPS to eliminate the protein.1)

An example of proteolysis targeting compounds

An example of proteolysis targeting compounds


Mechanism of proteolysis of disease-associated proteins

Mechanism of proteolysis of disease-associated proteins

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Bifunctional Linkers

Measuring the activity of these compounds has shown that the length of the linker is an important factor in triggering ubiquination.2) TCI now offers hetero-bifunctional linkers with a variety of lengths. We are also open to inquiries regarding scale up and custom synthesis of linkers and ligands. Please contact us for more information.

Bifunctional Linkers

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References

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