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Bioconjug Chem. 1998 Sep-Oct;9(5):573-82.

Liposome-anchored vascular endothelial growth factor aptamers.

Author information

1
NeXstar Pharmaceuticals, 2860 Wilderness Place, Boulder, Colorado 80301, USA.

Erratum in

  • Bioconjug Chem 1998 Sep-Oct;9(5):633. Collins B [corrected to Collins BD].

Abstract

Nuclease-resistant aptamers identified from randomized nucleic acid libraries represent a novel class of drug candidates. Aptamers are synthesized chemically and therefore can be readily modified with functional groups that modulate their properties. We report here on the preparation, initial characterization, and functional properties of a nuclease-resistant vascular endothelial growth factor (VEGF) aptamer anchored in liposome bilayers through a lipid group on the aptamer. While the high-affinity binding to VEGF is maintained, the plasma residence time of the liposome-anchored aptamer is considerably improved compared with that of the free aptamer. The lipid group attachment and/or liposome anchoring leads to a dramatic improvement in inhibitory activity of the aptamer toward VEGF-induced endothelial cell proliferation in vitro and vascular permeability increase and angiogenesis in vivo.

PMID:
9736491
DOI:
10.1021/bc980002x
[Indexed for MEDLINE]
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