A stapled chromogranin A-derived peptide is a potent dual ligand for integrins αvβ6 and αvβ8

Chem Commun (Camb). 2019 Dec 5;55(98):14777-14780. doi: 10.1039/c9cc08518a.

Abstract

Combining 2D STD-NMR, computation, biochemical assays and click-chemistry, we have identified a chromogranin-A derived compound (5) that has high affinity and bi-selectivity for αvβ6 and αvβ8 integrins and is stable in microsomal preparations. 5 is suitable for nanoparticle functionalization and delivery to cancer cells, holding promise for diagnostic and/or therapeutic applications.

MeSH terms

  • Amino Acid Sequence
  • Antigens, Neoplasm / metabolism*
  • Cell Line, Tumor
  • Chromogranin A / chemistry*
  • Humans
  • Integrins / antagonists & inhibitors
  • Integrins / metabolism*
  • Ligands
  • Microscopy, Fluorescence
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptides / chemistry
  • Peptides / metabolism*
  • Protein Binding

Substances

  • Antigens, Neoplasm
  • Chromogranin A
  • Integrins
  • Ligands
  • Peptides
  • integrin alphavbeta6
  • integrin alphavbeta8