Methods of X-aptamer generation and compositions thereof



Aptamers are structurally distinct RNA and DNA oligonucleotides (ODNs) that can mimic protein-binding molecules and exhibit high (nM) binding affinity based on their unique secondary three-dimensional structure conformations and not by pair-wise nucleic acid binding. Aptamers can be selected via high-throughput in vitro methods to bind target molecules. Aptamers are thus emerging as viable alternatives to small molecules and antibody-based therapies in the field of drug development.


Provided herein are methods for a novel bead-based next-generation “X-aptamer” selection scheme that extends aptamer technology to include X-modified bases, thus resulting in X-aptamers, at any position along the sequence because the aptamers are chemically synthesized via a split-pool scheme on individual beads. Also provides are application to a wide range of commonly used DNA modifications, including, but not limited to, monothioate and dithioate backbone substitutions. This new class of aptamer allows chemical modifications introduced to any of the bases in the aptamer sequence as well as the phosphate backbones and can be extended to other carbohydrate-based systems.


UTHealth Ref. No.: 2012-0015

Inventors: Gorenstein et al.

Patent Status: Issued U.S. Patent 9,988,623

License Available: world-wide; exclusive or non-exclusive


Patent Information:

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Christine Weaver
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University of Texas Health Science Center At Houston
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