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Fluorescing Isofunctional Ribonucleosides: Assessing Adenosine Deaminase Activity and Inhibition.


ABSTRACT: The enzymatic conversion of isothiazolo[4,3-d]pyrimidine-based adenosine (tz A) and 2-aminoadenosine (tz 2-AA) analogues to the corresponding isothiazolo[4,3-d]pyrimidine-based inosine (tz I) and guanosine (tz G) derivatives is evaluated and compared to the conversion of native adenosine to inosine. Henri-Michaelis-Menten analyses provides the foundation for a high-throughput screening assay, and the efficacy of the assay is showcased by fluorescence-based analysis of tz A conversion to tz I in the presence of known and newly synthesized inhibitors.

SUBMITTER: Ludford PT 

PROVIDER: S-EPMC6467514 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Fluorescing Isofunctional Ribonucleosides: Assessing Adenosine Deaminase Activity and Inhibition.

Ludford Paul T PT   Rovira Alexander R AR   Fin Andrea A   Tor Yitzhak Y  

Chembiochem : a European journal of chemical biology 20190221 5


The enzymatic conversion of isothiazolo[4,3-d]pyrimidine-based adenosine (<sup>tz</sup> A) and 2-aminoadenosine (<sup>tz</sup> 2-AA) analogues to the corresponding isothiazolo[4,3-d]pyrimidine-based inosine (<sup>tz</sup> I) and guanosine (<sup>tz</sup> G) derivatives is evaluated and compared to the conversion of native adenosine to inosine. Henri-Michaelis-Menten analyses provides the foundation for a high-throughput screening assay, and the efficacy of the assay is showcased by fluorescence-b  ...[more]

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