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1. 发明申请

WO2010015421A1 USE OF CONKUNITZIN-S1 FOR THE MODULATION OF GLUCOSE-INDUCED INSULIN SECRETION 审中-公开
标题翻译：用于调节葡萄糖诱导的胰岛素分泌的康宁嗪-S1
公开(公告)号：WO2010015421A1
公开(公告)日：2010-02-11
申请号：PCT/EP2009/005801
申请日：2009-08-10
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. BERLIN , UNIVERSITÄT ZU LÜBECK , TERLAU, Heinrich , FINOL-URDANETA, Rocio , BECKER, Stefan , RAASCH, Walter
发明人： TERLAU, Heinrich , FINOL-URDANETA, Rocio , BECKER, Stefan , RAASCH, Walter
IPC分类号： C07K14/435
CPC分类号： C07K14/43504 , C07K14/8114
摘要： The present invention relates to a (poly)peptide or a peptidomimetic thereof having the biological activity of Conkunitzin-S1, wherein said (poly)peptide is selected from (a) a polypeptide comprising or having the amino acid sequence of SEQ ID NO: 1; (b) a polypeptide having at least 85% sequence identity to SEQ ID NO:1; or (c) a fragment of a) or b); wherein said (poly)peptide or peptidomimetic specifically modulates the activity of a channel having the activity of a Kv1.7 containing channel, for the treatment or prevention of metabolic diseases or conditions, or secondary diseases or conditions related to said metabolic diseases or conditions. The present invention furthermore relates to a method of screening for (poly)peptides derived from Conkunitzin-S1 suitable for specifically modulating the activity of a channel having the activity of a Kv1.7 containing channel, comprising: (a) altering the amino acid sequence of Conkunitzin-S1 represented by SEQ ID NO: 1 by deleting and/or inserting and/or replacing at least one amino acid; and (b) determining the modulatory effect of the (poly)peptide obtained in step (a) (i) on a channel having the activity of a Kv1.7 containing channel and (ii) on channels, preferably potassium channels, not having the activity of a Kv1.7 containing channel, which are optionally expressed on the same cell as the channel having the activity of a Kv1.7 containing channel; wherein a modulatory effect of the (poly)peptide determined in step (i) that is at least 50% of the modulatory effect of Conkunitzin-S1 indicates that the (poly)peptide re suitable for modulating the activity of said channel having the activity of a Kv1.7 containing channel; and wherein the determination of essentially no modulatory effect in step (ii) indicates that the (poly)peptide is specifically modulating the activity of channels having the activity of a Kv1.7 containing channel.
摘要翻译：本发明涉及具有Conkunitzin-S1生物活性的（多）肽或其肽模拟物，其中所述（多）肽选自（a）包含或具有SEQ ID NO：1的氨基酸序列的多肽 ; （b）与SEQ ID NO：1具有至少85％序列同一性的多肽; 或（c）a）或b）的片段; 其中所述（多）肽或肽模拟物特异性调节具有Kv1.7含有通道活性的通道的活性，用于治疗或预防代谢疾病或病症，或与所述代谢疾病或病症有关的继发性疾病或病症。本发明还涉及一种筛选衍生自Conkunitzin-S1的（多）肽的方法，其适用于特异性调节含有Kv1.7含有通道活性的通道的活性，其包括：（a）改变氨基酸序列通过删除和/或插入和/或替换至少一个氨基酸的由SEQ ID NO：1表示的Conkunitzin-S1; （b）确定步骤（a）（i）中获得的（多）肽对具有Kv1.7含有通道活性的通道的调节作用，和（ii）在不具有含有Kv1.7的通道的活性，其任选地在与具有含有Kv1.7的通道的活性的通道相同的细胞上表达; 其中在步骤（i）中测定的所述（多）肽的调节作用是Conkunitzin-S1的调节作用的至少50％，这表明（多）肽适合于调节具有活性的所述通道的活性包含Kv1.7通道; 并且其中在步骤（ii）中基本上没有调节作用的测定表明（多）肽特异性调节具有含有Kv1.7的通道的活性的通道的活性。

