New class of small nonpeptidyl compounds blocks Plasmodium falciparum development in vitro by inhibiting plasmepsins

Antimicrobial Agents and Chemotherapy

Volumn 45, Issue 9, 2001, Pages 2577-2584

  Jiang, S ^a   Prigge, S T ^a   Wei, L ^a   Gao, Y E ^a   Hudson, T H ^a   Gerena, L ^a   Dame, J B ^a   Kyle, D E ^a  

^a NONE

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMALARIAL AGENT; CATHEPSIN D; PLASMEPSIN II; UNCLASSIFIED DRUG; UREA DERIVATIVE; WR 099444; WR 099445; WR 100080; WR 100081; WR 100392; WR 100400; WR 100484; WR 101653; WR 103412; WR 268961;

ANIMAL CELL; ANTIMALARIAL ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CYTOTOXICITY; DRUG SPECIFICITY; DRUG STRUCTURE; GROWTH INHIBITION; NONHUMAN; PARASITE DEVELOPMENT; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL;

ANIMALS; ANTIMALARIALS; ASPARTIC ENDOPEPTIDASES; CARBANILIDES; DRUG DESIGN; HUMANS; MODELS, MOLECULAR; PARASITIC SENSITIVITY TESTS; PLASMODIUM FALCIPARUM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034864129     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.45.9.2577-2584.2001     Document Type: Article

References (30)

1. Plasmodium falciparum: Differential sensitivity in vitro to E-64 (cysteine protease inhibitor) and pepstatin A (aspartyl protease inhibitor)
2. Screening aspartyl proteases with combinatorial libraries
3. Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D
4. Sequence, expression and modeled structure of an aspartic proteinase from the human malaria parasite Plasmodium falciparum
5. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique
6. Molecular characterization and inhibition of Plasmodmm falciparum aspartic hemoglobinase
7. Order and specificity of the Plasmodiu falciparum hemoglobin degradation pathway
8. Hemoglobin degradation in the malaria parasite Plasmodium falciparum: An ordered process in a unique organelle
9. Automated docking of substrates to proteins by simulated annealing
10. Automated docking of flexible ligands: Applications of AutoDock
11. Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II
12. High level expression and characterization of plasmepsin II, an aspartic proteinase from Plasmodium falciparum
13. Identification of hemoglobin degradation products in Plasmodium falciparum
14. Kinetic analysis of plasmepsin I and II aspartic proteases of the Plasmodium falciparum digestive vacuole
15. Novel fluorogenic substrates for assaying retroviral proteases by resonance energy transfer
16. Studies on plasmepsin I and II from the malarial parasite Plasmodium falciparum and their exploitation as drug targets
17. Expression and characterization of plasmepsin I from Plasmodium falciparum
18. Distributed automated docking of flexible ligands to proteins: Parallel applications of AutoDock 2.4
19. Evidence for the shikimate pathway in apicomplexan parasites
20. Plasmodium falciparum: Effects of proteinase inhibitors on globin hydrolysis by cultured malaria parasites
21. Proteases of malaria parasites: New targets for chemotherapy
22. Structure and inhibition of plasmepsin II, a hemoglobin-degrading enzyme from Plasmodium falciparum
23. Structural analysis of plasmepsin II. A comparison with human aspartic proteases
24. New colorimetric cytotoxicity assay for anticancer-drug screening
25. Porcine spleen cathepsin B is an exopeptidase
26. Human malaria parasites in continuous culture
27. Plasmepsin I and II from the malarial parasite Plasmodium falciparum
28. Plasmodium falciparum P. vivax. and P. malariae: A comparison of the active site properties of plasmepsins cloned and expressed from three different species of the malaria parasite
29. Drug resistance in malaria