PROTAC technology

Rochi Pharmaceutical PROTAC drug discovery technology summarizes the current popular target protein ligands; has established libraries for high-affinity targeting protein small molecule (TPSM) and small molecular fragments, libraries for high-affinity ubiquitin ligase small molecule (E3SM) and small molecular fragments, and linker systems that include diversified bi-functional linkers (BF-Linker). Those compound libraries help to quickly and efficiently synthesize a large number of high-activity PTROTAC bi-specific small molecules, thus greatly accelerating the process of drug R&D. Rochi will make every effort to establish and complete its PROTAC biological screening and testing platform, and the follow-up  development of preclinical stages，until the drug launch.
PROTAC technology mechanism of action:

1. The PROTAC molecule specifically recognizes and binds to the target protein through the target protein ligand (POI Ligand) at one end, and specifically recognizes and binds to E3 Ligase through the E3 ubiquitin ligase ligand (E3 Ligase Ligand) at the other end;
2. Form PO I - P R O T A C - E3 ligase ternary complex;
3. In this ternary complex, the target protein POI is ubiquitinated by E3 ligase, and the ubiquitinated POI is subsequently recognized and degraded by the proteasome, thereby inhibiting the function of the target protein.
PROTAC technical advantages
Changed the none-druggability of targets
The molecular mechanism of PROTAC's action is to degrade the target protein through the ubiquitin-proteasome system, instead of inhibiting protein function by blocking the functional region of the target protein through competitive binding. Therefore, the binding region of PROTAC for target protein recognition does not necessarily have to be an active region. The force also does not necessarily have to be high affinity; this makes some "non-drugable" target proteins that lack high-affinity small molecule binding "drugable".
Efficiency
Traditional small-molecule inhibitors inhibit the function of target proteins by competing for binding to the active functional domain of the target protein, and the amount of small molecules required is often large; while PROTAC degrades the target protein through the ubiquitin-proteasome system to relieve the function of the target protein, so it has the potential to degrade the function of the target protein. Recyclability, low dosage and high efficiency.
Not immunogenic
In contrast to antibody drugs, PROTAC does not elicit the production of anti-drug antibodies.