Creative Biolabs has knowledgeable and friendly customer services and technical support teams with many years of experience in the life sciences industry. Our powerful technology is designed to overcome the innate challenges of targeted protein degradation leveraging our broad knowledge of the ubiquitin-proteasome system to remove disease-causing proteins. Based on our powerful target protein degradation platform, we are confident to be a competent and trustworthy partner for your research and scientific projects.
Currently, proteolysis-targeting chimeras (Protein Degraders) have become a promising and attractive technology for modulating a protein of interest (POl) by degradation. Protein Degraders is a heterobifunctional molecule that connects a POl ligand to an E3 ubiquitin ligase (E3) recruiting ligand with an optimal linker. Degradation is initiated when Protein Degraders forms a ternary complex with POI and E3. Thereafter, subsequent ubiquitination of POI occurs, and then ubiquitinated POI is recognized and degraded by the 26S proteasome, which is part of the ubiquitin-proteasome system (UPS) in eukaryotic cells (Fig.1). Protein Degraders works in conjunction with the UPS system to achieve the regulation of protein levels.
Fig.1 Mode of action of Protein Degraders. (Sun, 2019)
BRD4, a member of the bromodomain and extra-terminal domain (BET) family, links acetylated histones and transcription factors to the assembled transcriptional apparatus at specific cis-regulatory elements. It plays a vital role in the proliferation of cancer cells by regulating the expression of oncogenes, such as c-myc, bcl-xL, and bcl-6, and is therefore an attractive target for cancer treatment. The following are two examples of Protein Degraders targeting BRD4.
Creative Biolabs has an experienced team of biologists and chemists. Led by outstanding scientists, our team is able to support various ligand designs that target BRD4, including small molecules, peptides, proteins, and antibodies, etc. In addition, we provide a variety of modifications and other strategies to increase the selectivity and potency of Protein Degraders, including adjusting the length and composition of the linker, changing the binding ligand to the target protein and/or E3 ligase, and changing the choice of recruited E3 ligases. With rich experience in molecular discovery, we can provide ligand designs with the following characteristics faster than other companies:
Creative Biolabs has a set of mature molecular discovery processes that cover all stages of Protein Degraders and offer professional after-sale services to achieve customer satisfaction. If you want to know more, please feel free to contact us and we will be happy to discuss our design services to help you.
Reference
Our customer service representatives are available 24 hours a day, from Monday to Sunday. Contact Us