PROTAC Linkers

PROTAC is a bifunctional molecule composed of three parts: one end is the target protein binding ligand, the other end is the E3 ubiquitin ligase ligand, and the middle is the linker chain. In cells, PROTAC molecules can recognize and selectively bind target proteins, recruit specific E3 ubiquitin ligases, and form a "target protein-PROTAC-E3 ubiquitin ligase" ternary complex. Afterwards, E3 ubiquitin ligase and E2 ubiquitin conjugating enzyme work together to ubiquitinate the target protein. Since the ubiquitin-proteasome system (UPS) is an important pathway for protein degradation in human cells, it is involved in the degradation of more than 80% of proteins in cells. Therefore, after the target protein is ubiquitinated, the PROTAC molecule interacts with the target protein and E3 ubiquitinase. Once isolated, the ubiquitin-tagged target protein is recognized and degraded by the proteasome. By relying on the physiological process of ubiquitination-degradation proteins existing in the human body, PROTAC molecules can efficiently and specifically catalyze the degradation of pathogenic proteins, so as to achieve the purpose of treating diseases. Unlike traditional protein small molecule inhibitors, the mechanism of action of PROTAC is event-driven and does not require prolonged occupation of the target. After PROTAC completes the ubiquitination labeling of a target protein, it can be separated from the target protein and E3 ubiquitin ligase and continue to label the next protein. Therefore, in the process of exerting the degradation effect, a small amount of PROTAC molecules can achieve the purpose of inducing degradation of a large number of target proteins. In addition, PROTAC can generate selectivity for different kinds of target proteins and E3 enzymes, and the openness of its molecular design further improves the selectivity of PROTAC for target protein degradation. More importantly, compared with kinase inhibitors, PROTAC molecules have lower requirements for the affinity of target proteins. By rationally designing the molecular structure of PROTAC, it has a wide range of applications in targeting some currently undruggable targets. Therefore, we provide PROTAC linkers for synthesizing PROTACs to advance related research on PROTACs.

CD Bioparticles manufactures and supplies PROTAC linkers for PROTACs synthesis. Contact us to find out how PROTAC linkers can help your work.