Literature summary for 3.4.11.7 extracted from

Goto, Y.; Hattori, A.; Ishii, Y.; Mizutani, S.; Tsujimoto, M.
Enzymatic properties of aminopeptidase A: regulation of its enzymatic activity by calcium and angiotensin IV (2006), J. Biol. Chem., 281, 23503-23513.

Cloned(Commentary)

Cloned (Comment)	Organism
expression of soluble C-terminally His-tagged enzyme, possessing an N-terminal human trypsin II signal peptide, in Spodoptera frugiperda Sf9 insect cells using the baculovirus transfection system	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
1,10-phenanthroline	IC50 is 0.06 mM	Homo sapiens
amastatin	IC50 is 157 nM	Homo sapiens
angiotensin II	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.065 mM in presence of Ca2+	Homo sapiens
angiotensin III	competitive against Glu-4-methylcoumaryl-7-amide	Homo sapiens
angiotensin IV	competitive feedback inhibition, negative regulatory function in absence or presence of Ca2+; IC50 is 0.010 mM	Homo sapiens
bradykinin	-	Homo sapiens
Ca2+	inhibits activity with Gln-substrate, regulatory function and influence on substrate specificity	Homo sapiens
cholecystokinin-8	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.024 mM in presence of Ca2+	Homo sapiens
chromogranin A	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.049 mM in presence of Ca2+	Homo sapiens
E64	slight inhibition at 1 mM	Homo sapiens
kallidin	competitive against Glu-4-methylcoumaryl-7-amide	Homo sapiens
leupeptin	slight inhibition at 1 mM	Homo sapiens
Met-enkephalin	-	Homo sapiens
Mg2+	inhibits the activity with Glu-substrate moderately	Homo sapiens
Mn2+	inhibits the activity with Glu-substrate moderately	Homo sapiens
additional information	inhibitory effects of peptide hormones on enzyme activity in presence or absence of Ca2+, overview, no or poor inhibition by 4-(amidinophenyl)-methanesulfonyl fluoride, pepstatin, and bestatin	Homo sapiens
Neurokinin A	-	Homo sapiens
neurokinin B	competitive against Glu-4-methylcoumaryl-7-amide,IC50 is 0.060 mM in presence of Ca2+	Homo sapiens
parathyroid hormone residues 69-84	-	Homo sapiens
Substance P	-	Homo sapiens
Zn2+	zinc-metallopeptidase, inhibits the activity with Glu- and Gln-substrates	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism
additional information	-	additional information	kinetics and substrate specificity in presence or absence of Ca2+	Homo sapiens
0.4	-	Glu-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens
0.6	-	Gln-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
1.2	-	Glu-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
1.4	-	Asp-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens
2.3	-	Asp-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
7.1	-	Gln-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
membrane	type II membrane-bound enzyme, membrane-spanning	Homo sapiens	16020	-

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Ca2+	activates activity with some substrates, decreases activity with other substrates, required for activity with Asp-/Glu-substrates, regulatory function and influence on substrate specificity	Homo sapiens
Zn2+	zinc-metallopeptidase, inhibits the activity with Glu- and Gln-substrates	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.
angiotensin II + H2O	Homo sapiens	angiotensin is the most active compound of the renin-angiotensin-system, RAS, involved in regulation of blood pressure in the brain	Asp + angiotensin III	-	?
cholecystokinin-8 + H2O	Homo sapiens	i.e. CCK8	?	-	?
chromogranin A + H2O	Homo sapiens	-	?	-	?
neurokinin B + H2O	Homo sapiens	-	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
glycoprotein	-	Homo sapiens

Purification (Commentary)

Purification (Comment)	Organism
recombinant soluble enzyme His-tagged from Sf9 insect cells to homogeneity by ultrafiltration, dialysis, anion exchange and cobalt affinity chromatography	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
brain	-	Homo sapiens	-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg]	Specific Activity Maximum [µmol/min/mg]	Comment	Organism
additional information	-	-	Homo sapiens

