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Literature summary extracted from

  • Sun, J.; Dahan, A.; Amidon, G.
    Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: A double-targeted prodrug approach (2010), J. Med. Chem., 53, 624-632.
    View publication on PubMedView publication on EuropePMC

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.43 0.009
-
 4-carbamimidamidobenzyl L-isoleucinate pH 7.4, 37°C Homo sapiens
3.1.1.43 0.046
-
 4-carbamimidamidobenzyl L-valinate pH 7.4, 37°C Homo sapiens
3.1.1.43 0.068
-
 valacyclovir pH 7.4, 37°C Homo sapiens
3.1.1.43 0.207
-
 4-carbamimidamidobenzyl L-phenylalaninate pH 7.4, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.43 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.43 Caco-2 cell
-
 Homo sapiens
-
3.1.1.43 HeLa cell
-
 Homo sapiens
-
3.1.1.43 small intestine
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.43 4-carbamimidamidobenzyl L-isoleucinate + H2O
-
 Homo sapiens L-isoleucine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
3.1.1.43 4-carbamimidamidobenzyl L-phenylalaninate + H2O
-
 Homo sapiens L-phenylalanine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
3.1.1.43 4-carbamimidamidobenzyl L-valinate + H2O
-
 Homo sapiens L-valine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
3.1.1.43 additional information all the L-amino acid 1-[4-(hydroxymethyl)phenyl]guanidine esters are effectively activated in HeLa and Caco-2 cell homogenates and are found to be good substrates of hVACVase. Substrate affinities for human peptide transporter 1, overview Homo sapiens ?
-
 ?
3.1.1.43 valacyclovir + H2O
-
 Homo sapiens L-valine + 2-amino-9-[(2-hydroxyethyloxy)methyl]-1,9-dihydro-6H-purin-6-one
-
 ?
3.1.1.43 valganciclovir + H2O
-
 Homo sapiens L-valine + 2-amino-9-[[(1,3-dihydroxpropan-2-yl)oxy]methyl]-1,9-dihydro-6H-purin-6-one
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.43 VACVase
-
 Homo sapiens
3.1.1.43 valacyclovirase
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.1.43 14
-
 4-carbamimidamidobenzyl L-isoleucinate pH 7.4, 37°C Homo sapiens
3.1.1.43 58
-
 valacyclovir pH 7.4, 37°C Homo sapiens
3.1.1.43 154
-
 4-carbamimidamidobenzyl L-valinate pH 7.4, 37°C Homo sapiens
3.1.1.43 345
-
 4-carbamimidamidobenzyl L-phenylalaninate pH 7.4, 37°C Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.1.1.43 850
-
 valacyclovir pH 7.4, 37°C Homo sapiens
3.1.1.43 1580
-
 4-carbamimidamidobenzyl L-isoleucinate pH 7.4, 37°C Homo sapiens
3.1.1.43 1660
-
 4-carbamimidamidobenzyl L-phenylalaninate pH 7.4, 37°C Homo sapiens
3.1.1.43 3370
-
 4-carbamimidamidobenzyl L-valinate pH 7.4, 37°C Homo sapiens