US2002168340A1PendingUtilityA1

Novel HIV-specific synthetic oligonucleotides and methods of their use

52
Priority: Aug 19, 1997Filed: Apr 18, 2001Published: Nov 14, 2002
Est. expiryAug 19, 2017(expired)· nominal 20-yr term from priority
Inventors:Sudhir Agrawal
C12N 2310/315C12N 15/1132A61K 38/00C12N 2310/346C12N 2310/321A61P 31/18
52
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Claims

Abstract

Disclosed are synthetic oligonucleotides having a nucleotide sequences specifically complementary to nucleotides 324 to 345 of a conserved gag region of the HIV-1 genome, the oligonucleotide consisting of 21 nucleotides which are linked via phosphorothioate internucleotide linkages. Also disclosed are methods for inhibiting and treating HIV-1 and HIV-2 infection.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A synthetic oligonucleotide having a nucleotide sequences specifically complementary to nucleotides 324 to 345 of a conserved gag region of the HIV-1 genome set forth as SEQ ID NO:5, the oligonucleotide consisting of 21 nucleotides which are linked via phosphorothioate internucleotide linkages.  
     
     
         2 . The oligonucleotide of  claim 1 , wherein the nucleotides comprise at least two 3′-terminal ribonucleotides, at least two 5′-terminal ribonucleotides, or at least two 3′-terminal and at least two 5′terminal ribonucleotides.  
     
     
         3 . The oligonucleotide of  claim 2 , wherein the ribonucleotides are 2′-substituted ribonucleotides.  
     
     
         4 . The oligonucleotide of  claim 3 , wherein the 3′-substituted ribonucleotides are 2′-O-alkyl ribonucleotides.  
     
     
         5 . The oligonucleotide of  claim 4 , wherein the ribonucleotides are 2′-O-methyl ribonucleotides.  
     
     
         6 . The method of  claim 2 , wherein the nucleotides consist essentially of four 3′-terminal ribonucleotides and four 3′-terminal ribonucleotides, flanking 13 deoxynucleotides.  
     
     
         7 . The oligonucleotide of  claim 6 , wherein the ribonucleotides are 2′-O-methyl ribonucleotides.  
     
     
         8 . The oligonucleotide of  claim 1  having SEQ ID NO:1.  
     
     
         9 . The oligonucleotide of  claim 1  having SEQ ID NO:3.  
     
     
         10 . The oligonucleotide of  claim 7  having SEQ ID NO:1.  
     
     
         11 . The oligonucleotide of  claim 7  having SEQ ID NO:3.  
     
     
         12 . The oligonucleotide of  claim 1  having SEQ ID NO:2.  
     
     
         13 . The oligonucleotide of  claim 1  having SEQ ID NO:4.  
     
     
         14 . The oligonucleotide of  claim 1  which inhibits HIV-1 or HIV-2 infection in a cell.  
     
     
         15 . The oligonucleotide of  claim 1  which exhibits antiviral activity against HIV-1 and HIV-2.  
     
     
         16 . A method of treating HIV-1 or HIV-2 infection in a mammal, comprising the step of administering to the mammal a synthetic oligonucleotide in an amount effective to inhibit the proliferation of HIV-1 or HIV-2, 
 the oligonucleotide being specifically complementary to nucleotides 324 to 345 of a conserved gag region of the HIV-1 genome set forth as SEQ ID NO:5, and consisting of 21 nucleotides which are linked via phosphorothioate internucleotide linkages.    
     
     
         17 . The method of  claim 16  wherein the nucleotides of the oligonucleotide comprise at least two 3′-terminal ribonucleotides, at least two 5′-terminal ribonucleotides, or at least two 3′-terminal and at least two 5′terminal ribonucleotides.  
     
     
         18 . The method of  claim 17 , wherein the ribonucleotides of the oligonucleotide are 2′-substituted ribonucleotides.  
     
     
         19 . The method of  claim 18 , wherein the 3′-substituted ribonucleotides of the oligonucleotides are 2′-O-alkyl ribonucleotides.  
     
     
         20 . The method of  claim 19 , wherein the ribonucleotides of the oligonucleotide are 2′-O-methyl ribonucleotides.  
     
     
         21 . The method of  claim 19 , wherein the nucleotides of the oligonucleotide consist essentially of four 3′-terminal ribonucleotides and four 3′-terminal ribonucleotides, flanking 13 deoxynucleotides.  
     
     
         22 . The method of  claim 21 , wherein the ribonucleotides of the oligonucleotide are 2′-O-methyl ribonucleotides.  
     
     
         23 . The method of  claim 16 , wherein the oligonucleotide has SEQ ID NO:1.  
     
     
         24 . The method of  claim 16 , wherein the oligonucleotide has SEQ ID NO:3.  
     
     
         25 . The method of  claim 21 , wherein the oligonucleotide has SEQ ID NO:1.  
     
     
         26 . The method of  claim 21 , wherein the oligonucleotide has SEQ ID NO:3.  
     
     
         27 . The method of  claim 16 , wherein the oligonucleotide has SEQ ID NO:2.  
     
     
         28 . The method of  claim 16 , wherein the oligonucleotide has SEQ ID NO:6.  
     
     
         29 . The method of  claim 16 , wherein the oligonucleotide is administered orally.  
     
     
         30 . The method of  claim 16 , wherein the oligonucleotide is administered intravenously.  
     
     
         31 . A pharmaceutical formulation comprising the oligonucleotide of  claim 1  in a pharmaceutically acceptable carrier.  
     
     
         32 . A pharmaceutical formulation comprising the oligonucleotide of  claim 6  in a pharmaceutically acceptable carrier.  
     
     
         33 . A pharmaceutical formulation comprising the oligonucleotide of  claim 7  in a pharmaceutically acceptable carrier.  
     
     
         34 . A method of inhibiting HIV-1 or HIV-2 infection in a cell comprising the step of contacting the cell with the synthetic oligonucleotide of  claim 1 .  
     
     
         35 . A method of inhibiting HIV-1 or HIV-2 infection in a cell comprising the step of contacting the cell with the synthetic oligonucleotide of  claim 6 .  
     
     
         36 . A method of inhibiting HIV-1 or HIV-2 infection in a cell comprising the step of contacting the cell with the synthetic oligonucleotide of  claim 7 .  
     
     
         37 . A method for introducing an intact oligonucleotide into a mammal, the method comprising the step of orally administering to the mammal the oligonucleotide of  claim 1 , 
 whereby the oligonucleotide is present in intact form in the systemic plasma following oral administration.    
     
     
         38 . A method for introducing an intact oligonucleotide into a mammal, the method comprising the step of orally administering to the mammal the oligonucleotide of  claim 6 , 
 whereby the oligonucleotide is present in intact form in the systemic plasma following oral administration.    
     
     
         39 . A method for introducing an intact oligonucleotide into a mammal, the method comprising the step of orally administering to the mammal the oligonucleotide of  claim 7 , 
 whereby the oligonucleotide is present in intact form in the systemic plasma following oral administration.

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