Rational Design of Proteasome Inhibitors as Antimalarial Drugs
| Autor: | Camille Le Chapelain, Michael Groll |
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| Rok vydání: | 2016 |
| Předmět: |
Models
Molecular Plasmodium falciparum Molecular Conformation Computational biology Biology Crystallography X-Ray 010402 general chemistry 01 natural sciences Catalysis Antimalarials Parasitic Sensitivity Tests parasitic diseases medicine Structure–activity relationship Artemisinin Low toxicity 010405 organic chemistry Rational design General Chemistry medicine.disease biology.organism_classification 0104 chemical sciences Proteasome Drug Design Proteasome inhibitor Proteasome Inhibitors Malaria medicine.drug |
| Zdroj: | Angewandte Chemie International Edition. 55:6370-6372 |
| ISSN: | 1433-7851 |
| Popis: | One life, two strategies: Crucial structural differences between the human and the Plasmodium falciparum proteasomes were recently identified. A combination of cryo-EM and functional characterization enabled the design of a selective antimalarial proteasome inhibitor that shows low toxicity in the host. When used with artemisinin, this ligand offers a new approach for the efficient treatment of malaria at all stages of the parasite lifecycle. |
| Databáze: | OpenAIRE |
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