openPR Logo
Press release

New Technology of PROTACs

Most of the drugs currently in clinical use are based on small molecules and use the "occupancy-driven" mode of action to inhibit the function of proteins and play a role in the treatment of diseases. Different from traditional small molecule inhibitors and antagonists, protein degradation technology has developed rapidly in recent years because of its ability to induce the degradation of therapeutic target proteins, providing a new idea for the development of new drugs.

PROTACs (Proteolysis-targeting Chimeras), which was first proposed by Crews et al in 2001, can reduce protein levels rather than inhibit protein functions by taking advantage of the natural protein cleaning system in the body. PROTAC is a heterobifunctional molecule with one end connected to a ligand that binds the target protein, one end to an E3 ubiquitin ligase, and a suitable Linker in the middle. PROTAC degradation of target proteins is achieved through the ubiquitin proteasome system (UPS).

Since PROTACs were developed on the basis of POI inhibitors, they still have a certain degree of off-target effects. Second, due to the large molecular weight of PROTAC, its poor cell membrane permeability and poor pharmacokinetic (PK) properties greatly reduce its biological and therapeutic effects. In addition, although some PROTACs can effectively induce the degradation of target proteins, their biological effects are weak and have no effective effect on disease. Finally, most proteins do not have corresponding small molecule conjugates to design PROTACs, such as transcription factors that play an important role in disease development. Since there are few inhibitors of transcription factors, there is no binder available when designing PROTACs targeting transcription factors. This greatly limits the application of PROTAC technology. In order to solve the above problems, different types of PROTAC technologies have emerged in recent years, such as Antibody-PROTAC, Aptamer-PROTAC conjugates, Dual-target PROTACs, Folate-caged PROTACs and TF-PROTACs.


Antibody-PROTAC is a new strategy to explore the assembly of new antibody-PROTAC conjugates in combination with antibodies. This technology enables specific degradation of proteins in different cells and tissues, thereby optimizing and maximizing the therapeutic window, reducing the side effects of broad-spectrum PROTACs, and increasing their potential as drugs or chemical tools.

Aptamer-PROTAC conjugates

Aptamers are single-stranded nucleic acids with complex three-dimensional structures, mainly including stems, loops, hairpins and G4 polymers. They bind to target proteins through special effects such as hydrogen bonds, base stacking forces, electrostatic effects, etc., with high specificity and affinity, and can improve the water solubility, membrane permeability, and tumor targeting of traditional PROTACs.

Dual-target PROTACS

In the occurrence and development of cancer, there are usually multiple factors that work together, including different kinds of kinases and growth factors, which can act independently or interfere with each other through signaling networks. This method is mainly to design a single molecule that binds two or more pharmacophore, and simultaneously targets two or more anti-tumor targets.

Folate-caged PROTACs

Folate receptor alpha (FOLR1) is low in normal tissues but highly expressed in many human cancers. Folic acid caged PROTACs is another technology to improve the targeting specificity of PROTACs. The basic principle is to introduce folic acid groups into PROTAC molecules to achieve release in target cells and tissues. In this technique, folic acid releases active PROTAC through the action of endogenous hydrolase in the cell, and then the degradant induces the degradation of the target protein.


Transcription factors (TFs) are a class of proteins involved in gene expression and regulation, and are also potential targets for tumor therapy. Transcription factors, unlike traditional kinases, do not have activity pockets or allosteric regulatory sites commonly found in kinases or other enzymes, making them difficult to target by small molecule inhibitors. Since TFs can bind to specific DNA sequences and regulate the transcription process, it is theoretically possible to target TFs with different DNA sequences instead of small molecule inhibitors. Therefore, TF-PROTAC replaces the small molecule ligand of the targeting protein with the corresponding DNA sequence to form TF-PROTAC, which targets specific TF and induces its degradation, thereby regulating the level and biological function of specific TF.

As a professional PEG derivatives supplier, Biopharma PEG is dedicated to the R&D of PROTAC Linker, providing high purity PEG linkers with various reactive groups to continuously assist your project development.

Biopharma PEG Scientific Inc.
Address: 108 Water Street, Room 4D, Watertown, MA 02472, USA
TEL: 1-857-366-6766
Fax: 617-206-9595

Biopharma PEG Scientific Inc. is a biotechnology-oriented company in Watertown, Massachusetts. We are dedicated to manufacturing and supplying high purity monodispersed and polydispersed polyethylene glycol (PEG) derivatives and PEG raw material, PEGylation services, and custom PEG derivative synthesis to clients worldwide. We continuously expand the capability to provide large-scale manufacture of high purity PEG derivatives with an extensive variety of functional groups, in both non-GMP and GMP grade. These PEG linkers have been widely used in bioconjugation, antibody-drug conjugates (ADCs) therapeutic, click chemistry, 3d bioprinting, drug delivery and diagnostics field, etc. 

This release was published on openPR.

Permanent link to this press release:

Please set a link in the press area of your homepage to this press release on openPR. openPR disclaims liability for any content contained in this release.

You can edit or delete your press release New Technology of PROTACs here

News-ID: 2688813 • Views: 537

More Releases from Biopharma PEG Scientific Inc.

