Literature summary for 3.4.23.50 extracted from

Towler, E.M.; Gulnik, S.V.; Bhat, T.N.; Xie, D.; Gustschina, E.; Sumpter, T.R.; Robertson, N.; Jones, C.; Sauter, M.; Mueller-Lantzsch, N.; Debouck, C.; Erickson, J.W.
Functional characterization of the protease of human endogenous retrovirus, K10: can it complement HIV-1 protease? (1998), Biochemistry, 37, 17137-17144.

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Cloned(Commentary)

Cloned (Comment)	Organism
213 amino acids of the 3'-end of the HERV-K protease open reading frame are expressed in Escherichia coli. Autocatalytic cleavage of the expressed polypeptide results in a catalytically active 18200 Da protein	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
ABT538	-	Homo sapiens
KNI227	-	Homo sapiens
KNI272	-	Homo sapiens
L735,524	-	Homo sapiens
additional information	the enzyme is highly resistant to all the HIV-1 PR inhibitors tested, including L-735,524, Ro31-8959, and ABT 538	Homo sapiens
pepstatin A	-	Homo sapiens
Ro31-8624	-	Homo sapiens
Ro31-8959	-	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.001	-	Lys-Ala-Arg-Val-Tyr-Phe(NO2)-Glu-Ala-Nle-NH2	pH 4.5, 11600 Da core domain	Homo sapiens
0.0103	-	Lys-Ala-Arg-Val-Tyr-Phe(NO2)-Glu-Ala-Nle-NH2	pH 4.5, 18200 Da enzyme form	Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da]	Molecular Weight Maximum [Da]	Comment	Organism
16470	-	avarage molecular weight under near physiological conditions, sedimentation equilibrium analysis	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
18200 Da enzyme form and 11600 Da core domain	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
HIV-1 matrix-capsid polyprotein + H2O	processing at the authentic HIV-1 PR recognition site	Homo sapiens	?	-	?
Lys-Ala-Arg-Val-Tyr-Phe(NO2)-Glu-Ala-Nle-NH2 + H2O	-	Homo sapiens	?	-	?

Subunits

Subunits	Comment	Organism
More	the 11600 Da core domain exists as a dimer at pH 7.0	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.8	-	Lys-Ala-Arg-Val-Tyr-Phe(NO2)-Glu-Ala-Nle-NH2	pH 4.5, 18200 Da enzyme form	Homo sapiens
2.1	-	Lys-Ala-Arg-Val-Tyr-Phe(NO2)-Glu-Ala-Nle-NH2	pH 4.5, 11600 Da core domain	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
4	5	11600 Da core domain	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	-	Homo sapiens
0.0000046	-	KNI227	pH 4.5, 11600 Da core domain	Homo sapiens
0.000015	-	KNI227	pH 4.5, 18200 Da enzyme form	Homo sapiens
0.00006	-	ABT538	pH 4.5, 11600 Da core domain	Homo sapiens
0.00012	-	KNI272	pH 4.5, 11600 Da core domain	Homo sapiens
0.00034	-	KNI272	pH 4.5, 18200 Da enzyme form	Homo sapiens

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Release 2023.1 (January 2023)