Inhibition of cell adhesion to fibronectin by oligopeptide-substituted polynorbornenes.
J Am Chem Soc
; 123(7): 1275-9, 2001 Feb 21.
Article
in En
| MEDLINE
| ID: mdl-11456698
ABSTRACT
Polynorbornenes substituted with two different peptide sequences from the RGD-containing integrin cell-binding domain of fibronectin are potent inhibitors of human foreskin fibroblast cell adhesion to fibronectin-coated surfaces. Ring-opening metathesis polymerization (ROMP) using Ru==CHPh(Cl)(2)(PCy(3))(DHIMes) (1) as an initiator produced polymers substituted with GRGDS and PHSRN peptide sequences. The inhibitory activity was quantified for these polymers and compared to the free peptides and GRGES-containing controls. A homopolymer substituted with GRGDS peptides was significantly more active than the free GRGDS peptide (IC(50) of 0.18 +/- 0.03 and 1.33 +/- 0.20 mM respectively), and the copolymer containing both GRGDS and PHSRN is the most potent inhibitor (IC(50) of 0.04 +/- 0.01 mM). These results demonstrate that significant enhancements of observed biological activity can be obtained from polymeric materials containing more than one type of multivalent ligand and that ROMP is a useful method to synthesize such well-defined copolymers.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oligopeptides
/
Plastics
/
Cell Adhesion
/
Fibronectins
Limits:
Humans
Language:
En
Journal:
J Am Chem Soc
Year:
2001
Document type:
Article
Affiliation country:
United States