Summary.
Targeted diagnostic agents are expected to have a significant impact in molecular imaging of cell-surface associated markers of proliferation, inflammation and angiogenesis. In this communication, we describe a new class of targeted polyamino acid-based protected graft copolymers (PGC) of poly-(L-lysine) and methyl poly-(ethylene glycol) (PGC) covalently conjugated with a monoclonal antibody fragment, F(ab′)2. We utilized targeted PGC conjugates as carriers of near-infrared indocyanine fluorophores (Cy5.5) for optical imaging of endothelial cell populations expressing IL-1β inducible proinflammatory marker E-selectin. We compared two conjugation chemistries, involving either introduction of sulfhydryl group to F(ab′)2, or via direct attachment of the antibody fragment directly to the chemically activated PGC. Both PGC-based targeted agents demonstrated high binding specificity (20–30 fold over non-specific uptake) and were utilized for imaging E-selectin expression on human endothelial cells activated with IL-1β.
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Received June 29, 2001 Accepted August 8, 2001 Published online August 9, 2002
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Kang, H., Weissleder, R. & Bogdanov, Jr., A. Targeting of MPEG-protected polyamino acid carrier to human E-selectin in vitro . Amino Acids 23, 301–308 (2002). https://doi.org/10.1007/s00726-001-0142-2
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DOI: https://doi.org/10.1007/s00726-001-0142-2