PROTAC
PROteolysis TArgeting Chimeras (PROTACs) is a chemical molecule with two different ligands at each end. One ligand binds to the E3 ligase, while the other ligand binds the intracellular target proteins. These two ligands are connected by a linker. Such chemical molecules can bind to both E3 ubiquitin ligase and target proteins at the same time. In this scenario, the targeted protein can get ubiquitinated and finally degraded by the proteasome. PROTAC cannot get degraded by the proteasome and can be recycled for the next round of protein degradation.
Figure 1. The principle of PROTAC
Cryogenic electron microscopy (cryo-EM) is the most advanced protein structure analysis technology at present and it will bring a revolutionary breakthrough to the research and development of drugs. It can also provide a better understanding of the PROTAC ternary complexes. Relying on cutting-edge structural analytical methodology and computation-based drug discovery technology, our cryo-EM platform provides comprehensive services to our customers, including new drug target validation, compound library screening, candidate compound discovery, and therapeutic antibody development.
At present, cryo-EM is no longer limited to the scope of basic research and has been further applied in the discovery and preparation of small molecule drugs, such as GPCR drugs, E3 ligases, and PROTACs. If you are interested in our cryo-EM services for drug discovery, please feel free to contact us. We are looking forward to cooperating with you.
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