发明名称 |
LYSOPHOSPHATIDIC ACID RECEPTOR TARGETING FOR SCLERODERMA AND OTHER FIBROTIC DISEASES |
摘要 |
LPA signaling through LPA1, but not LPA2, has been shown to be involved in the development of bleomycin-induced dermal fibrosis effecting both myofibroblast accumulation and TGF-ß-Smad signaling. In addition, genetic deletion, preventive pharmacological inhibition, and therapeutic pharmacological inhibition of LPA1 protected mice from dermal fibrosis. For example, a selective LPA1 receptor antagonist, AM095, attenuates dermal fibrosis when initiated after tissue injury onset in a therapeutic regimen. Consequently, antagonism of LPA1 may be effective in the treatment of patients with already existing fibrosis, as would be needed for clinically useful anti-fibrotic drugs. LPA-LPA1 inhibition has the potential to be an effective new therapeutic strategy for dermal fibrosis, and that LPA1 represents a viable target for pharmacological intervention. |
申请公布号 |
WO2011091167(A2) |
申请公布日期 |
2011.07.28 |
申请号 |
WO2011US21927 |
申请日期 |
2011.01.20 |
申请人 |
THE GENERAL HOSPITAL CORPORATION;TAGER, ANDREW, M.;LUSTER, ANDREW, D. |
发明人 |
TAGER, ANDREW, M.;LUSTER, ANDREW, D. |
分类号 |
A61K39/395;A61K9/06;A61K9/08;A61K31/42;A61K38/16;A61P1/16;A61P3/10;A61P9/10 |
主分类号 |
A61K39/395 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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