US2023183752A1PendingUtilityA1

Complexes for gene deletion and editing

Assignee: UNIV MASSACHUSETTSPriority: Jan 9, 2017Filed: Oct 26, 2022Published: Jun 15, 2023
Est. expiryJan 9, 2037(~10.5 yrs left)· nominal 20-yr term from priority
A01K 2207/12A61P 3/04C07K 7/06C12N 9/96C07K 14/4702C12N 2310/16C07K 14/003C07K 7/08C12N 2310/14A61K 47/549C07K 19/00A01K 2217/07A01K 2227/105C12N 2320/32C12N 15/113C07K 14/00C12N 15/907C12N 2310/3513A61K 47/64C12N 9/22C12N 5/0653A01K 67/0278A61K 9/0019A01K 2267/0362C12N 2310/20
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Claims

Abstract

Complexes comprising a nucleic acid-guided endonuclease, a sequence-specific targeting nucleic acid and an amphipathic helical peptide are provided. Compositions and methods for delivery of complexes comprising a nucleic acid-guided endonuclease, a sequence-specific targeting nucleic acid and an amphipathic helical peptide to mammals for both research and therapeutic use are provided. Methods of treating or reducing one or more symptoms of type 2 diabetes, prediabetes and/or gestational diabetes are provided.

Claims

exact text as granted — not AI-modified
1 . A composition comprising:
 a nucleic acid-guided endonuclease,   a sequence-specific targeting nucleic acid and   an amphipathic helical peptide,   wherein the nucleic acid-guided endonuclease, the sequence-specific targeting nucleic acid and the amphipathic helical peptide form a complex, and   wherein the amphipathic helical peptide mediates delivery of the complex to a target cell, and wherein the nucleic acid-guided endonuclease mediates editing or deletion of a target gene in the target cell.   
     
     
         2 . The composition of  claim 1 , wherein the amphipathic helical peptide is selected from the group consisting of: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 5) 
                 
                     
                   H2N-LHHLLHHLLHHLHHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   H2N-LHKLLHHLLHHLHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   H2N-LHKLLHHLLHKLHHLLHKLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 8) 
                 
                     
                   H2N-LHHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 9) 
                 
                     
                   H2N-HHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 10) 
                 
                     
                   H2N-LHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 11) 
                 
                     
                   H2N-LHHLLHLLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   H2N-LHKLLHHLLHHLHK-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   H2N-LHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   H2N-KLHHLLHKLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 15) 
                 
                     
                   H2N-HLHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 16) 
                 
                     
                   H2N-LHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 17) 
                 
                     
                   H2N-LHKLLHHLLHKLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 18) 
                 
                     
                   H2N-LHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 19) 
                 
                     
                   H2N-LHHLL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 20) 
                 
                     
                   H2N-LHKLL-COOH 
                 
                     
                   and 
                 
                     
                 
                     
                   Endo-Porter; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         wherein the amphipathic helical peptide is Endoporter; or, 
         wherein the nucleic acid-guided endonuclease is Cas9, optionally wherein the Cas9 is an  E. coli  Cas9, a  Streptococcus pyogenes  Cas9, or a  Staphylococcus aureus  Cas9. 
       
     
     
         3 - 5 . (canceled) 
     
     
         6 . The composition of  claim 1 , wherein the sequence-specific targeting nucleic acid is a guide RNA, optionally wherein:
 the guide RNA is between 15 and 30 bases in length, and comprises a region which is at least 90% homologous to GGTTTGGAGTCACGTCAGGG (SEQ ID NO: 1), GGATTTAAGGTGCTATGGCG (SEQ ID NO: 2), GGAGTCGAAGAACATCTGCA (SEQ ID NO: 3) or GGAGTACTGCAGGCATACGG (SEQ ID NO: 4), optionally wherein the guide RNA comprises a region that is at least 95% homologous to SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, or SEQ ID NO: 4 or the guide RNA comprises SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, or SEQ ID NO: 4.   
     
     
         7 - 9 . (canceled) 
     
     
         10 . The composition of  claim 1 , wherein the target gene is RIP140. 
     
     
         11 . The composition of  claim 1 , wherein the target cell is mammalian, optionally wherein the target cell is an adipocyte or a pre-adipocyte. 
     
     
         12 . (canceled) 
     
     
         13 . The composition of  claim 1 , wherein the complex further comprises an aptamer molecule with binding specificity for the target cell, optionally wherein:
 the aptamer forms a non-covalent binding interaction with the amphipathic helical peptide; or   the aptamer is conjugated to the amphipathic helical peptide.   
     
     
         14 - 15 . (canceled) 
     
     
         16 . The composition of  claim 1 , wherein the complex is encapsulated in a glucan particle (GP). 
     
     
         17 . A method of editing or deleting a target gene in a cell comprising contacting a cell with a complex comprising a nucleic acid-guided endonuclease, a sequence-specific targeting nucleic acid and an amphipathic helical peptide and allowing the complex to enter the cell and edit or delete the target gene. 
     
