发明公开
- 专利标题： GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS
- 专利标题（中）： COAGONISTEN DES GLUCAGON / GLP-1 ReZEPTORS
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申请号： EP10838149.2申请日： 2010-12-09
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公开(公告)号： EP2512503A2公开(公告)日： 2012-10-24
- 发明人: DIMARCHI, Richard, D.
- 申请人： Indiana University Research and Technology Corporation
- 申请人地址： 351 West 10th Street Indianapolis, IN 46204 US
- 专利权人： Indiana University Research and Technology Corporation
- 当前专利权人： Indiana University Research and Technology Corporation
- 当前专利权人地址： 351 West 10th Street Indianapolis, IN 46204 US
- 代理机构： Ponti Sales, Adelaida
- 优先权： US288248P 20091218
- 国际公布： WO2011075393 20110623
- 主分类号： A61K38/26
- IPC分类号： A61K38/26
摘要：
Provided herein are glucagon analogs comprising a modified amino acid sequence of native human glucagon (SEQ ID NO: 2) that exhibit activity at the glucagon receptor, activity at the GLP-I receptor, or activity at each of the glucagon recpeotr and the GLP-I receptor. In some embodiments, the glucagon analog exhibits at least 100% or more of the activity of native glucagon at the glucagon receptor and/or at least 100% or more of the activity of native GLP-I at the GLP-I receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is within 50-fold or less than the EC50 at the glucagon receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-I receptor which is two- to ten-fold greater than the EC50 at the glucagon receptor. Related conjugates, dimers and multimers, and pharmaceutical compositions, and uses thereof, are further provided.
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