Structure activity relationship, 6-modified purine riboside analogues to activate hSTING, stimulator of interferon genes

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2 Scopus citations

Abstract

Twenty-nine nucleoside analogues have been synthesized and evaluated in a cell based assay for their ability to activate the human Stimulator of Interferon Genes (hSTING), a key protein of the innate immune defense. Some 6-O-alkyl nucleoside analogues activate hSTING without associated cytotoxicity. SAR and combination studies were performed to decipher possible activation mechanism. The described nucleoside hSTING activators represent first-in-class modulators of the innate immune defense; a highly relevant target for antiviral, antibacterial, anticancer or Alzheimer's disease treatments and may present advantages over other types of hSTING activators.

Original languageEnglish (US)
Article number126819
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number2
DOIs
StatePublished - Jan 15 2020

Bibliographical note

Funding Information:
This research was supported by the Center for Drug Design, College of Pharmacy, University of Minnesota . Appendix A

Publisher Copyright:
© 2019 Elsevier Ltd

Keywords

  • Cell based assay
  • hSTING activation
  • Innate immune response
  • Interferons
  • Nucleoside analogues

PubMed: MeSH publication types

  • Journal Article
  • Research Support, Non-U.S. Gov't

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