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Published February 21, 2001 | Supplemental Material
Journal Article Open

Inhibition of Cell Adhesion to Fibronectin by Oligopeptide-Substituted Polynorbornenes


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.

Additional Information

© 2001 American Chemical Society. Received 7 September 2000. Published online 26 January 2001. Published in print 1 February 2001. We thank Bayer Corporation and the Air Force Office of Sponsored Research (Grant F49620-97-1-0014) for funding this research. Professor David Tirrell is gratefully acknowledged for allowing us to use his cell culture room and aqueous GPC. Sarah Heilshorn, Dr. Natalie Winblade, and Dr. Jason Schense are appreciated for their many helpful discussions.

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