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Molecular Targeting with Peptides or Peptide-Polymer Conjugates: Just a Question of Size?

Technische Universität München
Munich, Germany

View larger version (19K): [in a new window]   FIGURE 1. Factors influencing uptake of RGD-peptide-polymer conjugates: expression of vß3 integrins on tumor cells and vasculature (1), formation of clusters of activated vß3 integrins (2), enhanced permeability (3), impaired lymphatic drainage result in EPR (4), nonspecific tumor accumulation of peptide-polymer conjugates by EPR (5), nonspecific uptake in nontumor tissue (6), blood clearance (kinetics) (7), catabolism (8), and whole-body-retention and excretion kinetics (9).

View larger version (17K): [in a new window]   FIGURE 2. Subsequent steps of integrin activation and multimeric RGD binding. FAK = focal adhesion kinase.

View larger version (28K): [in a new window]   FIGURE 3. Selected characteristics of monovalent and polyvalent ligands and consequences for molecular targeting.