Nucleic Acids as a Nature-Inspired Scaffold for Macromolecular Prodrugs of Nucleoside Analogues.

Franziska Krüger,Alexander N Zelikin,Nikaïa Smith,Kurt V Gothelf,Vipin Kumar,Carina Conzelmann,Jan Münch,Pere Monge,Martin Tolstrup

doi:10.1002/advs.201802095

Abstract

Macromolecular prodrugs (MP) built on the natural phosphodiester and deoxyribose backbone are developed using marketed antiviral nucleoside analogues. These MP are synthesized using automated synthesis, have defined molecular composition, and have a natural mechanism for drug release. These unique attributes, coupled to the efficient cell entry and potent antiviral effects, position the prodrugs scaffolded on nucleic acids favorably for translational studies.

Highlights

Macromolecular prodrugs (MP) built on the natural phosphodiester and and the current front-runner MP in translational studies is based on deoxyribose backbone are developed using marketed antiviral nucleoside poly(glutamic acid).[6]
Nucleic acids are sibly comprised of different nucleoside analogues to make up a highly warranted in biomedicine, biotechnology, and nano- combination therapy
We offer a new prospect on nucleic acids is undefined and hypothesize that these form a unique scaffold for macro- and remains highly appealing

Summary

Introduction

Macromolecular prodrugs (MP) built on the natural phosphodiester and and the current front-runner MP in translational studies is based on deoxyribose backbone are developed using marketed antiviral nucleoside poly(glutamic acid).[6]. Nucleic acid scaffolds offer a fully natural mechanism for degradation and drug release. Www.advancedsciencenews.com www.advancedscience.com analyses revealed that degradation of TNA affords the expected nucleosides (thymidine, trifluridine, or idoxuridine) as the main product of natural oligomer decomposition (Figure 1F), providing the final element of validation of the composition for TNA.

Results

Conclusion