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国金证券:蛋白质降解剂有望弥补传统小分子不足

Sinolink: Protein degradation agents are expected to make up for the shortcomings of traditional small molecules.

Breakings ·  Oct 17 07:53

sinolink's research report points out that protein degraders are expected to compensate for the shortcomings of traditional small molecules. Traditional small molecule inhibitors mainly use an "occupancy-driven" mode of action, leading to: 1. Difficulties in targeting proteins lacking hydrophobic pockets; 2. Inability to disrupt the function of scaffold proteins; 3. Long-term use can lead to drug resistance. In contrast, protein degraders adopt a unique "event-driven" mode, which can directly induce the degradation of target proteins. Subsequently, the degraders can be continuously recycled without the need to remain bound to a specific target protein for a long time. The unique mechanism of action gives degraders a range of advantages. Compared to inhibitors, degraders theoretically have a wider range of protein targets. Due to their different mechanisms, degraders are expected to become optional treatment options for patients resistant to clinical inhibitors. In summary, the two major core application scenarios for protein degraders in the future are the population resistant to existing small molecule inhibitors and targeting the difficult-to-target sites of existing small molecule inhibitors. Also, in the field of cancer treatment, protein degraders are expected to enter first-line therapy by combining with other drugs. Recommended stocks: beigene, jiangsu hengrui pharmaceuticals, etc.

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