Artículo
X-aptamers: A bead-based selection method for random incorporation of druglike moieties onto next-generation aptamers for enhanced binding
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.
![Icon](/themes/CONICETDigital/images/conicet.png)
Fecha de publicación:
10/2012
Editorial:
American Chemical Society
Revista:
Biochemistry
ISSN:
0006-2960
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
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.
Palabras clave:
X-Aptamers
,
Structure-Based Drug Design
,
Molecular Dynamics
,
Cd44
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Articulos(IBIOBA - MPSP)
Articulos de INST. D/INV.EN BIOMED.DE BS AS-CONICET-INST. PARTNER SOCIEDAD MAX PLANCK
Articulos de INST. D/INV.EN BIOMED.DE BS AS-CONICET-INST. PARTNER SOCIEDAD MAX PLANCK
Citación
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
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