Biopharma PEG Supplies Cholesterol (Plant-Derived) Used As Excipients for Lipid Nanoparticles (LNPs)
Biopharma PEG Supplies Cholesterol (Plant-Derived) Used As Excipients for Lipid …
Cholesterol, a derivative of cyclopentane polyhydrophenanthrene, is the main steroid compound in mammals. Most of the traditional cholesterol comes from animal brainstem and lanolin, which is of animal origin and has the risk of carrying animal viruses. Biopharma PEG innovatively uses plant sterols as starting materials to prepare plant-derived cholesterol (CAS NO.: 57-88-5) through biological fermentation and green synthesis, eliminating the generation and carrying of viruses from the source. Cholesterol has
Development Trends And Potential Challenges of PROTACs
Development Trends And Potential Challenges of PROTACs
PROTAC technology has been in development for more than 20 years. PROTAC proof-of-concept studies date back to 2001, when Crews' team tested the possibility of artificially induced intracellular protein degradation with a peptide that was too large in molecular weight and required cells to penetrate the peptide to improve cell permeability. The discovery of the first small molecule PROTAC and the subsequent small molecule E3 ligand, reported in 2008, greatly
ADC Drugs For Breast Cancer Treatment
ADC Drugs For Breast Cancer Treatment
Breast cancer is the malignant tumor with the highest morbidity and mortality among women worldwide. At present, the main therapeutic methods include surgery, chemotherapy, radiotherapy, endocrine therapy and targeted therapy, etc. The development and marketing of new drugs have far-reaching significance in improving the survival of breast cancer patients and changing the pattern of breast cancer treatment. On February 24, 2023, The NMPA approved Enhertu, an injectable drug developed jointly by
History Development of Hydrogels
History Development of Hydrogels
Hydrogels are composed of hydrophilic polymers, whose three-dimensional network structure can not only absorb a large amount of water, but also be used to carry drugs. Hydrogels prepared with suitable materials have the characteristics of high biocompatibility, mechanical and viscoelastic control. Since the term was coined in the late 19th century, hydrogels have been widely used in drug delivery, wound dressing, tissue engineering, and hygiene products. This article mainly introduces

All 5 Releases

More Releases for PROTAC

Profacgen Provides Protein Ubiquitination Services to Accelerate Drug Developmen …
Profacgen, an experienced provider in biological research and drug discovery, provides various ubiquitin services to help customers accelerate research progress and obtain better results. Ubiquitination is one of the most prevalent post-translational modifications (PTMs) in cells. Ubiquitin modification induces protein degradation, which affects the function, localization, and activity of proteins. Therefore, the study of protein ubiquitination plays an important role in cell biology and drug discovery. With the comprehensive advanced platform, Profacgen
PROteolysis Targeting Chimera (PROTAC) Market Key-Players and Forecast Research …
The Global PROteolysis Targeting Chimera (PROTAC) Market Report is a valuable source of insightful data for business strategists. It provides the industry overview with growth analysis and historical & futuristic cost, revenue, demand, and supply data (as applicable). The research analysts provide an elaborate description of the value chain and its distributor analysis. This Market study provides comprehensive data that enhances the understanding, scope, and application of this report. "Due to Financial Year
PROteolysis Targeting Chimera (PROTAC) Market to Witness Huge Growth by Key Play …
The market report delivers an all-inclusive analysis of the market structure along with a forecast of the various segments and sub-segments of the PROteolysis Targeting Chimera (PROTAC) industry. This wide-ranging market research report acts as a backbone for the success of business in any niche. The PROteolysis Targeting Chimera (PROTAC) market survey report has been prepared by conducting market research in a systematic manner. Moreover, the PROteolysis Targeting Chimera (PROTAC)
Targeted Protein Degradation Market, 2021-2030
Targeted protein degradation has emerged as a revolutionary pharmacological concept that presents both viable and versatile drug development opportunities and is anticipated to introduce a new paradigm in modern healthcare London Roots Analysis has announced the addition of “Targeted Protein Degradation Market, 2021-2030” report to its list of offerings. Small-molecule-induced protein degradation has been demonstrated to possess the potential to drug a broader range of proteinaceous biological targets. It involves the
The targeted protein degradation enabling technologies market, featuring a healt …
Targeted protein degradation has emerged as a revolutionary pharmacological concept that presents both viable and versatile drug development opportunities and is anticipated to introduce a new paradigm in modern healthcare London Roots Analysis has announced the addition of “Targeted Protein Degradation Market, 2021-2030” report to its list of offerings. Small-molecule-induced protein degradation has been demonstrated to possess the potential to drug a broader range of proteinaceous biological targets. It involves the
The targeted protein degradation market is projected to grow at an annualized ra …
The concept of targeted protein degradation presents revolutionary drug development opportunities and is anticipated to bring about a paradigm shift in modern healthcare. The first targeted protein degrader, called proteolysis targeting chimera (PROTAC), was developed about a decade ago. Presently, a variety of other such chemical entities and molecular glues are under investigation. In fact, certain pipeline candidates are already in the mid to late-phase trials and are anticipated to