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Volume 4, Number 1—March 1998


Proteases of Malaria Parasites: New Targets for Chemotherapy

Philip J. RosenthalComments to Author 
Author affiliation: San Francisco General Hospital and University of California, San Francisco, California, USA

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Table 3

Protease targets for chemotherapy

Effective inhibitorsa
Protease Biologic role Compound (Reference) In vitrob
(IC50; μM) In vivoc (mg/kg/day)
Pf68 Erythrocyte invasion GlcA-Val-Leu-Gly-Lys-NHC2H5 (40) 900
Plasmepsin I Hemoglobin degradation SC-50083 (41)
Ro 40-4388 (42) 2-5
Plasmepsin II Hemoglobin degradation Compound 7 (43) 20
Falcipain Hemoglobin degradation Z-Phe-Arg-CH2F (44) 0.064
Mu-Phe-HPh-CH2F (45) ~0.03 400
Mu-Leu-HPh-VSPh (46) 0.01
Oxalic bis ((2-hydroxy-1-naph- thylmethylene)hydrazide) (47) 7
1-(2,5-dichlorophenyl)-3- (4-quinolinyl)-2-propen-1-one (48) 0.23
7-chloro-1,2-dihydro-2-(2,3-di- methoxy-phenyl)-5,5-dioxide- 4-(1H,10H)-phenothiazinone (49) 2

aThe structures of these compounds and details of the described studies are in the references noted.
bAssays compared the development of new ring-form parasites or the uptake of [3H]hypoxanthine by treated and control parasites.
cCure of Plasmodium vinckei-infected mice.

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