PDGF and VEGF aptamers having improved stability and their use in treating PDGF and VEGF mediated diseases and disorders
First Claim
Patent Images
1. A nucleic acid molecule comprising the nucleic sequence5′
- -C1-G-A-C1,2-A-G1-C1-A-Z2-G2-Z2-A2-Z-G1-C1-A1-C1-A1-Z-C1-Z1-3′
(SEQ ID NO;
833),wherein,C1 is independently, for each occurrence, selected from the group consisting of a cytidine, a deoxycytidine and a 2′
-O-methylcytidine;
C1,2 is independently, for each occurrence, selected from the group consisting of a cytidine, a cytidine comprising a phosphorothioate linkage, a deoxycytidine, a deoxycytidine comprising a phosphorothioate linkage, a 2′
-O-methylcytidine and a 2′
-O-methylcytidine comprising a phosphorothioate linkage;
G1 is independently, for each occurrence, selected from the group consisting of a guanosine, a deoxyguanosine and a 2′
-O-methylguanosine;
G2 is independently, for each occurrence, selected from the group consisting of a guanosine, a guanosine comprising a phosphorothioate linkage, a deoxyguanosine and a deoxyguanosine comprising a phosphorothioate linkage;
Z1 is independently, for each occurrence, selected from the group consisting of a uridine, a deoxyuridine, a 2′
-O-methyluridine, a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) comprising a 2′
-O-methyl group;
Z2 is independently, for each occurrence, selected from the group consisting of a uridine, a uridine comprising a phosphorothioate linkage, a deoxyuridine, a deoxyuridine comprising a phosphorothioate linkage, a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU)comprising a phosphorothioate linkage;
Z is independently, for each occurrence, selected from the group consisting of a uridine, a deoxyuridine and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU);
A1 is independently, for each occurrence, selected from the group consisting of an adenosine, a deoxyadenosine and a 2′
-O-methyladenosine;
A2 is independently, for each occurrence, selected from the group consisting of an adenosine, an adenosine comprising a phosphorothioate linkage, a deoxyadenosine and a deoxyadenosine comprising a phosphorothioate linkage; and
wherein, the nucleic acid molecule comprises at least one, two, three, four or five phosphorothioate linkages.
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Abstract
Aptamers having improved stability against nucleases that bind PDGF and aptamers that bind VEGF are provided. In addition, aptamer constructs comprising a PDGF aptamer and a VEGF aptamer are provided. Pharmaceutical compositions comprising the aptamers and aptamer constructs are provided, as well as methods of treating conditions using the aptamers and aptamer constructs.
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Citations
3 Claims
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1. A nucleic acid molecule comprising the nucleic sequence
5′ - -C1-G-A-C1,2-A-G1-C1-A-Z2-G2-Z2-A2-Z-G1-C1-A1-C1-A1-Z-C1-Z1-3′
(SEQ ID NO;
833),wherein, C1 is independently, for each occurrence, selected from the group consisting of a cytidine, a deoxycytidine and a 2′
-O-methylcytidine;C1,2 is independently, for each occurrence, selected from the group consisting of a cytidine, a cytidine comprising a phosphorothioate linkage, a deoxycytidine, a deoxycytidine comprising a phosphorothioate linkage, a 2′
-O-methylcytidine and a 2′
-O-methylcytidine comprising a phosphorothioate linkage;G1 is independently, for each occurrence, selected from the group consisting of a guanosine, a deoxyguanosine and a 2′
-O-methylguanosine;G2 is independently, for each occurrence, selected from the group consisting of a guanosine, a guanosine comprising a phosphorothioate linkage, a deoxyguanosine and a deoxyguanosine comprising a phosphorothioate linkage; Z1 is independently, for each occurrence, selected from the group consisting of a uridine, a deoxyuridine, a 2′
-O-methyluridine, a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) comprising a 2′
-O-methyl group;Z2 is independently, for each occurrence, selected from the group consisting of a uridine, a uridine comprising a phosphorothioate linkage, a deoxyuridine, a deoxyuridine comprising a phosphorothioate linkage, a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU) and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU)comprising a phosphorothioate linkage;Z is independently, for each occurrence, selected from the group consisting of a uridine, a deoxyuridine and a 5-(N-naphthylmethylcarboxyamide)-2′
-deoxyuridine (NapdU);A1 is independently, for each occurrence, selected from the group consisting of an adenosine, a deoxyadenosine and a 2′
-O-methyladenosine;A2 is independently, for each occurrence, selected from the group consisting of an adenosine, an adenosine comprising a phosphorothioate linkage, a deoxyadenosine and a deoxyadenosine comprising a phosphorothioate linkage; and wherein, the nucleic acid molecule comprises at least one, two, three, four or five phosphorothioate linkages. - View Dependent Claims (2, 3)
- -C1-G-A-C1,2-A-G1-C1-A-Z2-G2-Z2-A2-Z-G1-C1-A1-C1-A1-Z-C1-Z1-3′
Specification