IP Library › Granted Patent US 12,544,458
Granted Patent B2
US 12,544,458 · App. 18/495,276 · Granted Feb 10, 2026

PAH-modulating compositions and methods

Inventors: Robert Charles Altshuler (Newton, MA); Anne Helen Bothmer (Cambridge, MA); Daniel Raymond Chee (Cambridge, MA); Cecilia Giovanna Silvia Cotta-Ramusino (Cambridge, MA); Kyusik Kim (Worcester, MA); Randi Michelle Kotlar (Arlington, MA); Gregory David McAllister (Cambridge, MA); Ananya Ray (Melrose, MA); Nathaniel Roquet (Philadelphia, PA); Carlos Sanchez (Boston, MA); Barrett Ethan Steinberg (Somerville, MA); William Edward Salomon (West Roxbury, MA); Robert James Citorik (Somerville, MA); William Querbes (Cambridge, MA); Luciano Henrique Apponi (Cambridge, MA); Zhan Wang (Cambridge, MA)
Assignee: Flagship Pioneering Innovations VI, LLC
A61K48/005A61P3/00C12N9/22C12N15/11
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Quick Facts
Patent No.
US 12,544,458
App. No.
18/495,276
Granted
Feb 10, 2026
Kind
B2
Abstract

The disclosure provides, e.g., compositions, systems, and methods for targeting, editing, modifying, or manipulating a host cell's genome at one or more locations in a DNA sequence in a cell, tissue, or subject. Gene modifying systems for treating phenylketonuria (PKU) are described.

Claims (37)

1 . A template RNA comprising, from 5′ to 3′:

a) a gRNA spacer that is complementary to a first portion of a human PAH gene, wherein the gRNA spacer comprises an RNA sequence of nucleotides 1 to 20 of SEQ ID NO: 37,221;

b) a gRNA scaffold that binds a SpyCas9 domain;

c) a heterologous object sequence comprising a mutation region to correct a mutation in a second portion of the human PAH gene, wherein the heterologous object sequence comprises a nucleotide sequence of nucleotides 97 to 105 of SEQ ID NO: 37,221; and

d) a primer binding site (PBS) sequence comprising at least 3 bases with 100% identity to a third portion of the human PAH gene, wherein the PBS sequence comprises a nucleotide sequence of nucleotides 106 to 116 of SEQ ID NO: 37,221.

2 . The template RNA of claim 1 , wherein the mutation to be corrected in the human PAH gene is R408W.

3 . The template RNA of claim 1 , wherein the gRNA spacer has a length of 20 nucleotides.

4 . The template RNA of claim 1 , wherein the heterologous object sequence has a length of 9-16 nucleotides.

5 . The template RNA of claim 1 , wherein the heterologous object sequence comprises, from 5′ to 3′, a post-edit homology region, a mutation region, and a pre-edit homology region.

6 . The template RNA of claim 1 , wherein the heterologous object sequence consists of an RNA sequence of GGGCCGAGG.

7 . The template RNA of claim 1 , wherein the PBS sequence has a length of 11-12 nucleotides.

8 . The template RNA of claim 1 , wherein the PBS sequence consists of an RNA sequence of 106 to 116 of SEO ID NO: 37,221.

9 . The template RNA of claim 1 , wherein the gRNA scaffold comprises an RNA sequence having at least 90% identity to nucleotides 21 to 96 of SEQ ID NO: 37,221.

10 . The template RNA of claim 1 , wherein the gRNA scaffold comprises an RNA sequence of nucleotides 21 to 96 of SEQ ID NO: 37,221.

11 . The template RNA of claim 1 , which comprises an RNA sequence having at least 90% identity to SEQ ID NO: 37,221.

12 . The template RNA of claim 1 , which comprises an RNA sequence of SEQ ID NO: 37,221.

13 . The template RNA of claim 1 , which comprises one or more chemically modified nucleotides.

14 . The template RNA of claim 13 , which comprises the RNA sequence and chemical modifications of SEQ ID NO: 30,500.

