Invention Grant
US08435964B2 Ectonucleotidase pyrophosphate/phosphodiestrase-1 (ENPP-1) as a target for the treatment of aortic valve stenosis and cardiovascular calcification
有权
作为治疗主动脉瓣狭窄和心血管钙化的靶标的核糖核苷酸焦磷酸/磷酸二酯酶-1（ENPP-1）
- Patent Title: Ectonucleotidase pyrophosphate/phosphodiestrase-1 (ENPP-1) as a target for the treatment of aortic valve stenosis and cardiovascular calcification
- Patent Title (中): 作为治疗主动脉瓣狭窄和心血管钙化的靶标的核糖核苷酸焦磷酸/磷酸二酯酶-1（ENPP-1）
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Application No.: US12908467Application Date: 2010-10-20
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Publication No.: US08435964B2Publication Date: 2013-05-07
- Inventor: Patrick Mathieu
- Applicant: Patrick Mathieu
- Applicant Address: CA Quebec, Quebec
- Assignee: Universite Laval
- Current Assignee: Universite Laval
- Current Assignee Address: CA Quebec, Quebec
- Agency: Norton Rose Canada LLP
- Priority: CA2684017 20091022
- Main IPC: G01N33/573
- IPC: G01N33/573 ; C12Q1/44 ; A61K31/7076 ; C07H19/20 ; A61P9/00
Abstract:
Aortic valve stenosis (AS) is a chronic process related to a progressive mineralization of the aortic root and valve cusps. We found in human AS valves a high level of expression and enzymatic activity of ectonucleotide pyrophosphatase/phosphodiesterase-1 (ENPP-1), which correlated to the degree of mineralization. In vitro, inhibition of ENPP activity with ARL 67156 significantly reduced calcification of isolated valve interstitial cells. In a rat model of cardiovascular calcification, ARL 67156 significantly reduced calcification of the aortic root and valve cusps. This is the first study to demonstrate that increased expression and activity of ENPP-1 promotes the mineralization process in AS valves. Hence, inhibition of ectonucleotidase may represent a novel target of therapy for this frequent and serious cardiovascular disease.
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