BPHL hydrolyses VACV to ACV

Stable Identifier
Reaction [transition]
Homo sapiens
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Valacyclovir (VACV) is the 5'-valyl ester prodrug of acyclovir (ACV), an effective anti-herpetic drug. Systemic bioavailability of ACV in humans is up to five times higher when administered orally as the prodrug. After intestinal absorption, valacyclovir hydrolase (BPHL) mediates the rapid and complete hydrolysis to VACV to ACV (Kim et al. 2003, Lai et al. 2008). The subcellular location of human BPHL is unknown but rat Bhpl localises to the mitochondrial membrane (Kim et al. 2003).

Literature References
PubMed ID Title Journal Year
18256025 Molecular basis of prodrug activation by human valacyclovirase, an alpha-amino acid ester hydrolase

Amidon, GL, Lee, KD, Xu, Z, Zhou, J, Lai, L

J. Biol. Chem. 2008
12732646 Identification of a human valacyclovirase: biphenyl hydrolase-like protein as valacyclovir hydrolase

Kim, S, Amidon, GL, Lee, KD, Provoda, CJ, Chu, XY, Kim, I

J. Biol. Chem. 2003
Catalyst Activity

alpha-amino-acid esterase activity of BPHL [mitochondrial outer membrane]

Orthologous Events
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