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TargetPlasmepsin I
LigandStatine-like inhibitor 16
Substrate/CompetitorPeptide Substrate
Meas. Tech.Enzyme Inhibition Measurements
pH4.5±n/a
Temperature295.15±n/a K
Ki 0.5±n/a nM
Citation Johansson, POChen, YBelfrage, AKBlackman, MJKvarnstrom, IJansson, KVrang, LHamelink, EHallberg, ARosenquist, ASamuelsson, B Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.J Med Chem.47:3353-66(2004)[PubMed]
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Plasmepsin I
NamePlasmepsin I
SynonymsEC 3.4.23.38 | PFAPG | Plasmepsin-1 precursor
TypeEnzyme
Mol. Mass.51461
OrganismPlasmodium falciparum
Descriptionn/a
Residue452
Sequence
MALSIKEDFSSAFAKNESAVNSSTFNNNMKTWKIQKRFQILYVFFFLLITGALFYYLIDN
VLFPKNKKINEIMNTSKHVIIGFSIENSHDRIMKTVKQHRLKNYIKESLKFFKTGLTQKP
HLGNAGDSVTLNDVANVMYYGEAQIGDNKQKFAFIFDTGSANLWVPSAQCNTIGCKTKNL
YDSNKSKTYEKDGTKVEMNYVSGTVSGFFSKDIVTIANLSFPYKFIEVTDTNGFEPAYTL
GQFDGIVGLGWKDLSIGSVDPVVVELKNQNKIEQAVFTFYLPFDDKHKGYLTIGGIEDRF
YEGQLTYEKLNHDLYWQVDLDLHFGNLTVEKATAIVDSGTSSITAPTEFLNKFFEGLDVV
KIPFLPLYITTCNNPKLPTLEFRSATNVYTLEPEYYLQQIFDFGISLCMVSIIPVDLNKN
TFILGDPFMRKYFTVFDYDNHTVGFALAKKKL
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Statine-like inhibitor 16
NameStatine-like inhibitor 16
Synonyms:(3S,4S)-5-[(4-bromophenyl)methoxy]-N-[(1S)-1-{[(1S)-1-carbamoyl-3-methylbutyl]carbamoyl}ethyl]-3-hydroxy-4-[(2S)-3-methyl-2-(pyridin-2-ylformamido)butanamido]pentanamide | Pyridine-2-carboxylic Acid ((S)-1-{(1S,2S)-1-(4-Bromobenzyloxymethyl)3-[(S)-1-((S)-1-carbamoyl-3-methyl-butylcarbamoyl)ethylcarbamoyl]-2-hydroxypropylcarbamoyl}-2-methylpropyl)amide
TypeSmall organic molecule
Emp. Form.C32H45BrN6O7
Mol. Mass.705.64
SMILESCC(C)C[C@H](NC(=O)[C@H](C)NC(=O)C[C@H](O)[C@H](COCc1ccc(Br)cc1)NC(=O)[C@@H](NC(=O)c1ccccn1)C(C)C)C(N)=O |r|
Structure
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Peptide Substrate
NamePeptide Substrate
Synonymsn/a
TypePeptide
Mol. Mass.n/a
Organismn/a
Descriptionn/a
Residue8
Sequence
DABCYL-Glu-Arg-Nle-Phe-Leu-Ser-Phe-Pro-EDANS