Fluorescing Isofunctional Ribonucleosides: Assessing Adenosine Deaminase Activity and Inhibition |
| |
| Authors: | Paul T. Ludford III Alexander R. Rovira Andrea Fin Prof. Dr. Yitzhak Tor |
| |
| Affiliation: | Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA, 92093-0358 USA |
| |
| Abstract: | The enzymatic conversion of isothiazolo[4,3-d]pyrimidine-based adenosine (tzA) and 2-aminoadenosine (tz2-AA) analogues to the corresponding isothiazolo[4,3-d]pyrimidine-based inosine (tzI) and guanosine (tzG) 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 tzA conversion to tzI in the presence of known and newly synthesized inhibitors. |
| |
| Keywords: | adenosine adenosine deaminase enzyme catalysis high-throughput screening inhibitors |
|
|
