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Literature summary for 1.14.17.3 extracted from

  • Morris, K.M.; Cao, F.; Onagi, H.; Altamore, T.M.; Gamble, A.B.; Easton, C.J.
    Prohormone-substrate peptide sequence recognition by peptidylglycine alpha-amidating monooxygenase and its reflection in increased glycolate inhibitor potency (2012), Bioorg. Med. Chem. Lett., 22, 7015-7018.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(acetyloxy)acetic acid
-
Homo sapiens
([(2S)-2-[(2-aminopropanoyl)amino]-3-phenylpropanoyl]oxy)acetic acid
-
Homo sapiens
([N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]-L-phenylalanyl]oxy)acetic acid
-
Homo sapiens
([N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]glycyl]oxy)acetic acid
-
Homo sapiens
([[(2S)-1-(2-aminopropanoyl)pyrrolidin-2-yl]carbonyl]oxy)acetic acid
-
Homo sapiens
([[(2S)-1-[[(2-aminopropanoyl)amino]acetyl]pyrrolidin-2-yl]carbonyl]oxy)acetic acid
-
Homo sapiens
([[(4-amino-6-methyl-3-oxoheptanoyl)amino]acetyl]oxy)acetic acid
-
Homo sapiens
[[(2S)-2-(acetylamino)-3-phenylpropanoyl]oxy]acetic acid
-
Homo sapiens
[[(2S)-2-([[(2-aminopropanoyl)amino]acetyl]amino)-3-phenylpropanoyl]oxy]acetic acid
-
Homo sapiens
[[(2S)-2-amino-3-phenylpropanoyl]oxy]acetic acid
-
Homo sapiens
[[(2S)-pyrrolidin-2-ylcarbonyl]oxy]acetic acid
-
Homo sapiens
[[(acetylamino)acetyl]oxy]acetic acid
-
Homo sapiens
[[N-(4-amino-6-methyl-3-oxoheptanoyl)-L-phenylalanyl]oxy]acetic acid
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.007
-
N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.011
-
N-(4-amino-6-methyl-3-oxoheptanoyl)-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.016
-
N-acetyl-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.018
-
alanylglycylvalyl-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.035
-
alanylglycyl-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.2
-
alanyl-L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
0.55
-
N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]glycylglycine pH and temperature not specified in the publication Homo sapiens
0.86
-
N-(4-amino-6-methyl-3-oxoheptanoyl)glycylglycine pH and temperature not specified in the publication Homo sapiens
0.88
-
L-prolylglycine pH and temperature not specified in the publication Homo sapiens
0.96
-
alanylglycylvalyl-L-prolylglycine pH and temperature not specified in the publication Homo sapiens
1.2
-
N-acetylglycylglycine pH and temperature not specified in the publication Homo sapiens
3
-
alanylglycyl-L-prolylglycine pH and temperature not specified in the publication Homo sapiens
4
-
alanyl-L-prolylglycine pH and temperature not specified in the publication Homo sapiens
6.5
-
L-phenylalanylglycine pH and temperature not specified in the publication Homo sapiens
9.9
-
N-acetylglycine pH and temperature not specified in the publication Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Cu2+ required for activity Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
peptidylglycine + ascorbate + O2 Homo sapiens
-
peptidyl(2-hydroxyglycine) + dehydroascorbate + H2O
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DMS-53 cell
-
Homo sapiens
-
small cell lung cancer cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
alanyl-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
alanyl-L-prolylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
alanylglycyl-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
alanylglycyl-L-prolylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
alanylglycylvalyl-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
alanylglycylvalyl-L-prolylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
L-prolylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
additional information the enzyme peptidylglycine alpha-amidating monooxygenase consists of two subunits: peptidylglycine alpha-hydroxylating monooxygenase that initiates formation of a radical at a substrate's C-terminal glycine alpha-carbon to then give an alpha-hydroxylated glycine derivative, and peptidylamidoglycolate lyase which catalyzes cleavage of this hydroxyglycine intermediate to give the amidated product with consequent release of glyoxylate Homo sapiens ?
-
?
N-(4-amino-6-methyl-3-oxoheptanoyl)-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-(4-amino-6-methyl-3-oxoheptanoyl)glycylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-acetyl-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-acetylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-acetylglycylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]-L-phenylalanylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]glycylglycine + ascorbate + O2
-
Homo sapiens ? + dehydroascorbate + H2O
-
?
peptidylglycine + ascorbate + O2
-
Homo sapiens peptidyl(2-hydroxyglycine) + dehydroascorbate + H2O
-
?

Synonyms

Synonyms Comment Organism
PAM
-
Homo sapiens
peptidylglycine alpha-amidating monooxygenase
-
Homo sapiens
peptidylglycine alpha-hydroxylating monooxygenase
-
Homo sapiens
PHM
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ascorbate
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.009
-
pH and temperature not specified in the publication Homo sapiens [[N-(4-amino-6-methyl-3-oxoheptanoyl)-L-phenylalanyl]oxy]acetic acid
0.011
-
pH and temperature not specified in the publication Homo sapiens [[(2S)-2-(acetylamino)-3-phenylpropanoyl]oxy]acetic acid
0.038
-
pH and temperature not specified in the publication Homo sapiens ([N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]-L-phenylalanyl]oxy)acetic acid
0.16
-
pH and temperature not specified in the publication Homo sapiens [[(2S)-2-([[(2-aminopropanoyl)amino]acetyl]amino)-3-phenylpropanoyl]oxy]acetic acid
0.18
-
pH and temperature not specified in the publication Homo sapiens ([N-[3-(1-leucylpyrrolidin-2-yl)-3-oxopropanoyl]glycyl]oxy)acetic acid
0.2
-
pH and temperature not specified in the publication Homo sapiens ([[(4-amino-6-methyl-3-oxoheptanoyl)amino]acetyl]oxy)acetic acid
0.29
-
pH and temperature not specified in the publication Homo sapiens ([[(2S)-1-(2-aminopropanoyl)pyrrolidin-2-yl]carbonyl]oxy)acetic acid
0.37
-
pH and temperature not specified in the publication Homo sapiens ([(2S)-2-[(2-aminopropanoyl)amino]-3-phenylpropanoyl]oxy)acetic acid
0.5
-
pH and temperature not specified in the publication Homo sapiens [[(2S)-pyrrolidin-2-ylcarbonyl]oxy]acetic acid
1.1
-
pH and temperature not specified in the publication Homo sapiens (acetyloxy)acetic acid
1.1
-
pH and temperature not specified in the publication Homo sapiens ([[(2S)-1-[[(2-aminopropanoyl)amino]acetyl]pyrrolidin-2-yl]carbonyl]oxy)acetic acid
1.6
-
pH and temperature not specified in the publication Homo sapiens [[(2S)-2-amino-3-phenylpropanoyl]oxy]acetic acid
1.8
-
pH and temperature not specified in the publication Homo sapiens [[(acetylamino)acetyl]oxy]acetic acid