Literature summary for 3.4.23.39 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 .

Search for more literature for 3.4.23.39

Cloned(Commentary)

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

Crystallization (Commentary)

Crystallization (Comment)	Organism
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

Inhibitors	Comment	Organism	Structure
KNI-10333	nanomolar inhibition activity	Plasmodium falciparum
KNI-10343	nanomolar inhibition activity	Plasmodium falciparum
KNI-10395	nanomolar inhibition activity	Plasmodium falciparum
KNI-10742	nanomolar inhibition activity	Plasmodium falciparum
KNI-10743	nanomolar inhibition activity	Plasmodium falciparum
pepstatin A	-	Plasmodium falciparum

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
vacuole	-	Plasmodium falciparum	5773	-

Organism

Organism	UniProt	Comment	Textmining
Plasmodium falciparum	-	isolate 3D7	-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

Synonyms	Comment	Organism
PMII	-	Plasmodium falciparum

Ki Value [mM]

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

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Release 2023.1 (January 2023)