PROTACs & 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. PROTACs, also known as Active Degraders, 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.

Targets
Literature (4)

Bio-Techne's Complete Solution for PROTACs & Targeted Protein Degradation

The Bio-Techne family of brands offers a complete solution for TPD research and development. Click the image below to find out more about our 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.


Resources for PROTACs & Targeted Protein Degradation

A Short Animation Explaining Degrader Technology

Our short animation explains the fundamentals of Targeted Protein Degradation (TPD) using small molecule Degraders or PROTACs. 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?

What is dTAG?

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.

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What is dTAG?

Webinar: New Frontiers in TPD and Degrader Development

This webinar provides an introduction to the field of Targeted Protein Degradation, discussing design and optimization of Degrader, or PROTAC, 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.

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New Frontiers in TPD and Degrader Development

Blog Post: dTAG - A Protein Degradation Platform for Target Validation

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.

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What is dTAG?

Research Paper: Developing Degraders

Tocris scientists have established a set of guidelines relating to the physicochemical properties required in the design and synthesis of cell-permeable Degrader/ PROTAC molecules. Read the paper in MedChemComm to find out more.

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Principles of Degrader Design


PROTAC is a registered trademark of Arvinas, Inc.

Literature for PROTACs & Targeted Protein Degradation

Tocris offers the following scientific literature for PROTACs & 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.


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
Developing Degraders

Developing Degraders Poster

This poster describes the generation of a database of Degraders (PROTACs) from the literature. The Degraders were profiled according to the constituent ligands, linker type, linker length and physicochemical properties and this information was used to establish a set of guidelines for the design and synthesis of cell-permeable Degrader molecules. Presented at the 20th SCI/RSC Medicinal Chemistry Symposium 2019, Cambridge, UK.
Enabling Research By Provision of Chemical Tools

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.
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. Presented at EFMC 2018, Ljubljana, Slovenia