New York, USA – July 19, 2021 – PROTACs are small heterobifunctional molecules based on the combination of ubiquitin E3 ligase ligands with the protein of interest (POI) ligands via different types of linkers. These small molecules are promising specific protein degraders with the ability to induce selective intracellular proteolysis.
Being capable of targeting specific proteins that are denatured, mutated, or harmful and inducing protein degradation in cells, PROTAC enables the development of more potent and selective cancer therapies and changes the traditional concept in drug discovery that proteome are undruggable. Creative Biolabs, as a top-tier service provider in the field of biological research and drug discovery, is dedicated to comprehensive solutions to PROTAC discovery and research.
The key part of a PROTAC molecule is two ligands, one of which binds to the POI, and the other binds to an E3 ligase to engage the ubiquitin system of the cell. The human genome encodes more than 600 E3 ligases, and the ligands to E3 proteins should at least be equal to E3 ligases in quantity. Different ligand products are available at Creative Biolabs, such as E3 ligase ligands, ligand-linker conjugates, target protein ligands, as well as intact PROTAC molecules.
E3 Ligase and Target Proteins
Rather than directly occupying an active site to modify protein function, PROTAC takes advantage of the cell’s own ubiquitin-proteasome system (UPS). The targeted protein degradation machinery to irreversibly destroy target proteins greatly relies on the affinity of PROTAC molecules to the POI and to the E3 ligase proteins. However, many of the ligases remain relatively uncharacterized excluding the 600 identified ligases in the human genome. Creative Biolabs provides different products of E3 ligase proteins and target proteins to better optimization and characterization of PROTACs.
What bridges the POI ligand and the E3 ligand in a PROTAC is a linker. The most commonly used PROTAC linkers in the development of PROTACs are alkyl-chains, PEGs, alkyl/ethers, etc. Research suggests that the length and types of the linker are critical to the activity of PROTAC molecules, so Creative Biolabs introduces a wide range of linkers to help customers’ acquire the best result in target protein ubiquitination and degradation.
More solutions, products, and platforms for PROTAC drug discovery are available at: https://www.creative-biolabs.com/protac.
About Creative Biolabs
With advanced platforms and competent scientists, Creative Biolabs is specialized in providing one-stop PROTAC solutions in the process of novel PROTAC drug discovery, including services of PROTAC molecule discovery, PROTAC in vitro evaluation, and PROTAC in vivo animal test, as well as products of linkers, ligands, and a variety of proteins.