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Literature summary extracted from

  • Mishra, V.; Rathore, I.; Arekar, A.; Sthanam, L.K.; Xiao, H.; Kiso, Y.; Sen, S.; Patankar, S.; Gustchina, A.; Hidaka, K.; Wlodawer, A.; Yada, R.Y.; Bhaumik, P.
    Deciphering the mechanism of potent peptidomimetic inhibitors targeting plasmepsins - biochemical and structural insights (2018), FEBS J., 285, 3077-3096 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.23.39 expressed in Escherichia coli Rosetta-gami B (DE3) pLysS cells Plasmodium falciparum

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.23.39 in complex with inhibitors, sitting drop vapor diffusion method, using either 0.1 M HEPES pH 7.5 and 1.4 M sodium citrate tribasic dihydrate or 0.2 M lithium sulfate, 1.26 M ammonium sulfate, 0.1 M Tris pH 8.5 Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.23.B14 KNI-10333 nanomolar inhibition activity Plasmodium falciparum
3.4.23.B14 KNI-10743 nanomolar inhibition activity Plasmodium falciparum
3.4.23.B14 pepstatin A
-
 Plasmodium falciparum
3.4.23.38 KNI-10333 nanomolar inhibition activity Plasmodium falciparum
3.4.23.38 KNI-10743 nanomolar inhibition activity Plasmodium falciparum
3.4.23.38 pepstatin A
-
 Plasmodium falciparum
3.4.23.39 KNI-10333 nanomolar inhibition activity Plasmodium falciparum
3.4.23.39 KNI-10343 nanomolar inhibition activity Plasmodium falciparum
3.4.23.39 KNI-10395 nanomolar inhibition activity Plasmodium falciparum
3.4.23.39 KNI-10742 nanomolar inhibition activity Plasmodium falciparum
3.4.23.39 KNI-10743 nanomolar inhibition activity Plasmodium falciparum
3.4.23.39 pepstatin A
-
 Plasmodium falciparum

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.23.B14 vacuole
-
 Plasmodium falciparum 5773
-
3.4.23.38 vacuole
-
 Plasmodium falciparum 5773
-
3.4.23.39 vacuole
-
 Plasmodium falciparum 5773
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.23.B14 Plasmodium falciparum
-
 isolate 3D7
-
3.4.23.38 Plasmodium falciparum
-
 isolate 3D7
-
3.4.23.39 Plasmodium falciparum
-
 isolate 3D7
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.23.39 Ni-NTA column chromatography and Superdex 75 gel filtration Plasmodium falciparum

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.23.B14 EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
-
 Plasmodium falciparum ?
-
 ?
3.4.23.B14 Hemoglobin + H2O
-
 Plasmodium falciparum ?
-
 ?
3.4.23.38 EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
-
 Plasmodium falciparum ?
-
 ?
3.4.23.38 Hemoglobin + H2O
-
 Plasmodium falciparum ?
-
 ?
3.4.23.39 EDANS-CO-CH2-CH2-CO-Ala-Leu-Glu-Arg-Met-Phe-Leu-Ser-Phe-Pro-Dap-(DABCYL)-OH + H2O
-
 Plasmodium falciparum ?
-
 ?
3.4.23.39 Hemoglobin + H2O
-
 Plasmodium falciparum ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.23.39 ? x * 37000, mature enzyme, SDS-PAGE Plasmodium falciparum
3.4.23.39 ? x * 43000, truncated zymogen, SDS-PAGE Plasmodium falciparum
3.4.23.39 ? x * 60000, thioredoxin-tagged enzyme, SDS-PAGE Plasmodium falciparum

Synonyms

EC Number Synonyms Comment Organism
3.4.23.B14 PMIV
-
 Plasmodium falciparum
3.4.23.38 PMI
-
 Plasmodium falciparum
3.4.23.39 PMII
-
 Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.23.39 0.00000007
-
 pepstatin A at pH 5.0 and 25°C Plasmodium falciparum
3.4.23.39 0.0000013
-
 KNI-10333 at pH 5.0 and 25°C Plasmodium falciparum
3.4.23.39 0.000003
-
 KNI-10343 at pH 5.0 and 25°C Plasmodium falciparum
3.4.23.39 0.0000033
-
 KNI-10743 at pH 5.0 and 25°C Plasmodium falciparum
3.4.23.39 0.000004
-
 KNI-10395 at pH 5.0 and 25°C Plasmodium falciparum
3.4.23.39 0.0000056
-
 KNI-10742 at pH 5.0 and 25°C Plasmodium falciparum