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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.
The Bio-Techne family of brands offers a complete solution for TPD research and development, including Active Degraders (PROTACs), TAG Degradation Platform (aTAG, dTAG), Degrader Building Blocks, Ubiquitin Proteasome System Proteins and Assays, Assays for Protein Degradation and Custom Degrader Services.
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!
Our short animation explains the dTAG system, which provides an alternative to genetic methods of target validation. dTAG harnesses the ubiquitin/proteasome system to selectively degrade fusion proteins comprising mutant FKBP12 and a target protein of interest.Watch Now!
This webinar provides an introduction to the field of Targeted Protein Degradation, discussing design and optimization of Degrader molecules and how structural biology and rational design can shed light on the Degrader development process. The second section of the webinar presents the dTAG platform for target validation.Watch Now!
Read our blog post to find out more about dTAG Degraders and their potential for use in the validation of targets for which there is no know ligand.Read Now!
Tocris scientists have established a set of guidelines relating to the physicochemical properties required in the design and synthesis of cell-permeable Degrader molecules. Read the paper in MedChemComm to find out more.Read Now!
PROTAC is a registered trademark of Arvinas, Inc.
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.