High affinity HIV integrase inhibitors
First Claim
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1. A method of identifying nucleic acid ligands to a target molecule comprising:
- a) contacting a candidate mixture with the target molecule, wherein nucleic acids having an increased affinity to the target molecule relative to the candidate mixture may be partitioned from the remainder of the candidate mixture and wherein the candidate mixture comprises a first and a second pool of nucleic acids, wherein the first pool of nucleic acid is amplifiable and the second pool of nucleic acids is non-amplifiable;
b) partitioning the increased affinity nucleic acids from the remainder of the candidate mixture; and
c) amplifying the increased affinity nucleic acids under conditions wherein only the first pool of nucleic acids is amplified, to yield a ligand enriched mixture of nucleic acids whereby nucleic acid ligands to the target molecule may be identified.
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Abstract
Methods are described for the identification and preparation of nucleic acid ligands to HIV integrase. Included in the invention are specific RNA ligands to HIV integrase identified by the SELEX method. Also included in the invention are specific RNA ligands that are inhibitors of HIV integrase.
18 Citations
10 Claims
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1. A method of identifying nucleic acid ligands to a target molecule comprising:
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a) contacting a candidate mixture with the target molecule, wherein nucleic acids having an increased affinity to the target molecule relative to the candidate mixture may be partitioned from the remainder of the candidate mixture and wherein the candidate mixture comprises a first and a second pool of nucleic acids, wherein the first pool of nucleic acid is amplifiable and the second pool of nucleic acids is non-amplifiable; b) partitioning the increased affinity nucleic acids from the remainder of the candidate mixture; and c) amplifying the increased affinity nucleic acids under conditions wherein only the first pool of nucleic acids is amplified, to yield a ligand enriched mixture of nucleic acids whereby nucleic acid ligands to the target molecule may be identified. - View Dependent Claims (2)
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3. A method of identifying nucleic acid ligands to HIV integrase, comprising:
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a) contacting a candidate mixture of nucleic acids with HIV integrase, wherein nucleic acids having an increased affinity to the HIV integrase relative to the candidate mixture may be partitioned from the remainder of the candidate mixture; and b) partitioning the increased affinity nucleic acids from the remainder of the candidate mixture; and c) amplifying the increased affinity nucleic acids to yield a mixture of nucleic acids enriched for nucleic acid sequences with relatively higher affinity and specificity for binding to HIV integrase, whereby nucleic acid ligands of HIV integrase may be identified. - View Dependent Claims (4, 5, 6, 7, 8, 9, 10)
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Specification