Current Drug Targets

Francis J. Castellino
Kleiderer-Pezold Professor of Biochemistry
Director, W.M. Keck Center for Transgene Research
Dean Emeritus, College of Science
230 Raclin-Carmichael Hall, University of Notre Dame
Notre Dame, IN 46556
USA

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Progress in Thioaptamer Development

Author(s): Xianbin Yang and David G. Gorenstein

Affiliation: Sealy Center for Structural Biology, University of Texas Medical Branch, 301 University Boulevard,Galveston, TX 77555-1157, USA.

Abstract:

Thioaptamers are thiophosphate ester modified nucleic acids that are isolated via in vitro or bead-based thioaptamer selection against a target molecule such as a protein. Thioaptamers offer advantages over traditional aptamers in their enhanced affinity and specificity and higher stability, largely due to the properties of the sulfur backbone-modifications. An in vitro thioaptamer selection procedure that simultaneously selects for sequence and optimized hybrid phosphoromonothioate or phosphate backbone substitutions is outlined. A novel bead-based thioaptamer selection protocol that can produce mixed phosphorodithioate, phosphoromonothioate or phosphate hybrid backbones is also described. Several examples of thioaptamers targeting specific protein are provided. Such thioaptamers are shown to modulate protein activity in vivo.

Keywords: thioaptamer, oligonucleoside phosphoromonothioate, oligonucleoside phosphorodithioate, bead-based selection

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Article Details

VOLUME: 5
ISSUE: 8
Page: [705 - 715]
Pages: 11
DOI: 10.2174/1389450043345074
Price: $58