Structural and inhibitory properties of a plant proteinase inhibitor containing the RGD motif

Int J Biol Macromol. 2006 Dec 15;40(1):22-9. doi: 10.1016/j.ijbiomac.2006.05.008. Epub 2006 May 26.

Abstract

Purified from Bauhinia rufa seeds, BrTI is a Kunitz proteinase inhibitor that contains the RGD sequence. BrTI inhibits trypsin (K(iapp) 2.9 nM) and human plasma kallikrein (K(iapp) 14.0 nM) but not other related enzymes. The synthetic peptide YLEPVARGDGGLA-NH(2) (70 microM) inhibited the adhesion to fibronectin of B16F10 (high-metastatic B16 murine mouse melanoma cell line) and of Tm5 (murine melanoma cell lines derived from a non-tumorigenic lineage of pigmented murine melanocytes, melan-a). YLEPVARGEGGLA-NH(2) in which Asp(9) was changed into Glu does not affect the cell attachment. Moreover, this peptide was functional only when the sequence present in the native protein was preserved, since YLIPVARGDGGLA-NH(2) in which Glu(3) was changed into Ile does not interfere with B16F10 and was less effective on Tm5 cell line adhesion. Neither YLEPVARGDGGLA-NH(2), YLIPVARGDGGLA-NH(2) or YLEPVARGEGGLA-NH(2) inhibit the interaction of RAEC (endothelial cell line from rabbit aorta) with fibronectin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Bauhinia / chemistry*
  • Bauhinia / genetics
  • Cell Adhesion / drug effects
  • Cell Line, Tumor
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects
  • Humans
  • In Vitro Techniques
  • Kallikreins / antagonists & inhibitors
  • Melanoma, Experimental / drug therapy
  • Mice
  • Molecular Sequence Data
  • Oligopeptides
  • Peptides / chemistry*
  • Peptides / genetics
  • Peptides / pharmacology*
  • Plant Proteins / chemistry*
  • Plant Proteins / genetics
  • Plant Proteins / pharmacology*
  • Rabbits
  • Sequence Homology, Amino Acid

Substances

  • Kunitz-type protease inhibitor, plant
  • Oligopeptides
  • Peptides
  • Plant Proteins
  • arginyl-glycyl-aspartic acid
  • Kallikreins