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Synthesis and characterization of valyloxy methoxy luciferin for the detection of valacyclovirase and peptide transporter.

ABSTRACT: An amino acid ester derivative of luciferin (valoluc) was synthesized to mimic the transport and activation of valacyclovir. This molecule was characterized in vitro for specificity and enzymatic constants, and then assayed in two different, physiologically-relevant conditions. It was demonstrated that valoluc activation is sensitive to the same cellular factors as valacyclovir and thus has the potential to elucidate the dynamics of amino acid ester prodrug therapies in a functional, high-throughput manner.

SUBMITTER: Walls ZF

PROVIDER: S-EPMC4192071 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature

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Synthesis and characterization of valyloxy methoxy luciferin for the detection of valacyclovirase and peptide transporter.

Walls Zachary F ZF Gupta Sheeba Varghese SV Amidon Gordon L GL Lee Kyung-Dall KD

Bioorganic & medicinal chemistry letters 20140916 20

An amino acid ester derivative of luciferin (valoluc) was synthesized to mimic the transport and activation of valacyclovir. This molecule was characterized in vitro for specificity and enzymatic constants, and then assayed in two different, physiologically-relevant conditions. It was demonstrated that valoluc activation is sensitive to the same cellular factors as valacyclovir and thus has the potential to elucidate the dynamics of amino acid ester prodrug therapies in a functional, high-throug ...[more]

PMID: 25240255

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