Liposome-anchored vascular endothelial growth factor aptamers

Michael C. Willis, Brian Collins, Tong Zhang, Louis S. Green, David P. Sebesta, Carol Bell, Elizabeth Kellogg, Stanley C. Gill, Anna Magallanez, Susan Knauer, Ray A. Bendele, Parkash S. Gill, Nebojša Janjić

Research output: Contribution to journalArticlepeer-review

183 Scopus citations


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.

Original languageEnglish
Pages (from-to)573-582
Number of pages10
JournalBioconjugate Chemistry
Issue number5
StatePublished - 1998


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