IP Library Granted Patent US 11,389,546
Granted Patent B2
US 11,389,546 · App. 15/781,827 · Granted Jul 19, 2022

Heterologous UTR sequences for enhanced mRNA expression

Inventors: David H. Burkhardt (Somerville, MA); Romesh R. Subramanian (Framingham, MA); Christian Cobaugh (Newton Highlands, MA)
Assignee: ModernaTX, Inc.
A61K48/0058A61K31/712A61K31/7115A61K31/7125A61K48/0066A61P1/16A61P31/14C12N15/1086C12N15/67C12N2840/00
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Quick Facts
Patent No.
US 11,389,546
App. No.
15/781,827
Granted
Jul 19, 2022
Kind
B2
Abstract

mRNAs containing an exogenous open reading frame (ORF) flanked by a 5′ untranslated region (UTR) and a 3′ UTR is provided, wherein the 5′ and 3′ UTRs are derived from a naturally abundant mRNA in a tissue. Also provided are methods for identifying the 5′ and 3′ UTRs, and methods for making and using the mRNAs.

Claims (12)

1. A method of expressing a protein in a liver tissue, comprising providing an mRNA to said liver tissue, wherein the mRNA comprises an open reading frame (ORF) that encodes said protein, flanked by a heterologous 5′ untranslated region (UTR) and/or a heterologous 3′ UTR, wherein the 5′ UTR and/or the 3′ UTR are derived from a gene selected from the group consisting of Haptoglobin (HP), Haptoglobin-Related Protein (HPR), Complement Component 3 (C3), Alpha-1-antitrypsin (SERPINA1), Alpha-1-antichymotrypsin (SERPINA3), Fibrinogen Alpha Chain (FGA), and Fibrinogen Beta Chain (FGB).

2. The method of claim 1 , wherein the mRNA comprises at least one modified or non-naturally occurring nucleotide.

3. The method of claim 2 , wherein the at least one modified or non-naturally occurring nucleotide comprises at least one backbone modification, sugar modification or base modification.

4. The method of claim 3 , wherein the at least one modified or non-naturally occurring nucleotide comprises at least one base modification.

5. The method of claim 4 , wherein the at least one base modification is selected from the group consisting of: 2-amino-6-chloropurine riboside 5′ triphosphate, 2-aminoadenosine 5′ triphosphate, 2-thiocytidine 5′ triphosphate, 2-thiouridine 5′ triphosphate, 4-thiouridine 5′ triphosphate, 5-aminoallylcytidine 5′ triphosphate, 5-aminoallyluridine 5′ triphosphate, 5-bromocytidine 5′ triphosphate, 5-bromouridine 5′ triphosphate, 5-iodocytidine 5′ triphosphate, 5-iodouridine 5′ triphosphate, 5-methylcytidine 5′ triphosphate, 5-methyluridine 5′ triphosphate, 6-azacytidine 5′ triphosphate, 6-azauridine 5′ triphosphate, 6-chloropurine riboside 5′-triphosphate, 7-deazaadenosine 5′ triphosphate, 7-deazaguanosine 5′ triphosphate, 8-azaadenosine 5′ triphosphate, 8-azidoadenosine 5′ triphosphate, benzimidazole riboside 5′ triphosphate, N 1 -methyladenosine 5′ triphosphate, N 1 -methylguanosine 5′ triphosphate, N 6 -methyladenosine 5′ triphosphate, O 6 -methylguanosine 5′ triphosphate, N 1 -methyl-pseudouridine 5′ triphosphate, puromycin 5′-triphosphate and xanthosine 5′ triphosphate.

6. The method of claim 5 , wherein the at least one modified or non-naturally occurring nucleotide is N 1 -methyl-pseudouridine 5-triphosphate.

7. The method of claim 1 , wherein the mRNA comprises a heterologous 5′ UTR derived from a gene selected from the group consisting of: HP, FGB, HPR, C3, FGA, SERPINA1 and SERPINA3.

8. The method of claim 1 , wherein the 5′ UTR comprises a nucleotide sequence selected from the group consisting of: SEQ ID NOS:1-3, 5-7, and 10.

9. The method of claim 1 , wherein the ORF is therapeutic gene.

10. The method of claim 9 , wherein the therapeutic gene is selected from the group consisting of: interferon alpha, TNF related apoptosis-inducing ligand, vascular adhesion protein 1, hepatocyte growth factor, G6PC, ABCB11, ABCB4, ASL1, ASS, Arg1, AGXT, OTC, CBS, PAH, GBE, GALE, HADH, MCCC1, MMA, ADAMTS13, SLC25A15, C2, F2, PROS1, SERPINA1, GALT1, ETFA, GCDH, CTNS, FAH, TAT, HPD, HSD17b4, SLC2A2, GALC, ABCC6, AHSG, PDC-E2, GAA, ATP8B1, MMACHC, GK, PCCA, PCCB and UGT1A1.

11. The method of claim 1 , wherein the mRNA comprises a heterologous 5′ UTR derived from the FGB gene.

12. The method of claim 1 , wherein the 5′ UTR comprises the nucleotide sequence set forth in SEQ ID NO:2.

Assignments (3)
SECURITY INTEREST Recorded Nov 19, 2025
From: MODERNATX, INC.
To: ARES CAPITAL CORPORATION, AS AGENT
Reel/Frame 073634/0354 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2018
From: BURKHARDT, DAVID H.; SUBRAMANIAN, ROMESH R.; COBAUGH, CHRISTIAN
To: ALEXION PHARMACEUTICALS, INC.
Reel/Frame 046313/0494 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2018
From: ALEXION PHARMACEUTICALS, INC.
To: MODERNATX, INC.
Reel/Frame 046313/0517 →
Continuity (2)
Provisional Application 62265233 · Dec 9, 2015
Related Publication 20180353618A1 · Dec 13, 2018