15 . A gene modifying system comprising:

a template RNA of claim 1 , and

a gene modifying polypeptide comprising a SpyCas9 nickase domain, or a nucleic acid encoding the gene modifying polypeptide.

16 . The gene modifying system of claim 15 , which comprises the nucleic acid encoding the gene modifying polypeptide, wherein the nucleic acid comprises RNA.

17 . The gene modifying system of claim 15 , wherein the gene modifying polypeptide comprises:

a reverse transcriptase (RT) domain;

a SpyCas9 nickase domain; and

a linker disposed between the RT domain and the SpyCas9 nickase domain.

18 . The gene modifying system of claim 17 , wherein the RT domain is an RT domain from a murine leukemia virus (MMLV), a porcine endogenous retrovirus (PERV), an Avian reticuloendotheliosis virus (AVIRE), a feline leukemia virus (FLV), a simian foamy virus (SFV), a bovine leukemia virus (BLV), a Mason-Pfizer monkey virus (MPMV), a human foamy virus (HFV), or a bovine foamy/syncytial virus (BFV/BSV).

19 . The gene modifying system of claim 18 , wherein the simian foamy virus is a SFV3L.

20 . The gene modifying system of claim 17 , which further comprises a second strand-targeting gRNA spacer that directs a second nick to a second strand of the human PAH gene.

21 . A pharmaceutical composition, comprising the gene modifying system of claim 15 and a pharmaceutically acceptable excipient or carrier.

22 . The pharmaceutical composition of claim 21 , wherein the pharmaceutically acceptable excipient or carrier is selected from the group consisting of a plasmid vector, a viral vector, a vesicle, and a lipid nanoparticle.

23 . A method for modifying a target site in the human PAH gene in a cell, the method comprising contacting the cell with the gene modifying system of claim 15 , or DNA encoding the same, thereby modifying the target site in the human PAH gene in a cell.

24 . A method for treating a subject having phenylketonuria (PKU) or hyperphenylalaninemia, the method comprising administering to the subject the gene modifying system of claim 15 thereby treating the subject havingPKU or hyperphenylalaninemia.

25 . A method of making the template RNA of claim 1 , the method comprising synthesizing the template RNA by in vitro transcription, solid-phase synthesis, or by introducing a DNA encoding the template RNA into a host cell under conditions that allow for production of the template RNA.

26 . A template RNA comprising a sequence having at least 90% identity to SEQ ID NO: 37221.

27 . The template RNA of claim 26 , which comprises a sequence having at least 95% identity to SEQ ID NO: 37221.

28 . The template RNA of claim 26 , which comprises a sequence having at least 99% identity to SEQ ID NO: 37221.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 18, 2024
From: ALTSHULER, ROBERT CHARLES; BOTHMER, ANNE HELEN; CHEE, DANIEL RAYMOND; COTTA-RAMUSINO, CECILIA GIOVANNA SILVIA; KIM, KYUSIK; KOTLAR, RANDI MICHELLE; MCALLISTER, GREGORY DAVID; RAY, ANANYA; ROQUET, NATHANIEL; SANCHEZ, CARLOS; STEINBERG, BARRETT ETHAN; SALOMON, WILLIAM EDWARD; CITORIK, ROBERT JAMES; QUERBES, WILLIAM; APPONI, LUCIANO HENRIQUE; WANG, ZHAN
To: TESSERA THERAPEUTICS, INC.
Reel/Frame 068942/0661 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 18, 2024
From: TESSERA THERAPEUTICS, INC.
To: FLAGSHIP PIONEERING INNOVATIONS VI, LLC
Reel/Frame 068942/0787 →
Continuity (5)
Continuation PCTUS2022076058 · Sep 7, 2022
Provisional Application 63367025 · Jun 24, 2022
Provisional Application 63303927 · Jan 27, 2022
Provisional Application 63241897 · Sep 8, 2021
Related Publication 20240082429A1 · Mar 14, 2024
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