期刊
BIOMACROMOLECULES
卷 9, 期 2, 页码 603-609出版社
AMER CHEMICAL SOC
DOI: 10.1021/bm701185p
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资金
- NCI NIH HHS [1 R33 CA112141, R01 CA119409, 1 R01 CA119409, R33 CA112141] Funding Source: Medline
- NCRR NIH HHS [1 R21 RR021893] Funding Source: Medline
- NIDDK NIH HHS [5P60 DK20572] Funding Source: Medline
Binding of ligands on to epidermal growth factor receptor (EGFR) can stimulate cell growth; therefore, any application employing EGF as a targeting ligand for a drug carrier must evaluate the effect of the conjugate on cell growth. We report the synthesis and in vitro biological activity of EGF molecules coupled to a fluorescein-labeled polyamidoamine dendrimer. The conjugate bound and internalized into several EGFR-expressing cell lines in a receptor-specific fashion. The conjugate effectively induced EGFR phosphorylation and acted as a superagonist by stimulating cell growth to a greater degree than free EGF. Concomitant administration of the chemotherapeutic drug methotrexate completely inhibited cell growth to a degree similar to its effect in the absence of the conjugate. Thus, dendrimer-EGF conjugates serve as EGFR superagonists, but this activity can be overcome by chemotherapeutic drugs. The agonist activity of these materials must be taken into consideration when using EGF conjugates for imaging applications.
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