The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 28, 2016

Filed:

Aug. 14, 2014
Applicant:

Tufts Medical Center, Inc., Boston, MA (US);

Inventors:

Athan Kuliopulos, Winchester, MA (US);

Georgios Koukos, Boston, MA (US);

Assignee:

Tufts Medical Center, Inc., Boston, MA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07K 16/40 (2006.01); A61K 31/00 (2006.01); A61K 45/06 (2006.01); A61L 17/00 (2006.01); A61L 27/54 (2006.01); A61L 29/16 (2006.01); A61L 31/16 (2006.01); A61K 31/65 (2006.01); A61K 38/08 (2006.01); A61K 38/10 (2006.01); A61K 39/395 (2006.01); A61K 39/00 (2006.01);
U.S. Cl.
CPC ...
C07K 16/40 (2013.01); A61K 31/00 (2013.01); A61K 31/65 (2013.01); A61K 38/08 (2013.01); A61K 38/10 (2013.01); A61K 39/3955 (2013.01); A61K 45/06 (2013.01); A61L 17/005 (2013.01); A61L 27/54 (2013.01); A61L 29/16 (2013.01); A61L 31/16 (2013.01); A61K 2039/505 (2013.01); A61L 2300/42 (2013.01); A61L 2300/434 (2013.01); A61L 2300/436 (2013.01); C07K 2317/76 (2013.01);
Abstract

Matrix metalloproteases (MMPs) play many important roles in normal and pathological remodeling processes including atherothrombotic disease, inflammation, angiogenesis and cancer. This invention relates to the activation of protease-activated receptor-1 (PAR-1) by endogenous platelet MMP-1 collagenase on the surface of platelets. Exposure of platelets to fibrillar collagen converts the surface-bound pro-MMP-1 zymogen to active MMP-1, which promotes aggregation through PAR-1. MMP-1 is shown to cleave the PAR-1 extracellular domain at a novel site, which then strongly activates Rho-GTP signaling pathways, cell shape change and motility, and MAPK signaling. Blockade of MMP-PAR1 suppresses thrombogenesis under arterial flow conditions and inhibited thrombosis in animals. These studies provide a link between matrix-dependent activation of metalloproteases and platelet-G protein signaling and identify MMP-1/PAR-1 as a new target for the treatment and prevention of arterial thrombosis and other thrombotic diseases.


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