High affinity nucleic acid ligands containing modified nucleotides
AssigneeNeXstar Pharmaceuticals, Inc.
InventorsWolfgang Pieken, Diane Tasset, Nebojsa Janjic, Larry Gold, Gary P Kirschenheuter
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Abstract
Nucleic acid ligands containing modified nucleotides are described as are methods for producing such oligonucleotides. Such ligands enrich the chemical diversity of the candidate mixture for the SELEX process. Specific examples are provided of nucleic acids containing nucleotides modified at the 2′- and 5-position. Specific 2-OH and 2′-NH2 modified RNA ligands to thrombin are described.
Claims2
A method of preparing 5-iodo,2′-amino deoxyuridine from uridine comprising:
- a) dehydrating uridine to 2,2′-anhydrouridine;
- b) converting 2,2′-anhydrouridine to an unprotected 2′-azido,2′-deoxyuridine;
- c) iodinating the unprotected 2′-azido,2′-deoxyuridine to 5-iodo, 2′-azido,2′-deoxyuridine;
- and
- d) reducing the unprotected 5-iodo,2′-azido,2′-deoxyuridine to 5-iodo,2′-amino,2′-deoxyuridine.
A method of preparing 5-iodo,2′-amino,2′-deoxy uridine 5′-triphosphate from 2′-amino,2′-deoxyuridine, comprising:
- a) trifluoroacetylating 2′-amino,2′-deoxyuridine to form 2′-trifluoroacetylamino,2′-deoxyuridine;
- b) phosphorylating 2′-trifluoroacetylamino,2′-deoxyuridine to 2′-amino,2′-deoxyuridine 5′-triphosphate;
- and
- c) iodinating 2′-trifluoroacetylamino,2′-deoxyuridine by mercuration to form 5′-iodo,2′-amino,2′-deoxyuridine 5′-triphosphate.
Dependencies are inferred from the claim text.