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Synthesis and Characterization of Chemical Conjugate Targeting KDR
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Abstract:
Objective: One strategy for improving the selectively and toxicity profile of antitumor agents is to design drug carrier systems. Thus a reagent targeting KDR expressed on tumor vasculature was prepared by a peptide binding to KDR specifically which screened from C7 peptide library coupled covalently to NHS-d-Biotin and BSA. Methods: A high affinity peptide specific for KDR was screened by phage display. ELISA, Gradient-ELISA, Competitive-ELISA and Blocking-ELISA were used to detect whether synthesized peptide bind to KDR. To explore whether peptide could be used to deliver agent to target site, synthesized peptide was chemically conjugated with large molecule-BSA and NHS-d-Biotin easily detected by avidin. The binding activity to KDR of chemical compound was determined by Cell-ELISA and Cell-immunohistology. Results:Synthesized P5 peptide having a dissociation constant (Kd) of about 168.6 nM with KDR was approximately 3 fold lower than Kd of VEGF with KDR. P5 blocked VEGF-KDR interaction while did not competes effectively with VEGF for binding KDR. The chemical conjugate, P5-BSA-Biotin, binds specifically to soluble KDR as well as KDR expressed on human endothelial cells. Conclusion:The peptide P5 that home to KDR expressed on tumor vasculature may also be useful in targeting therapies specifically to tumors.
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