April 4, 2008Nucleosides Nucleotides & Nucleic Acids

Acyclic Phosphonate Nucleotides and Human Adenylate Kinases: Impact of a Borano Group on α-P Position

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Structured PICO

Population

Recombinant human AMP kinases 1 and 2 (in vitro model)

Intervention

PMEA and PMPA bearing a borano- or a H- group on the phosphorus atom

Outcome

In vitro phosphorylation activitysurrogate

The addition of an alpha-borano or alpha-H group to PMEA and PMPA impairs their phosphorylation by human AMP kinases 1 and 2, likely due to disruption of critical arginine interactions.

Authors

DTDimitri TopalisCentre National de la Recherche Scientifique KAKarine AlvarezCentre National de la Recherche Scientifique KBKarine BarralCentre National de la Recherche Scientifique

Discussion

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Implication

These modifications may hinder PMEA/PMPA activation in humans; leaves open optimal designs for kinase-dependent nucleotide analogs.

Cite This Study

Topalis et al. (2008) studied this question.

synapsesocial.com/papers/6a8d16cee44cc01ba0daca67 https://doi.org/10.1080/15257770801941952

View Full Paper

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Acyclic Phosphonate Nucleotides and Human Adenylate Kinases: Impact of a Borano Group on α-P Position

Structured PICO

Discussion

Implication

Cite This Study

Acyclic Phosphonate Nucleotides and Human Adenylate Kinases: Impact of a Borano Group on α-P Position

Structured PICO

Discussion

Implication

Cite This Study

Also Consider

Also Consider