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

Authors :: Walls ZF
Gupta SV
Amidon GL
Lee KD
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Oct 15; Vol. 24 (20), pp. 4781-4783. Date of Electronic Publication: 2014 Sep 16.
Publication Year :: 2014
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.<br /> (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Subjects :: Bacteria metabolism
Biological Transport
Carboxylic Ester Hydrolases metabolism
Firefly Luciferin chemical synthesis
HEK293 Cells
High-Throughput Screening Assays
Humans
Hydrolysis
Luminescence
Membrane Transport Proteins metabolism
Molecular Structure
Species Specificity
Carboxylic Ester Hydrolases analysis
Firefly Luciferin analogs & derivatives
Firefly Luciferin chemistry
Membrane Transport Proteins analysis

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