动物造模,抵御耐药性疟疾新型疗法 z-bio 2021-06-09 298

　　Researcher Tilley said that artemisinin can promote the protein damage of the malaria parasite, but the malaria parasite often develops a special way to deal with this damage, so the development of new drugs against drug-resistant malaria parasites is imminent;

　　The new drug developed by the researchers in the article can target the Plasmodium's waste disposal system, which is the proteasome system. The Plasmodium proteasome system is similar to a shredder, which can chew damaged or depleted proteins; Moreover, when the malaria parasite transitions from one life stage to another stage, a large number of damaged proteins will be produced. These proteins are very dependent on the proteasome system, and they may also be used as new drug targets to help develop new anti-malarial drugs.

　　Researchers at Stanford University purified the Plasmodium proteasome and used a new method to test the activity of the proteasome in digesting a variety of different peptide sequences. Then they designed a selective target inhibition of the Plasmodium proteasome. New inhibitor; then researchers from the Cambridge Medical Research Council (MRC) used a technique called single-particle cryo-electron microscopy to generate a three-dimensional high-resolution protein structure, which can help further design to resist drug-resistant malaria Targeted drugs for protozoa. The researchers pointed out that this new type of proteasome inhibitor can actually supplement the treatment of artemisinin. Artemisinin induces protein damage, while the proteasome inhibitor inhibits the repair of damaged proteins by malaria parasites. This two-in-one therapy Perhaps it will have a double blow to the malaria parasites, thereby enhancing the effect of artemisinin and the ability to resist drug-resistant malaria parasites during the recovery period.

　　In the next step, researchers plan to screen Takeda Pharmaceutical (a pharmaceutical company) library to find similar drugs that do not affect human proteasomes. The current proteasome inhibitors may be a good start, but they are not suitable for humans. It may take a long time for humans to be taken orally in the later period; the researchers said that if a drug that can be matched with the new malaria drug can be found in Takeda’s library, then it may be possible to quickly perform clinical trials in the human body. Experimented.