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Literature summary for 3.1.1.43 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
Search for more literature for 3.1.1.43

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-carbamimidamidobenzyl L-isoleucinate + H2O
-
 Homo sapiens L-isoleucine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
4-carbamimidamidobenzyl L-phenylalaninate + H2O
-
 Homo sapiens L-phenylalanine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
4-carbamimidamidobenzyl L-valinate + H2O
-
 Homo sapiens L-valine + 1-[4-(hydroxymethyl)phenyl]guanidine
-
 ?
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 ?
-
 ?
valacyclovir + H2O
-
 Homo sapiens L-valine + 2-amino-9-[(2-hydroxyethyloxy)methyl]-1,9-dihydro-6H-purin-6-one
-
 ?
valganciclovir + H2O
-
 Homo sapiens L-valine + 2-amino-9-[[(1,3-dihydroxpropan-2-yl)oxy]methyl]-1,9-dihydro-6H-purin-6-one
-
 ?

Synonyms

Synonyms Comment Organism
VACVase
-
 Homo sapiens
valacyclovirase
-
 Homo sapiens

Turnover Number [1/s]

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

kcat/KM [mM/s]

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