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PROTAC Technology Services

PROTACs are bifunctional molecules that hijack the ubiquitin–proteasome system to selectively degrade disease-relevant proteins, providing a route to targets that are difficult or impossible to address with conventional small-molecule inhibitors. PROTAC technology has therefore emerged as one of the most promising and actively investigated approaches in targeted protein degradation (TPD).PROTAC molecules consist of three components, an E3 ubiquitin ligase ligand, a linker, and a target protein-binding ligand.

The ubiquitinated target protein is then recognized and degraded by the proteasome. PROTAC molecules are designed to bring together protein of interest (POI) and E3 ligases—which would otherwise have no interaction—to form a ternary complex consisting of the “target protein–PROTAC–E3 ligase,” thereby achieving precise targeting and degradation of the target protein.

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Figure 1: Schematic diagram illustrating the mechanism of action of PROTAC molecules

 

Leveraging its extensive experience in PROTAC development and an integrated PROTAC development platform, which includes the selection or customized screening of target protein-binding ligand, the design and diverse selection of linkers, the diverse selection of E3 ubiquitin ligase ligands, in vitro efficacy evaluation (cell-level degradation detection), and in vivo efficacy evaluation (animal model experiments), TekBiotech provides one-stop services ranging from the design and optimization of preclinical research protocols, PROTAC development to downstream efficacy evaluation, to accelerate the development of drug candidates and advance them from the laboratory to the clinical stage.

█ PROTAC Technology Services

TekBiotech offers a standardized PROTAC development process. Customers need only provide target information (primarily disease targets) or directly supply the corresponding target agonists or inhibitors, as well as project requirements such as the preferred E3 ubiquitin ligase ligand. TekBiotech’s scientists can then design and select appropriate linkers and ligands based on the target’s characteristics and the experimental objectives, with the aim of obtaining effective PROTAC molecules. If no off-the-shelf inhibitors, agonists, or other ligands are available for the target, TekBiotech’s scientists can design and synthesize screening antigens based on the target’s characteristics. Using established platforms such as the targeted peptide discovery platform and the SELEX platform, they screen for high-quality targeting molecules to design and synthesize PROTAC molecules that meet client requirements. Additionally, TekBiotech can provide downstream in vitro and in vivo efficacy evaluation experiments to meet the diverse project needs of various clients.

TekBiotech offers several types of PROTACs, including small-molecule PROTACs, peptide PROTACs, and Nucleic Acid-Based PROTACs, and also provides customized PROTAC design and synthesis services based on customer needs.

 

Major PROTAC Types:

PROTAC Types

Structure and Applications

Linker

E3 Ubiquitin  Ligase Ligand

Small-Molecule PROTACs

Composed entirely of organic small molecules, they have a relatively low molecular weight and exhibit better cellular permeability and oral bioavailability.

PEG chains, alkyl chains, rigid chains (including aromatic rings, piperazine, etc.)

CRBN, VHL, etc.

Peptide PROTACs

The “warhead” used to target a specific protein or recruit an E3 ligase is a peptide segment.

PEG chains, alkyl chains, rigid chains (including aromatic rings, piperazine, etc.)

CRBN, VHL, etc.

Nucleic Acid-Based PROTACs

Using nucleic acid molecules such as DNA or RNA as targeting moieties, specifically designed to degrade “undruggable” targets—such as transcription factors—that lack small-molecule binding sites

PEG chains, alkyl chains, rigid chains (including aromatic rings, piperazine, etc.)

CRBN, VHL, etc.

   

█ PROTAC Characterization and Analysis Services

 

TekBiotech provides a full range of analytical services that comply with industry standards, covering all stages from early-stage design and synthesis to process scale-up. We utilize a variety of detection methods—including HPLC, mass spectrometry (MS) analysis, NMR, cell-based assays, and animal model detection—to conduct evaluations, providing critical data for process optimization.

 

TekBiotech offers the following characterization and analysis services:

HPLC and MS

NMR

Cell Experiments

Detection in Animal Models

Detect the product's purity and molecular weight

Detect molecular structure

Detection of drug efficacy at the cellular level

Evaluation of drug efficacy in animals


█ Advantages of the PROTAC Technology Service Platform


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One-Stop Solution

Custom PROTAC Solution Design

Comprehensive Characterization and Analysis Evaluation

Mature Downstream Detection Platform

One-stop services ranging from design and synthesis to in vitro and in vivo detection

Diverse design and synthesis of PROTACs

Analysis at the molecular level, analysis at the cellular level, and in vivo analysis

In vitro efficacy detection, In vivo efficacy evaluation

 


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