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