Biochemistry · 2012 · 69 citations · 10 references
PharmacyMedicinal ChemistryMolecular BiologyDrug DesignDrug DiscoveryProtein EngineeringAntibody-drug ConjugatesLigand BindingLigand-based DesignProtein DesignProtein-ligand BindingProtein-ligand InteractionsAptamer - Target Binding AffinityAptamer DesignAptamer DiscoveryAptamer Library ConstructionAptamersClick Chemistry Surface ConjugationConjugation Chemistry For AntibodiesLigand Conjugation Chemistry
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.
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In vitro selection of RNA molecules that bind specific ligands
Andrew D. Ellington, Jack W. Szostak · Nature · 1990 · 9.7K citations
DOCK 6: Combining techniques to model RNA–small molecule complexes
P. Therese Lang, Scott R. Brozell, Sudipto Mukherjee et al. · RNA · 2009 · 749 citations · Full text