Microplate-based screening for small molecule inhibitors of neuropilin-2/vascular endothelial growth factor-C interactions

Matthew W. Parker, Craig W. Vander Kooi

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

Vascular endothelial growth factor-C (VEGF-C) is a secreted growth factor essential for lymphangiogenesis. VEGF-C functions in both physiological and pathological lymphangiogenesis, particularly in tumor metastasis, making it an attractive therapeutic target. Members of two families of cell surface receptors transduce VEGF-C signals: neuropilin-2 (Nrp2) and VEGF-receptor (VEGFR)-2/3. Nrp2 is a promising target for inhibition because it is highly expressed in lymphatic vessels. Here we describe a microplate-based assay for discovery of VEGF-C/Nrp2 inhibitors. We optimize this assay for use in screening an inhibitor library and identify three novel Nrp2/VEGF-C binding inhibitors from the National Institutes of Health (NIH) Clinical Collection small molecule library.

Original languageEnglish (US)
Pages (from-to)4-6
Number of pages3
JournalAnalytical biochemistry
Volume453
Issue number1
DOIs
StatePublished - May 15 2014
Externally publishedYes

Keywords

  • Assay
  • Inhibitor
  • Ligand
  • Neuropilin
  • Receptor
  • VEGF

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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