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Targeted Protein Degradation (TPD) refers to the use of heterobifunctional small molecule "degraders" (e.g. PROTACs) to achieve knockdown of target proteins within cells. These small molecules consist of binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. The binding of both moieties results in the formation of a ternary complex between target protein and E3 ligase, leading to polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation.
PROTAC is a registered trademark of Arvinas, Inc.
Tocris offers a custom service for the design and synthesis of degrader (PROTAC) building blocks for your targeted protein degradation research. Additionally, we can partner with your discovery project for the custom design and synthesis of active degraders.
Please complete our custom degrader services form to let us know your custom degrader requirements
Our short animation explains the fundamentals of Targeted Protein Degradation (TPD) using small molecule Degraders. Degraders are heterobifunctional compounds that harness the ubiquitin/proteasome system to selectively remove proteins from cells.Watch Now!
Figure 1: Schematic showing the catalytic mode of action of heterobifunctional degrader molecules. Degraders initiate the formation of a ternary complex between an E3 ubiquitin ligase and a target protein which results in polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation. Degraders act catalytically by repeatedly engaging and directing the ubiquitination of target molecules.
Adapted from Tinworth et al. (2016) Med.Chem.Comm. 7 2206.
Are you developing Degraders in your lab? For quantitative, reproducible and automated analysis of protein degradation, check out the Simple Western™ range from our sister brand, Protein Simple.
Tocris offers the following scientific literature for Targeted Protein Degradation to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed.