Synthesis and in vitro characterization of glycopeptide drug candidates related to pacap1–23

Christopher R. Apostol, Parthasaradhireddy Tanguturi, Lajos Z. Szabò, Daniel Varela, Thiago Gilmartin, John M. Streicher, Robin Polt

Research output: Contribution to journalArticlepeer-review

Abstract

The search for efficacious treatment of neurodegenerative and progressive neuroinflammatory diseases continues, as current therapies are unable to halt or reverse disease progression. PACAP represents one potential therapeutic that provides neuroprotection effects on neurons, and also modulates inflammatory responses and circulation within the brain. However, PACAP is a relatively long peptide hormone that is not trivial to synthesize. Based on previous observations that the shortened isoform PACAP1–23 is capable of inducing neuroprotection in vitro, we were inspired to synthesize shortened glycopeptide analogues of PACAP1–23 . Herein, we report the synthesis and in vitro characterization of glycosylated PACAP1–23 analogues that interact strongly with the PAC1 and VPAC1 receptors, while showing reduced activity at the VPAC2 receptor.

Original languageEnglish (US)
Article number4932
JournalMolecules
Volume26
Issue number16
DOIs
StatePublished - Aug 2 2021

Keywords

  • Alzheimer’s
  • Glycopeptide
  • Glycosylation
  • Parkinson’s
  • Stroke

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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