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[Selective inhibitors of plasmepsin II from Plasmodium falciparum based on pepstatin]. 2008
L D Rumsh, and
A G Mikhaĭlova, and
I V Mikhura, and
I A Prudchenko, and
L D Chikin, and
I I Mikhaleva, and
E N Kaliberda, and
N I Dergousova, and
E E Mel'nikov, and
A A Formanovskiĭ
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, Moscow, 117997 Russia. rumsh@enzyme.siobc.ras.ru
A number of new inhibitors of plasmepsin II (PlmII) from Plasmodium falciparum, one of the key factors of malarial parasite survival, were synthesized. The inhibitors are analogues of pepstatin with various variants of Ala residue substitutions. Effects of the inhibitors on human PlmII and cathepsin D were studied. Inhibition of PlmII by the substrate was found, which required the use of the modified Henderson method for the determination of inhibition constants. Two synthesized inhibitors were shown to exhibit a pronounced selectivity to PlmII (K(i) = 5.5 and 5 nM) in comparison with cathepsin D (K(i) = 230 and 3000 nM, respectively).
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N I Dergousova, and
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A A Formanovskiĭ
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September 1998,
Bioorganic & medicinal chemistry letters,
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Current medicinal chemistry,
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L D Chikin, and
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February 2003,
Journal of medicinal chemistry,
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Phytochemistry,
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E E Mel'nikov, and
A A Formanovskiĭ
October 2016,
Biochimica et biophysica acta,
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I V Mikhura, and
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I I Mikhaleva, and
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E E Mel'nikov, and
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April 2014,
Fitoterapia,
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N I Dergousova, and
E E Mel'nikov, and
A A Formanovskiĭ
January 2018,
PloS one,
L D Rumsh, and
A G Mikhaĭlova, and
I V Mikhura, and
I A Prudchenko, and
L D Chikin, and
I I Mikhaleva, and
E N Kaliberda, and
N I Dergousova, and
E E Mel'nikov, and
A A Formanovskiĭ
September 1996,
Proceedings of the National Academy of Sciences of the United States of America,
