IP Library Granted Patent US 8,981,051
Granted Patent B2
US 8,981,051 · App. 13/625,162 · Granted Mar 17, 2015

Na+/K+-ATPase-specific peptide inhibitors/activators of Src and Src family kinases

Inventors: Zi-Jian Xie (Saline, MI); Joseph I. Shapiro (Toledo, OH); Jiang Tian (Perrysburg, OH); Zhichuan Li (Williamsville, NY)
Assignee: The University of Toledo
C07K14/4703A61K38/45A61K38/46C07K7/08C07K14/4705G01N33/573C12Y306/03009C12Y207/10002
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Quick Facts
Patent No.
US 8,981,051
App. No.
13/625,162
Granted
Mar 17, 2015
Kind
B2
Abstract

A method for regulating Src and its downstream signaling pathway which includes binding between Src and Na+/K+-ATPase is disclosed. The Na+/K+-ATPase/Src complex is a functional receptor for cardiotonic steroids such as ouabain. Also disclosed are Src inhibitors or activators which include either Na+/K+-ATPase or Src that interfere with the interaction between the Na/K-ATPase and Src, act via a different mechanism from ATP analogs, and is pathway (Na+/K+-ATPase) specific.

Claims (8)

1. A pharmaceutical composition for regulation of one or more signaling pathways involved in fibrosis, the composition comprising:

one or more Src and Src family kinases inhibitors comprised of one or more isolated peptides, or fragments thereof, that do not inhibit the ion pumping function of Na+/K+-ATPase;

wherein the one or more isolated peptides comprises the active isolated Src-inhibitory peptide (P3) consisting of the amino acid sequence of SEQ ID NO: 2.

2. The composition of claim 1 , wherein the one or more Src and Src family kinases inhibitors or activators modulates one or more signaling pathways that are related to cardiac fibrosis.

3. The composition of claim 1 , wherein the Src-modulating peptide (P3) is conjugated to a penetratin (TAT) peptide.

4. The composition of claim 3 , wherein the conjugated TAT-P3 peptide consists of the amino acid sequence of SEQ ID NO: 49.

5. The composition of claim 1 , wherein the Src-modulating peptide (P3) is conjugated to an antennapedia (AP) peptide.

6. The composition of claim 5 , wherein the AP-P3 peptide consists of the amino acid sequence of SEQ ID NO: 50.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 30, 2014
From: LI, ZHICHUAN
To: THE UNIVERSITY OF TOLEDO
Reel/Frame 032094/0593 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 28, 2013
From: XIE, ZI-JIAN; SHAPIRO, JOSEPH T.; TIAN, JIANG
To: THE UNIVERSITY OF TOLEDO
Reel/Frame 029900/0977 →
CONFIRMATORY LICENSE Recorded Nov 5, 2012
From: UNIVERSITY OF TOLEDO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 029244/0480 →
Continuity (3)
Division 12446856
Provisional Application 60855482 · Oct 21, 2006
Related Publication 20130150294A1 · Jun 13, 2013