2. 发明公开

EP2367848A1 USE OF CONKUNITZIN-S1 FOR THE MODULATION OF GLUCOSE-INDUCED INSULIN SECRETION 审中-公开
标题翻译： CONKUNITZIN-S1的调制糖诱导INSULINSEZERNIERUNG的使用
公开(公告)号：EP2367848A1
公开(公告)日：2011-09-28
申请号：EP09804528.9
申请日：2009-08-10
申请人： Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. , Universität zu Lübeck
发明人： TERLAU, Heinrich , FINOL-URDANETA, Rocio , BECKER, Stefan , RAASCH, Walter
IPC分类号： C07K14/435
CPC分类号： C07K14/43504 , C07K14/8114
摘要： The present invention relates to a (poly)peptide or a peptidomimetic thereof having the biological activity of Conkunitzin-S1, wherein said (poly)peptide is selected from (a) a polypeptide comprising or having the amino acid sequence of SEQ ID NO: 1; (b) a polypeptide having at least 85% sequence identity to SEQ ID NO:1; or (c) a fragment of a) or b); wherein said (poly)peptide or peptidomimetic specifically modulates the activity of a channel having the activity of a Kv1.7 containing channel, for the treatment or prevention of metabolic diseases or conditions, or secondary diseases or conditions related to said metabolic diseases or conditions. The present invention furthermore relates to a method of screening for (poly)peptides derived from Conkunitzin-S1 suitable for specifically modulating the activity of a channel having the activity of a Kv1.7 containing channel, comprising: (a) altering the amino acid sequence of Conkunitzin-S1 represented by SEQ ID NO: 1 by deleting and/or inserting and/or replacing at least one amino acid; and (b) determining the modulatory effect of the (poly)peptide obtained in step (a) (i) on a channel having the activity of a Kv1.7 containing channel and (ii) on channels, preferably potassium channels, not having the activity of a Kv1.7 containing channel, which are optionally expressed on the same cell as the channel having the activity of a Kv1.7 containing channel; wherein a modulatory effect of the (poly)peptide determined in step (i) that is at least 50% of the modulatory effect of Conkunitzin-S1 indicates that the (poly)peptide re suitable for modulating the activity of said channel having the activity of a Kv1.7 containing channel; and wherein the determination of essentially no modulatory effect in step (ii) indicates that the (poly)peptide is specifically modulating the activity of channels having the activity of a Kv1.7 containing channel.

3. 发明申请

WO2006098764A2 POTASSIUM CHANNEL BLOCKERS 审中-公开
标题翻译：钾通道阻塞剂
公开(公告)号：WO2006098764A2
公开(公告)日：2006-09-21
申请号：PCT/US2005/032129
申请日：2005-09-09
申请人： UNIVERSITY OF UTAH RESEARCH FOUNDATION , COGNETIX, INC. , MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. , OLIVERA, Baldomero, M. , TERLAU, Heinrich , IMPERIAL, Julita, S. , GARRETT, James, E.
发明人： OLIVERA, Baldomero, M. , TERLAU, Heinrich , IMPERIAL, Julita, S. , GARRETT, James, E.
IPC分类号： A61K38/16 , C07K14/435
CPC分类号： C07K14/43504 , A61K38/00
摘要： The present invention is directed to conopeptides termed conkunitzins and their use for blocking the flow of potassium ions through voltage-gated potassium channels. In view of the Kunitz domain in the conkunitzins, they are also useful for inhibiting platelet aggregation and as protease inhibitors.
摘要翻译：本发明涉及称为康尼他嗪的肽，以及它们用于阻断钾离子通过电压门控钾通道流动的用途。鉴于康un嗪中的Kunitz结构域，它们也可用于抑制血小板聚集和蛋白酶抑制剂。

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