Synthesis and evaluation of locostatin-based chemical probes towards PEBP-proteins

Jorin Hoogenboom, Martijn Fiers, Richard Immink, Han Zuilhof, Tom Wennekes*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

2 Citations (Scopus)

Abstract

Phosphatidyl ethanolamine-binding proteins (PEBPs) are implicated in various critical physiological processes in all eukaryotes. Among them is Flowering Locus T (FT), the protein recently discovered as the vital flowering hormone in plants. Small molecule inhibitors and activators of FT could provide control over plant flowering and are therefore an interesting target for industrial agriculture. No small molecule inhibitors or activators are known for FT, but for a structurally similar PEBP, RKIP, an inhibitor called locostatin has been reported to covalently bind in the RKIP ligand binding pocket. Herein, we report the synthesis of novel locostatin-based chemical PEBP probes and evaluate their ability and selectivity towards the binding of FT and RKIP.

Original languageEnglish
Pages (from-to)2406-2409
JournalTetrahedron Letters
Volume57
Issue number22
DOIs
Publication statusPublished - 2016

Keywords

  • Chemical probes
  • Flowering Locus T
  • Inhibitor
  • Locostatin
  • PEBP
  • RKIP

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