Starving the malaria parasite:: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

Starving the malaria parasite:: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV
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DOI:
10.1002/anie.200504119
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发表时间:
2006-01-01
影响因子:
16.6
通讯作者:
Diederich, F
Diederich, F
中科院分区:
化学1区
文献类型:
--
作者:
Hof, F;Schütz, A;Diederich, F

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钳制:报道了一类新的针对疟疾蛋白酶家族Plasmepsin的天冬氨酸蛋白酶抑制剂。这些配体利用一种新的”二胺钳”来接合催化二联体。它们是血浆蛋白酶I、II和IV的有效抑制剂,同时保留对密切相关的人组织蛋白酶D和E的良好选择性。(化学方程式)。
Clamping down: A new class of aspartic protease inhibitors that target the malarial protease family Plasmepsin are reported. These ligands utilize a novel" diamine clamp" to engage the catalytic dyad. They are potent inhibitors of plasmepsins I, II, and IV, while retaining good selectivity against the closely related human cathepsins D and E.(Chemical Equation Presented).