Metabolic profile directed aptamer medicinal chemistry
First Claim
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1. ) A method for modifying an aptamer comprising the steps of:
- a) incubating a parent aptamer with a test fluid to result in a mixture;
b) analyzing the mixture to identify metabolites of the parent aptamer, thereby detecting at least one aptamer cleavage site in the parent aptamer; and
c) introducing a chemical substitution at a position proximal to the at least one aptamer cleavage site to result in a modified aptamer.
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Abstract
The present invention provides materials and methods for enhancing aptamers. More specifically, the materials and methods of the present invention are directed toward the modification of aptamers by the identification of one or more cleavage sites, and introduction of a chemical substitution at a position proximal to the cleavage site(s). Such aptamers are useful for the treatment of disease, in diagnostic and detection applications, and/or research, e.g., target validation.
27 Citations
36 Claims
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1. ) A method for modifying an aptamer comprising the steps of:
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a) incubating a parent aptamer with a test fluid to result in a mixture; b) analyzing the mixture to identify metabolites of the parent aptamer, thereby detecting at least one aptamer cleavage site in the parent aptamer; and c) introducing a chemical substitution at a position proximal to the at least one aptamer cleavage site to result in a modified aptamer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
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34. ) A method for modifying an aptamer comprising the steps of:
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a) incubating a parent aptamer with a biological matrix that contains an enzyme to result in a mixture; b) analyzing the mixture to identify metabolites of the parent aptamer, thereby detecting at least one aptamer cleavage site in the parent aptamer; and c) introducing a chemical substitution at a position proximal to the at least one aptamer cleavage site to result in a modified aptamer.
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35. ) A method for enhancing the stability of an aptamer comprising the steps of:
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a) incubating a parent aptamer with a test fluid to result in a mixture; b) analyzing the mixture to identify metabolites of the parent aptamer, thereby detecting at least one aptamer cleavage site in the parent aptamer; and c) introducing a chemical substitution at a position proximal to the at least one aptamer cleavage site to result in a modified aptamer.
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36. ) A method for enhancing the stability of an aptamer to exonucleases and endonucleases comprising the steps of:
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a) incubating a parent aptamer with a test fluid to result in a mixture; b) analyzing the mixture to identify metabolites of the parent aptamer, thereby detecting at least one aptamer cleavage site in the parent aptamer; and c) introducing a chemical substitution at a position proximal to the at least one aptamer cleavage site to result in a modified aptamer.
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Specification