The all-D-configuration segment containing the IKVAV sequence of laminin A chain has similar activities to the all-L-peptide in vitro and in vivo

J Biol Chem. 1992 Jul 15;267(20):14118-21.

Abstract

Laminin is a basement membrane glycoprotein that has diverse biological activities. A sequence on the A chain containing IKVAV (Ile-Lys-Val-Ala-Val) has been shown to promote neurite outgrowth, cell adhesion, and tumor growth and metastasis. Here we have determined the structural requirements of this synthetic peptide for biological activity. Twelve-amino acid-long all-L- (LAM-L) and all-D-peptide (LAM-D) segments as well as an alternating D- and L-amino acid-containing peptide (LAM-DL), which included the IKVAV sequence (residues 2097-2108), were synthesized. Circular dichroism spectral analysis revealed a mirror image conformation of LAM-D and LAM-L with mainly beta-sheet and to a minor extent alpha-helical structure. LAM-DL did not exhibit any significant ordered conformational features. LAM-D and LAM-L showed similar cell attachment activities for rat pheochromocytoma cells (PC12), whereas LAM-DL was inactive. A peptide analog with randomized IKVAV sequence (LAM-RM) was also inactive. A similar trend was observed in competition experiments of the four peptides with laminin in analogous cell attachment assays. In in vivo experiments, both LAM-D and LAM-L were capable of increasing tumor growth when subcutaneously injected into mice with murine melanoma cells B16F10. Results indicate that the conformational status of the IKVAV domain is a contributing factor in determining the biological activity but that there is no strict requirement for a specific chirality. There is a likely sequence specificity to the IKVAV region.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cell Adhesion / drug effects*
  • Cell Division / drug effects
  • Circular Dichroism
  • Kinetics
  • Laminin / chemistry*
  • Laminin / pharmacology
  • Macromolecular Substances
  • Melanoma, Experimental / pathology*
  • Mice
  • Mice, Inbred C57BL
  • Molecular Sequence Data
  • PC12 Cells
  • Peptide Fragments / chemistry*
  • Peptide Fragments / pharmacology
  • Peptides / chemical synthesis*
  • Peptides / pharmacology
  • Protein Conformation
  • Structure-Activity Relationship

Substances

  • Laminin
  • Macromolecular Substances
  • Peptide Fragments
  • Peptides