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.
angiotensin II + H2O	angiotensin is the most active compound of the renin-angiotensin-system, RAS, involved in regulation of blood pressure in the brain	Homo sapiens	Asp + angiotensin III	-	?
angiotensin II + H2O	i.e. Asp-Tyr-Arg-Val-Tyr-Ile-His-Pro-Phe	Homo sapiens	Asp + angiotensin III	i.e. Tyr-Arg-Val-Tyr-Ile-His-Pro-Phe	?
angiotensin III + H2O	i.e. Tyr-Arg-Val-Tyr-Ile-His-Pro-Phe, low activity in absence of Ca2+	Homo sapiens	? + angiotensin IV	-	?
Asp-4-methylcoumaryl-7-amide + H2O	low activity in absence and presence of Ca2+	Homo sapiens	Asp + 7-amino-4-methylcoumarin	-	?
cholecystokinin-8 + H2O	i.e. CCK8	Homo sapiens	?	-	?
cholecystokinin-8 + H2O	i.e. CCK8 or DYMGWMDF-NH2	Homo sapiens	Asp + YMGWMDF-NH2	-	?
chromogranin A + H2O	-	Homo sapiens	?	-	?
chromogranin A + H2O	i.e. EEEEEMAVVPQGLFRG-NH2	Homo sapiens	Glu + EEEEMAVVPQGLFRG-NH2	-	?
Gln-4-methylcoumaryl-7-amide + H2O	low activity in absence and presence of Ca2+	Homo sapiens	Gln + 7-amino-4-methylcoumarin	-	?
Glu-4-methylcoumaryl-7-amide + H2O	low activity in absence of Ca2+	Homo sapiens	Glu + 7-amino-4-methylcoumarin	-	?
kallidin + H2O	i.e. Lys-bradykinin or KRPPGFSPFR, the reaction is performed only in absence of Ca2+	Homo sapiens	Lys + bradykinin	i.e. RPPGFSPFR	?
additional information	substrate specificity in presence or absence of Ca2+	Homo sapiens	?	-	?
neurokinin B + H2O	-	Homo sapiens	?	-	?
neurokinin B + H2O	i.e. DMHDFFVGLM-NH2	Homo sapiens	Asp + MHDFFVGLM-NH2	-	?

Subunits

Subunits	Comment	Organism
dimer	-	Homo sapiens

Synonyms

Synonyms	Comment	Organism
aminopeptidase A	-	Homo sapiens
APA	-	Homo sapiens
More	the enzyme belongs to the M1 family	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism
2.8	-	Asp-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
9.5	-	Gln-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
12.2	-	Asp-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens
13.3	-	Glu-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in absence of Ca2+	Homo sapiens
14.1	-	Gln-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens
33.3	-	Glu-4-methylcoumaryl-7-amide	recombinant enzyme, pH 7.5, 37°C, in presence of 1 mM Ca2+	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7	-	-	Homo sapiens

pH Range

pH Minimum	pH Maximum	Comment	Organism
additional information	-	pH-profile, recombinant enzyme	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.000157	-	IC50 is 157 nM	Homo sapiens	amastatin
0.01	-	IC50 is 0.010 mM	Homo sapiens	angiotensin IV
0.024	-	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.024 mM in presence of Ca2+	Homo sapiens	cholecystokinin-8
0.049	-	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.049 mM in presence of Ca2+	Homo sapiens	chromogranin A
0.06	-	competitive against Glu-4-methylcoumaryl-7-amide,IC50 is 0.060 mM in presence of Ca2+	Homo sapiens	neurokinin B
0.06	-	IC50 is 0.06 mM	Homo sapiens	1,10-phenanthroline
0.065	-	competitive against Glu-4-methylcoumaryl-7-amide, IC50 is 0.065 mM in presence of Ca2+	Homo sapiens	angiotensin II