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Synthesis, Characterisation and in vitro Anti‐Angiogenic Potential of Dendron VEGF Blockers
Author(s) -
Meikle Steven T.,
Perugini Valeria,
Guildford Anna L.,
Santin Matteo
Publication year - 2011
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201100267
Subject(s) - dendrimer , angiogenesis , extracellular matrix , chemistry , in vitro , in vivo , branching (polymer chemistry) , extracellular , peptide , vegf receptors , biophysics , biochemistry , microbiology and biotechnology , cancer research , biology , organic chemistry
To overcome the lack of in vivo stability of certain peptides used in cancer treatment and to increase their retention time in the extracellular matrix of the target tissue, the anti‐angiogenic WHLPFKC sequence is synthesised at the uppermost branching generation of a poly( ε ‐lysine) dendron. The root of these dendrons is designed to interact preferentially with macromolecules of the extracellular matrix, whilst the uppermost branching generation of the dendron increased the exposed density of the bioactive peptide. Bioactivity testing of the blockers is performed on HUVECs. The results show that the dendron tethered with VEGF blockers was still able to inhibit proliferation and angiogenesis. Their relatively larger structure did not prevent the interaction with VEGF.