PROTAC® Degraders & Targeted Protein Degradation

Targeted Protein Degradation (TPD) refers to the use of heterobifunctional small molecule "degraders" (e.g. PROTAC molecules) 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
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Bio-Techne's Complete Solution for PROTACs & Targeted Protein Degradation

The Bio-Techne family of brands offers a complete solution for Targeted Protein Degradation research and development. Click the image below to find out more about our Protein Degraders (PROTACs), TAG Degradation Platform (aTAG, dTAG), Degrader Building Blocks, Ubiquitin Proteasome System Proteins and Assays, Automated Assays for Protein Degradation and Custom Degrader Services, including our new, easy to use PROTAC Panel Builder.

 

Learn more about Bio-Techne's complete solution for Targeted Protein Degradation research by visiting biotechne.com/tpd.


Resources for PROTACs & Targeted Protein Degradation

3rd Bio-Techne Targeted Protein Degradation Symposium

Bio-Techne's 3rd virtual symposium on TPD covered some of the hottest topics in the field and included talks on antiviral PROTACs, a clinical candidate BRD9 Degrader, the BromoTag® degradation platform, degraders targeting the CBP/p300, new cereblon-recruiting ligands for PROTAC design, and the first public presentation of CoraFluor TR-FRET probes for TPD assays.

Stream the TPD Symposium On Demand
Targeted Protein Degradation Virtual Symposium

Blog Post: Opportunities and Perspectives on the Design and Synthesis of PROTAC Degraders

This blog post discusses the design and synthesis of PROTAC Degraders and the use of building blocks comprising E3 ligase ligands preconjugated to a linker with reactive handle to expedite the process. Opportunities arising from development of new E3 ligases are also explored.

Read PROTAC Design Blog
PROTAC Design and Synthesis Blog

PROTAC Panel Builder

With our new PROTAC Panel Builder you can quickly and easily request a quote for a selected panel of E3 ligase ligands plus linkers for your Degrader discovery project.

View Panel Builder Tool
PROTAC Panel Builder Tool

Blog Post: Development of a KRAS-Targeting PROTAC

In this question-and-answer session, our Senior Product Specialist, Alex Moloney PhD, talks to Michael Bond (Yale University) about the development of a KRAS-G12C-targeting PROTAC®, LC 2, which is now available from Tocris.

Read KRAS-Targeting PROTAC Blog Now
LC 2 - First Endogenous KRAS-G12C Degrader

Whitepaper: Validating Targets for Targeted Protein Degradation Using dTAG

Our whitepaper describes a comprehensive workflow solution for target validation using the TAG Degradation Platform. The whitepaper provides guidance on TAG knock-in cell-line generation, the use of dTAG Degraders to knockdown your POI, and Simple Western™ instruments and antibodies validated for western blotting to measure target knockdown.

Request TAG Degradation Whitepaper
dTAG Whitepaper

Paper: Reviewing the Toolbox for Degrader Development in Oncology

This review written by our in-house experts and published in Current Opinion in Pharmacology discusses the guidelines, reagents, and technologies available to support Degrader research and development in oncology.

Read Degrader Toolbox Paper
Current Opinion in Pharmacology Review Paper

Webinar: Tackling Targeted Protein Degradation - Workflow Solutions for PROTAC® Degrader Development Programs

This webinar outlines the comprehensive workflow solution available from Bio-Techne for Degrader development programs, from target validation and design of small molecule degraders to proteins and assays for profiling candidate degraders. Presented by our Innovation Manager, Hannah Maple, PhD, the webinar was originally given as a tech talk at Cell Bio Virtual 2020.

Watch Tackling TPD Webinar Now!
Webinar: Tackling 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.

Watch Degrader Technology Animation
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.

View dTAG Animation
What is dTAG?

Webinar: New Frontiers in Targeted Protein Degradation 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.

Watch New Frontiers in TPD Webinar
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.

Read dTAG For Target Validation Blog
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.

Learn About Developing Degraders
Principles of Degrader Design

Meet Jess Your Complete Protein Analysis Solution

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Literature for PROTAC® Degraders & Targeted Protein Degradation

Tocris offers the following scientific literature for PROTAC® Degraders & Targeted Protein Degradation to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Targeted Protein Degradation Research Product Guide

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
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Developing Degraders Poster

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.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Enabling Research By Provision of Chemical Tools Poster

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 Poster

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

Validating Targets for TPD Using dTAG Poster

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.