info:eu-repo/semantics/article
X-aptamers: A bead-based selection method for random incorporation of druglike moieties onto next-generation aptamers for enhanced binding
Fecha
2012-10Registro en:
He, Weiguo; Elizondo Riojas, Miguel Angel; Li, Xin; Lokesh, Ganesh Lakshmana Rao; Somasunderam, Anoma; et al.; X-aptamers: A bead-based selection method for random incorporation of druglike moieties onto next-generation aptamers for enhanced binding; American Chemical Society; Biochemistry; 51; 42; 10-2012; 8321-8323
0006-2960
CONICET Digital
CONICET
Autor
He, Weiguo
Elizondo Riojas, Miguel Angel
Li, Xin
Lokesh, Ganesh Lakshmana Rao
Somasunderam, Anoma
Thiviyanathan, Varatharasa
Volk, David E.
Durland, Ross H.
Englehardt, Johnnie
Cavasotto, Claudio Norberto
Gorenstein, David G.
Resumen
By combining pseudorandom bead-based aptamer libraries with conjugation chemistry, we have created next-generation aptamers, X-aptamers (XAs). Several X-ligands can be added in a directed or random fashion to the aptamers to further enhance their binding affinities for the target proteins. Here we describe the addition of a drug (N-acetyl-2,3-dehydro-2-deoxyneuraminic acid), demonstrated to bind to CD44-HABD, to a complete monothioate backbone-substituted aptamer to increase its binding affinity for the target protein by up to 23-fold, while increasing the drug's level of binding 1-million fold.