Premium
Cover Feature: A pH‐sensitive Macromolecular Prodrug as TLR7/8 Targeting Immune Response Modifier (Chem. Eur. J. 70/2017)
Author(s) -
Aichhorn Stefan,
Linhardt Anne,
Halfmann Angela,
Nadlinger Markus,
Kirchberger Stefanie,
Stadler Manuela,
Dillinger Barbara,
Distel Martin,
Dohnal Alexander,
Teasdale Ian,
Schöfberger Wolfgang
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201704767
Subject(s) - prodrug , chemistry , endosome , macromolecule , tlr7 , in vivo , inflammation , toll like receptor , combinatorial chemistry , biochemistry , receptor , biology , innate immune system , immunology , microbiology and biotechnology
The chemical synthesis and biological activity of new functionalized imidazoquinoline derivatives (ImQ) to generate Toll‐like receptor (TLR) 7/8 specific prodrugs are presented. In vivo activity of ImQs to induce inflammation was confirmed in zebrafish larvae. After covalent ligation to fully biodegradable polyphosphazenes (ImQ‐polymer), the macromolecular prodrugs were designed to undergo intracellular pH‐sensitive release of ImQs to induce inflammation through binding to endosomal TLR7/8. More information can be found in the Full Paper by M. Distel, A. Dohnal, I. Teasdale, W. Schöfberger et al. on page 17721.