     
         18 . The method of  claim 17 , wherein the amphipathic helical peptide is selected from the group consisting of: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 5) 
                 
                     
                   H2N-LHHLLHHLLHHLHHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   H2N-LHKLLHHLLHHLHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   H2N-LHKLLHHLLHKLHHLLHKLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 8) 
                 
                     
                   H2N-LHHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 9) 
                 
                     
                   H2N-HHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 10) 
                 
                     
                   H2N-LHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 11) 
                 
                     
                   H2N-LHHLLHLLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   H2N-LHKLLHHLLHHLHK-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   H2N-LHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   H2N-KLHHLLHKLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 15) 
                 
                     
                   H2N-HLHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 16) 
                 
                     
                   H2N-LHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 17) 
                 
                     
                   H2N-LHKLLHHLLHKLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 18) 
                 
                     
                   H2N-LHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 19) 
                 
                     
                   H2N-LHHLL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 20) 
                 
                     
                   H2N-LHKLL-COOH 
                 
                     
                 
                     
                   and 
                 
                     
                   Endo-Porter; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 wherein the amphipathic helical peptide is Endo-Porter. 
 
     
     
         19 . (canceled) 
     
     
         20 . The method of  claim 17 , wherein said target gene is RIP140, optionally wherein:
 said cell is an adipocyte or a pre-adipocyte; or   said sequence-specific targeting nucleic acid is a guide RNA.   
     
     
         21 - 22 . (canceled) 
     
     
         23 . The method of claim  22 , wherein the guide RNA is between 15 and 30 bases in length, and comprises a region which is at least 90% homologous to GGTTTGGAGTCACGTCAGGG (SEQ ID NO: 1), GGATTTAAGGTGCTATGGCG (SEQ ID NO: 2), GGAGTCGAAGAACATCTGCA (SEQ ID NO: 3) or GGAGTACTGCAGGCATACGG (SEQ ID NO: 4), optionally wherein:
 the guide RNA comprises a region that is at least 95% homologous to SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3 or SEQ ID NO: 4; or   the guide RNA comprises SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3 or SEQ ID NO: 4.   
     
     
         24 - 25 . (canceled) 
     
     
         26 . The method of  claim 18 , wherein:
 said nucleic acid-guided endonuclease is Cas9; or   the complex further comprises an aptamer molecule with binding specificity for the target cell, optionally wherein the aptamer forms a non-covalent binding interaction with the amphipathic helical peptide or is conjugated to the amphipathic helical peptide.   
     
     
         27 - 29 . (canceled) 
     
     
         30 . The method of  claim 18 , wherein the complex is encapsulated in a glucan particle (GP). 
     
     
         31 . A method of improving glucose tolerance in a subject, comprising:
 administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a complex including a nucleic acid-guided endonuclease, a sequence-specific targeting nucleic acid and an amphipathic helical peptide, wherein the complex edits or deletes a target gene in the subject; or   contacting an adipocyte cell or pre-adipocyte cell ex vivo with a complex including a Cas9, a RIP140 guide RNA and an amphipathic helical peptide for a sufficient amount of time to delete or inactivate RIP140 gene in the cell, and implanting into the subject the cell having the deleted or inactivated RIP140 gene.   
     
     
         32 . The method of  claim 31 , wherein the amphipathic helical peptide is selected from the group consisting of: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 5) 
                 
                     
                   H2N-LHHLLHHLLHHLHHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   H2N-LHKLLHHLLHHLHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   H2N-LHKLLHHLLHKLHHLLHKLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 8) 
                 
                     
                   H2N-LHHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 9) 
                 
                     
                   H2N-HHLLHHLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 10) 
                 
                     
                   H2N-LHLLHHLLHHLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 11) 
                 
                     
                   H2N-LHHLLHLLHHLLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   H2N-LHKLLHHLLHHLHK-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   H2N-LHKLLHHLHHLLHKL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   H2N-KLHHLLHKLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 15) 
                 
                     
                   H2N-HLHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 16) 
                 
                     
                   H2N-LHLLHHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 17) 
                 
                     
                   H2N-LHKLLHHLLHKLHHL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 18) 
                 
                     
                   H2N-LHLLHH-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 19) 
                 
                     
                   H2N-LHHLL-COOH; 
                 
                     
                 
                     
                   (SEQ ID NO: 20) 
                 
                     
                   H2N-LHKLL-COOH 
                 
                     
                 
                     
                   and 
                 
                     
                   Endo-Porter; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         wherein the amphipathic helical peptide is Endo-Porter; or 
         wherein the sequence-specific targeting nucleic acid is a guide RNA. 
       
     
     
         33 - 34 . (canceled) 
     
     
         35 . The method of  claim 31 , wherein the target gene is RIP140, optionally wherein the RIP140 gene is inactivated or deleted. 
     
     
         36 . (canceled) 
     
     
         37 . The method of  claim 31 , wherein:
 the method results in increased fatty acid oxidation in the subject;   the nucleic acid-guided endonuclease is Cas9;   the complex further comprises an aptamer molecule with binding specificity for the target cell;   the aptamer forms a non-covalent binding interaction with the amphipathic helical peptide.   the aptamer is conjugated to the amphipathic helical peptide; or   the complex is encapsulated in a glucan particle (GP).   
     
     
         38 - 42 . (canceled) 
     
     
         43 . The method of  claim 31 , wherein the subject is at risk for or suffering from a disorder related to glucose metabolism, optionally wherein the disorder is type 2 diabetes, prediabetes or gestational diabetes, optionally wherein the method results in one or more of a decrease in white fat levels, an increase in brown fat levels and an increase in beige fat levels. 
     
     
         44 - 52 . (canceled) 
     
     
         53 . A guide RNA of between 15 and 30 bases in length, that comprises a region which is at least 95% or 98% homologous to SEQ ID NO: 1, 2, 3, or 4. 
     
     
         54 - 68 . (canceled)

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