Targeted Protein Degradation

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.

Tocris has a range of Active Degraders targeting different proteins, as well as a toolbox of Degrader Building Blocks to support TPD research and development.

PROTAC is a registered trademark of Arvinas, Inc.

Targets
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Custom Degrader Services

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


A Short Animation Explaining Degrader Technology

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.

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What is Targeted Protein Degradation?

Active Degraders - Tools for Targeted Protein Degradation

Active Degraders - Tools for Targeted Protein Degradation

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.


Our sister Bio-Techne brands offer a range of E3 ligase enzymes, custom E3 ligase enzyme production, as well as assays and kits for ubiquitin research and proteomic analysis of ubiquitination.

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.

Literature for Targeted Protein Degradation

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.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders (e.g. PROTACs)
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Targeted Protein Degradation

Targeted Protein Degradation Poster

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.