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PDBsum entry 4k5m
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Hydrolase/hydrolase inhibitor
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PDB id
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4k5m
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References listed in PDB file
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Key reference
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Title
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Synthesis and structure-Activity relationships of phosphonic arginine mimetics as inhibitors of the m1 and m17 aminopeptidases from plasmodium falciparum.
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Authors
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K.Kannan sivaraman,
A.Paiardini,
M.Sieńczyk,
C.Ruggeri,
C.A.Oellig,
J.P.Dalton,
P.J.Scammells,
M.Drag,
S.Mcgowan.
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Ref.
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J Med Chem, 2013,
56,
5213-5217.
[DOI no: ]
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PubMed id
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Abstract
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The malaria parasite Plasmodium falciparum employs two metallo-aminopeptidases,
PfA-M1 and PfA-M17, which are essential for parasite survival. Compounds that
inhibit the activity of either enzyme represent leads for the development of new
antimalarial drugs. Here we report the synthesis and structure-activity
relationships of a small library of phosphonic acid arginine mimetics that probe
the S1 pocket of both enzymes and map the necessary interactions that would be
important for a dual inhibitor.
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