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Literature summary for 3.4.23.B19 extracted from

  • Sittikul, P.; Songtawee, N.; Kongkathip, N.; Boonyalai, N.
    In vitro and in silico studies of naphthoquinones and peptidomimetics toward Plasmodium falciparum plasmepsin V (2018), Biochimie, 152, 159-173 .
    View publication on PubMed
Search for more literature for 3.4.23.B19

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 (DE3) cells Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,2-dimethylpropyl heptanoate 58.6% residual activity at 0.05 mM Plasmodium falciparum
3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,2-dimethylpropyl tridecanoate 49.5% residual activity at 0.05 mM Plasmodium falciparum
Cu2+
-
 Plasmodium falciparum
Fe3+
-
 Plasmodium falciparum
Hg2+
-
 Plasmodium falciparum
additional information not influenced by Ca2+; pepstatin A cannot inhibit refolded enzyme activity Plasmodium falciparum
NKPSL4 59.3% residual activity at 0.05 mM Plasmodium falciparum
rhinacanthin-M 60.9% residual activity at 0.05 mM Plasmodium falciparum
rhinacanthin-N 63.3% residual activity at 0.05 mM Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
erythrocyte membrane protein 2 + H2O Plasmodium falciparum i.e. Dabcyl-RYVRILSETEE-Edans ?
-
 ?
histidine-rich protein II + H2O Plasmodium falciparum i.e. Dabcyl-LNKRLLHETQE-Edans ?
-
 ?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8I6Z5 isolate 3D7
-

Purification (Commentary)

Purification (Comment) Organism
HiTrap Q column chromatography and HisTrap column chromatography Plasmodium falciparum

Renatured (Commentary)

Renatured (Comment) Organism
using a 10-volume rapid dilution into 20 mM Tris-HCl pH 8, 0.15 M NaCl, 1 mM GSH, 0.1 mM GSSG, and 10% (v/v) glycerol with gentle stirring at 25°C for 24 h Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
erythrocyte membrane protein 2 + H2O i.e. Dabcyl-RYVRILSETEE-Edans Plasmodium falciparum ?
-
 ?
histidine-rich protein II + H2O i.e. Dabcyl-LNKRLLHETQE-Edans Plasmodium falciparum ?
-
 ?

Subunits

Subunits Comment Organism
? x * 50620, mature enzyme, calculated from amino acid sequence Plasmodium falciparum

Synonyms

Synonyms Comment Organism
PMV
-
 Plasmodium falciparum
PMVm84 mature truncated enzyme Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02225
-
 at pH 6.5 and 25°C Plasmodium falciparum 3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,2-dimethylpropyl heptanoate
0.06894
-
 at pH 6.5 and 25°C Plasmodium falciparum 3-(3-hydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-2,2-dimethylpropyl tridecanoate