IP Library › Granted Patent US 12,351,610
Granted Patent B2
US 12,351,610 · App. 17/608,487 · Granted Jul 8, 2025

Interferon regulatory factor 5 inhibitors and uses thereof

Inventors: Betsy J. Barnes (Glenwood Landing, NY); Shan Sun (Wingdale, NY)
Assignee: THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
C07K14/47A61P37/00A61K38/00
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Quick Facts
Patent No.
US 12,351,610
App. No.
17/608,487
Granted
Jul 8, 2025
Kind
B2
Abstract

Polypeptides comprising a cell penetrating amino acid sequence and an interferon regulatory factor 5 (IRF5) targeting amino acid sequence are disclosed, where the IRF5 targeting amino acid sequence is one or more of RHATRHG (SEQ ID NO:1), KSRDFRL (SEQ ID NO:2) and GPRDMPP (SEQ ID NO:3), as well as methods of using these polypeptides to treat diseases, such as autoimmune and inflammatory diseases.

Claims (11)

1. A polypeptide consisting of a cell penetrating amino acid sequence and an interferon regulatory factor 5 (IRF5) targeting amino acid sequence, wherein the IRF5 targeting amino acid sequence consists of one or more of RHATRHG (SEQ ID NO:1), KSRDFRL (SEQ ID NO:2) and GPRDMPP (SEQ ID NO:3).

2. The polypeptide of claim 1 , wherein the cell penetrating amino acid sequence comprises a sequence at least 90% identical to DRQIKIWFQNRRMKWKK (SEQ ID NO: 4), AAVALLPAVLLALLAP (SEQ ID NO:5), GRKKRRQRRRPPQ (SEQ ID NO:6), CSIPPEVKFNKPFVYLI (SEQ ID NO:7), KKWKMRRNQFWVKVQRG (SEQ ID NO:8), KLLKLLLKLWLKLLKLLL (SEQ ID NO:9), INLKALAALAKKIL (SEQ ID NO:10), RQIKIWFQNRRMKWKKGG (SEQ ID NO:11), GWTLNSAGYLLGKINLKALAALAKKIL (SEQ ID NO:12), YLKFIPLKRAIWLIK ID NO: 13), (SEQ MANLGYWLLALFVTMWTDVGLCKKRPKP (SEQ ID NO:14), RQIKIWFQNRRMKWKK (SEQ ID NO:15) or LCLRPVG (SEQ ID NO:16).

3. The polypeptide of claim 1 , wherein the cell penetrating amino acid sequence comprises DRQIKIWFQNRRMKWKK (SEQ ID NO:4), AAVALLPAVLLALLAP (SEQ ID NO:5), GRKKRRQRRRPPQ (SEQ ID NO:6), CSIPPEVKFNKPFVYLI (SEQ ID NO:7), KKWKMRRNQFWVKVQRG (SEQ ID NO:8), KLLKLLLKLWLKLLKLLL (SEQ ID NO:9), INLKALAALAKKIL (SEQ ID NO:10), RQIKIWFQNRRMKWKKGG (SEQ ID NO:11), GWTLNSAGYLLGKINLKALAALAKKIL (SEQ ID NO:12), (SEQ YLKFIPLKRAIWLIK ID NO: 13), MANLGYWLLALFVTMWTDVGLCKKRPKP (SEQ ID NO:14), RQIKIWFQNRRMKWKK (SEQ ID NO:15) or LCLRPVG (SEQ ID NO:16).

4. A polypeptide comprising a cell penetrating amino acid sequence and an interferon regulatory factor 5 (IRF5) targeting amino acid sequence, wherein the polypeptide comprises an amino acid sequence at least 90% identical to DRQIKIWFQNRRMKWKKRHATRHG (SEQ ID NO:17), DRQIKIWFQNRRMKWKKKSRDFRL (SEQ ID NO:18) or DRQIKIWFQNRRMKWKKGPRDMPP (SEQ ID NO:19).

5. A polypeptide comprising a cell penetrating amino acid sequence and an interferon regulatory factor 5 (IRF5) targeting amino acid sequence, wherein the polypeptide comprises amino acid sequence DRQIKIWFQNRRMKWKKRHATRHG (SEQ ID NO: 17), DRQIKIWFQNRRMKWKKKSRDFRL (SEQ ID NO:18) or DRQIKIWFQNRRMKWKKGPRDMPP (SEQ ID NO:19).

6. The polypeptide of claim 4 , wherein the polypeptide consists of an amino acid sequence at least 90% identical to DRQIKIWFQNRRMKWKKRHATRHG (SEQ ID NO: 17), DRQIKIWFQNRRMKWKKKSRDFRL (SEQ ID NO:18) or DRQIKIWFQNRRMKWKKGPRDMPP (SEQ ID NO:19).

7. The polypeptide of claim 5 , wherein the polypeptide consists of amino acid sequence DRQIKIWFQNRRMKWKKRHATRHG (SEQ ID NO:17), DRQIKIWFQNRRMKWKKKSRDFRL (SEQ ID NO: 18) or DRQIKIWFQNRRMKWKKGPRDMPP (SEQ ID NO:19).

8. A nucleic acid sequence encoding the polypeptide of claim 1 .

9. A pharmaceutical composition comprising the polypeptide of claim 1 and a pharmaceutically acceptable carrier.

10. A kit comprising the polypeptide of claim 1 , at least one other therapeutic agent, and instructions for administering the polypeptide and the other therapeutic agent(s) to a patient to treat an autoimmune disease, classical Hodgkin lymphoma, atherosclerosis, cardiovascular disease, neuropathic pain, leukemia or lymphoma.

11. The polypeptide of claim 1 , wherein the cell penetrating amino acid sequence is selected from the group consisting of DRQIKIWFQNRRMKWKK (SEQ ID NO:4), AAVALLPAVLLALLAP (SEQ ID NO:5), GRKKRRQRRRPPQ (SEQ ID NO:6), CSIPPEVKFNKPFVYLI (SEQ ID NO:7), KKWKMRRNQFWVKVQRG (SEQ ID NO:8), KLLKLLLKLWLKLLKLLL (SEQ ID NO:9), INLKALAALAKKIL (SEQ ID NO:10), RQIKIWFQNRRMKWKKGG (SEQ ID NO:11), GWTLNSAGYLLGKINLKALAALAKKIL (SEQ ID NO:12), YLKFIPLKRAIWLIK (SEQ ID NO:13), MANLGYWLLALFVTMWTDVGLCKKRPKP (SEQ ID NO:14), RQIKIWFQNRRMKWKK (SEQ ID NO:15) and LCLRPVG (SEQ ID NO:16).

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2021
From: BARNES, BETSY J.; SUN, SHAN
To: THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
Reel/Frame 058003/0574 →
Continuity (2)
Provisional Application 62844894 · May 8, 2019
Related Publication 20220220168A1 · Jul 14, 2022
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