PROTAC Assay Service
PROTAC, a distinctive drug development technology, leverages UPS to induce the degradation of target proteins. Unlike conventional proteomics approaches, the primary focus of PROTAC assay is to monitor dynamic changes in protein levels rather than characterizing and quantifying the proteins themselves. Drawing upon our extensive expertise, Creative Proteomics offers specialized PROTAC assay service, providing a valuable perspective for your protein research or drug development endeavors.
What is PROTAC Assay
PROTAC (Proteolysis Targeting Chimeras) made its debut in 2001, introducing a groundbreaking approach that harnesses the body's natural protein-cleaning system to diminish protein levels, rather than merely inhibit protein function, for therapeutic purposes. This innovative strategy achieves targeted protein degradation through the ubiquitin proteasome system (UPS), the primary cellular pathway responsible for regulating protein levels. The UPS, involved in breaking down over 80% of intracellular proteins, serves as nature's mechanism for disposing of damaged or unnecessary proteins within the cell. Ubiquitin molecules, guided by a series of enzymes, selectively identify target proteins among a multitude of intracellular proteins, marking them for degradation.
Fig. 1 Schematic of PROTAC degradation proteins
PROTAC stands as a bifunctional marvel, wielding a ligand that binds to the target protein on one end and an E3 ligase-binding ligand on the other. This dynamic molecule is bridged by a well-designed linker, forming a powerful tool to tag specific proteins and setting the UPS into action, marking the target protein for degradation. The versatility of PROTAC technology is impressive, having successfully degraded over 100 different proteins. Its range spans diverse targets, from kinases and BET proteins to nuclear receptors. Notably, PROTAC has even tackled "non-druggable targets," exemplified by its success with proteins like the transcription factor regulator PIRIN and the epigenetic player PCAF/GCN5.
Applications of PROTAC Assay
PROTAC assay has a wide range of applications in basic research and drug discovery, providing insight into the mechanisms of targeted protein degradation and contributing to the development of novel therapeutic agents. It has been used in many studies, such as:
Protein functional validation
PROTAC assays are used to validate the specificity and selectivity of target proteins. By demonstrating target engagement and degradation, researchers can confirm the functional relevance of a target in a cellular.
Targeted therapy development
PROTAC assays are vital for assessing PROTAC molecules' therapeutic potential. In relevant cell lines or disease models, they demonstrate target engagement and degradation, supporting the development of targeted therapies.
Drug development
During drug development, the PROTAC assay can be used to screen potential PROTAC pharmacodynamic molecules for potency and selectivity, helping to optimize lead compounds for further development.
Drug resistance
PROTAC assays can be used to study mechanisms of drug resistance. Monitoring changes in the degradation of target proteins during treatment can help identify potential resistance mechanisms.
In addition, it has been used in selective analysis, kinetic evaluation, biomarker discovery, cell signaling pathway studies, etc. PROTAC assay is an integral part of advancing the field of targeted protein degradation and contributes to efforts to utilize the ubiquitin-proteasome system to achieve precision medicine and therapeutic efficacy.
Our Service
With advanced protein detection technology, Creative Proteomics provides targeted services for researchers and scientists to help them utilize powerful analytical techniques to reveal the complexity of the proteome. Our services are thoughtful and detailed, and the PROTAC assay service process is as follows:
Fig. 2 Workflow of PROTAC assay service
Creative Proteomics brings a wealth of experience to the field of protein research. Our comprehensive services and products cover the entire spectrum of utilizing suitable and efficient gateways. Utilizing our proprietary platform, we have successfully implemented many proteomics research projects. If you are interested, please contact us for more information and a quote.