Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit tumor growth and angiogenesis. Covalent linkage of naproxen to human serum albumin (HSA) has been shown to target it efficiently to the liver and this may potentially be exploited for liver-selective inhibition of angiogenesis. With the aim of investigating the anti-angiogenic efficiency of NSAID-HSA conjugates in vitro, three NSAIDs, aspirin, ibuprofen, and naproxen were conjugated to HSA using different concentrations of their N-hydroxysuccinimide esters. Conjugation ratios from 10 to 50 were achieved and the conjugates retained a growth inhibitory effect on endothelial cells at or above the level of the non-conjugated NSAIDs in an in vitro angiogenesis assay.
Keywords: Angiogenesis, HUVEC, NSAID, HSA, conjugation
Protein & Peptide Letters
Title: Synthesis and Anti-Angiogenic Effect of Conjugates Between Serum Albumin and Non-Steroidal Anti-Inflammatory Drugs
Volume: 17 Issue: 1
Author(s): B. Kjær, C. Struve, T. Friis, A.-M. Engel, N. H. Beyer, P. Hojrup and G. Houen
Affiliation:
Keywords: Angiogenesis, HUVEC, NSAID, HSA, conjugation
Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit tumor growth and angiogenesis. Covalent linkage of naproxen to human serum albumin (HSA) has been shown to target it efficiently to the liver and this may potentially be exploited for liver-selective inhibition of angiogenesis. With the aim of investigating the anti-angiogenic efficiency of NSAID-HSA conjugates in vitro, three NSAIDs, aspirin, ibuprofen, and naproxen were conjugated to HSA using different concentrations of their N-hydroxysuccinimide esters. Conjugation ratios from 10 to 50 were achieved and the conjugates retained a growth inhibitory effect on endothelial cells at or above the level of the non-conjugated NSAIDs in an in vitro angiogenesis assay.
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Cite this article as:
Kjær B., Struve C., Friis T., Engel A.-M., Beyer H. N., Hojrup P. and Houen G., Synthesis and Anti-Angiogenic Effect of Conjugates Between Serum Albumin and Non-Steroidal Anti-Inflammatory Drugs, Protein & Peptide Letters 2010; 17 (1) . https://dx.doi.org/10.2174/092986610789909511
DOI https://dx.doi.org/10.2174/092986610789909511 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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