Moiety of a new bivalent inhibitor blocking the active site of thrombin. This generation of polypeptide inhibitors was discovered through rational design in combination with phagedisplay selection. The figure shows a three-dimensional model of the bivalent peptide bound to thrombin, suggesting intricate communications between P3 and P'3 residues. The P'3 residue projects its side chain into contacts with the side chain of the P3 site, which may be the structural mechanism for enhanced potencies of the new thrombin inhibitors. For further details, see Su et al., pages 647-657.
[Table of Contents]