Granted Patent
B2
US 12,286,625 · App. 16/947,905 · Granted Apr 29, 2025
Inhibition of mir-22 miRNA by APT-110
Assignee:
APTAMIR THERAPEUTICS, INC.
C12N15/113A61K9/127A61K31/202A61K31/7125A61K47/14A61K47/66A61K47/6917A61P3/04C12N2310/113C12N2310/321C12N2310/3341
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Abstract
Increase of energy expenditure as an effective treatment of obesity and related disorders is a target for drug research and development. A 15% increase of energy expenditure is believed to be sufficient to achieve significant weight and fat mass reduction while providing meaningful improvement of metabolic parameters. Disclosed herein is a method for pharmacological inhibition of miR-22-3p, which represents a new therapeutic approach for treating human obesity, diabetes, and hypercholesterolemia.
Claims (16)
1. A mir-22 miRNA antagonist of the formula (SEQ ID NO: 4)
2. The mir-22 miRNA antagonist of claim 1 , wherein the mir-22 miRNA is the mature miR-22-3p.
3. A method of increasing thermogenesis in a subject comprising administering to the subject the mir-22 miRNA antagonist of claim 1 .
4. The mir-22 miRNA antagonist of claim 1 , wherein the mir-22 miRNA antagonist is conjugated to a fatty acid.
5. The mir-22 miRNA antagonist of claim 4 , wherein the fatty acid is a C10-35 chain fatty acid.
6. The mir-22 miRNA antagonist of claim 4 , wherein the fatty acid is selected from decanoic acid, palmitic acid, dodecanoic acid, oleic acid, stearic acid, eicosapentaenoic acid, docosanoic acid, docosahexaenoic acid, and dotriacontahexaenoic acid.
7. A method for delivering a mir-22 miRNA antagonist to an adipocyte of a subject comprising administering the mir-22 miRNA antagonist of claim 2 to the adipocyte.
8. The method of claim 7 , wherein the adipocyte is in vivo.
9. The method of claim 7 , wherein at least 50% of the mir-22 miRNA antagonist is delivered to adipocytes of the subject.
10. The mir-22 miRNA antagonist of claim 1 , wherein the mir-22 miRNA antagonist is conjugated to a polypeptide.
11. The mir-22 miRNA antagonist of claim 10 , wherein the polypeptide is a polypeptide comprising the sequence GVITRIR (SEQ ID NO: 1).
12. The mir-22 miRNA antagonist of claim 10 , wherein the polypeptide is a polypeptide comprising the sequence CKGGRAKDC (SEQ ID NO: 3).
13. The mir-22 miRNA antagonist of claim 10 , wherein the polypeptide is Hexarelin (His-(D)2-methyl-Trp-Ala-Trp-(D)Phe-Lys-NH 2 ).
14. The mir-22 miRNA antagonist of claim 1 , wherein the mir-22 miRNA antagonist is conjugated to a targeting element.
15. A mir-22 miRNA antagonist, wherein the mir-22 miRNA antagonist structure comprises SEQ ID NO: 16.
16. A mir-22 miRNA antagonist, wherein the mir-22 miRNA antagonist structure comprises SEQ ID NO: 18.
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Aug 24, 2020
From: THIBONNIER, MARC
To: APTAMIR THERAPEUTICS, INC.
Reel/Frame 053574/0706 →
Continuity (3)
Continuation
16097012
Provisional Application
62329537
· Apr 29, 2016
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