Functionalized Acyclic (l)‐Threoninol Nucleic Acid Four‐Way Junction with High Stability In Vitro and In Vivo

Abstract: Oligonucleotides are increasingly being used as a programmable connection material to assemble molecules and proteins in well‐defined structures. For the application of such assemblies for in vivo diagnostics or therapeutics it is crucial that the oligonucleotides form highly stable, non‐toxic, and non‐immunogenic structures. Only few oligonucleotide derivatives fulfil all of these requirements. Here we report on the application of acyclic l‐threoninol nucleic acid (aTNA) to form a four‐way junction (4WJ) that is highly stable and enables facile assembly of components for in vivo treatment and imaging. The aTNA 4WJ is serum‐stable, shows no non‐targeted uptake or cytotoxicity, and invokes no innate immune response. As a proof of concept, we modify the 4WJ with a cancer‐targeting and a serum half‐life extension moiety and show the effect of these functionalized 4WJs in vitro and in vivo, respectively.

Object Details

• Location: Deutsche Nationalbibliothek Frankfurt am Main
• Extent: Online-Ressource
• Language: Englisch

References and Relationships

• Bibliographic citation: Functionalized Acyclic (l)‐Threoninol Nucleic Acid Four‐Way Junction with High Stability In Vitro and In Vivo ; day:13 ; month:04 ; year:2022 ; extent:1 ; Angewandte Chemie / International edition. International edition ; (13.04.2022) (gesamt 1)

Contributors, Places and Time

• Creator: Märcher, Anders ; Kumar, Vipin ; Andersen, Veronica L. ; El‐Chami, Kassem ; Nguyen, Thuy J. D. ; Skaanning, Mads K. ; Rudnik‐Jansen, Imke ; Nielsen, Jesper S. ; Howard, Kenneth A. ; Kjems, Jørgen ; Gothelf, Kurt V.

Further information

• DOI: 10.1002/anie.202115275
• URN: urn:nbn:de:101:1-2022041415123295436922
• Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
• Last update: 15.08.2025, 7:28 AM CEST