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1. 发明授权

US08148083B2 Methods of screening for TRPM4 modulators of insulin secretion 有权
标题翻译：筛选胰岛素分泌的TRPM4调节剂的方法
公开(公告)号：US08148083B2
公开(公告)日：2012-04-03
申请号：US11753914
申请日：2007-05-25
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： G01N33/53
CPC分类号： G01N33/507 , G01N33/6872 , G01N2333/62 , G01N2333/705 , G01N2800/042
摘要： The invention relates to methods useful in identifying candidate agents that modulate insulin secretion from an insulin secreting cell, where such molecules modulate TRPM4 activity and expression in the insulin secreting cell.
摘要翻译：本发明涉及用于鉴定调节胰岛素分泌细胞的胰岛素分泌的候选试剂的方法，其中这样的分子调节TRPM4活性并在胰岛素分泌细胞中表达。

2. 发明申请

US20090098546A1 Methods of Screening for LTRPC7 Modulators 有权
标题翻译： LTRPC7调制器筛选方法
公开(公告)号：US20090098546A1
公开(公告)日：2009-04-16
申请号：US12128471
申请日：2008-05-28
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： C12Q1/68 , G01N33/53
CPC分类号： G01N33/6872 , C07K14/705 , G01N2500/04
摘要： The present invention relates to the identification and isolation of a novel family of ATP regulated calcium transmembrane channel polypeptides designated herein as “LTRPC7” (Long Transient Receptor Potential Channel). Channels comprising these polypeptides close in response to concentrations of cytoplasmic ATP in the millimolar range, are subject to inhibition by high intracellular levels of calcium and/or magnesium, and do not respond to depletion or reduction in intracellular calcium stores. The invention further relates to the methods of utilizing LTRPC7 for binding, and the methods for modulating LTRPC7 activity and for measuring LTRPC2 permeability. The invention further relates to the methods of modulating expression of LTRPC7.
摘要翻译：本发明涉及鉴定和分离本文称为“LTRPC7”（长瞬态受体电位通道）的ATP调节的钙跨膜通道多肽的新家族。包含这些多肽的通道在毫微克范围内响应细胞质ATP的浓度而接近的细胞受到钙和/或镁的高细胞内水平的抑制，并且不对细胞内钙储存物的消耗或减少作出反应。本发明还涉及使用LTRPC7进行结合的方法，以及调节LTRPC7活性和测量LTRPC2渗透性的方法。本发明还涉及调节LTRPC7表达的方法。

3. 发明申请

US20090053753A1 FUNCTIONAL IDENTIFICATION OF PROTEINS UNDERLYING Icrac ACTIVITY IN A CELL 有权
标题翻译：在细胞中的Icrac活性的蛋白质的功能鉴定
公开(公告)号：US20090053753A1
公开(公告)日：2009-02-26
申请号：US12053318
申请日：2008-03-21
申请人： Reinhold PENNER , Andrea Fleig
发明人： Reinhold PENNER , Andrea Fleig
IPC分类号： C12Q1/02
CPC分类号： G01N33/6872 , G01N2500/10
摘要： The invention provides methods and compositions for determining the identity of CRACM homologs underlying Icrac activity in cells.
摘要翻译：本发明提供用于确定细胞中Icrac活性的CRACM同系物的身份的方法和组合物。

4. 发明申请

US20110230368A1 High Throughput Assays for TRPM7 审中-公开
标题翻译： TRPM7的高吞吐量测定
公开(公告)号：US20110230368A1
公开(公告)日：2011-09-22
申请号：US12916222
申请日：2010-10-29
申请人： Reinhold PENNER , Andrea Fleig , F. David Horgen
发明人： Reinhold PENNER , Andrea Fleig , F. David Horgen
IPC分类号： C40B30/06 , C07D311/94
CPC分类号： G01N33/6872 , G01N2500/10
摘要： The present invention provides high throughput assays for TRPM7 activity. The present invention encompasses methods and compositions for screening a sample for inhibitors of TRPM7, including methods and compositions for competitive high throughput assays.
摘要翻译：本发明提供TRPM7活性的高通量测定。本发明包括用于筛选TRPM7抑制剂样品的方法和组合物，包括用于竞争性高通量测定的方法和组合物。

5. 发明申请

US20050202472A1 Methods of screening for LTRPC2 modulators 审中-公开
标题翻译：筛选LTRPC2调节剂的方法
公开(公告)号：US20050202472A1
公开(公告)日：2005-09-15
申请号：US11035150
申请日：2005-01-12
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： G01N33/50 , C07K14/705 , C12N15/09 , C12N15/12 , C12Q1/02 , C12Q1/68 , G01N33/15 , G01N33/68 , C12N15/85
CPC分类号： G01N33/6872 , C07K14/705 , C12Q1/6876 , C12Q2600/136 , C12Q2600/158
摘要： The present invention relates to the identification and isolation of a novel family of ADP ribose (“ADPR) regulated calcium transmembrane channel polypeptides designated herein as “LTRPC2” (Long Transient Receptor Potential Channel). Channels comprising these polypeptides open in response to concentrations of cytoplasmic ADPR in the micromolar range, exhibit enhanced activity in the presence of high intracellular levels of calcium, and do not respond to depletion or reduction in intracellular calcium stores. The invention further relates to the methods of utilizing LTRPC2 for binding, and the methods for modulating LTRPC2 activity and for measuring LTRPC2 permeability. The invention further relates to the methods of modulating expression of LTRPC2.
摘要翻译：本发明涉及鉴定和分离本文称为“LTRPC2”（长时间受体电位通道）的ADP核糖（“ADPR”）调节的钙跨膜通道多肽的新家族。包含这些多肽的通道响应于细胞质浓度而开放 ADPR在微摩尔范围内，在高细胞内钙浓度的存在下表现出增强的活性，并且不对细胞内钙储存物的耗尽或减少作出反应。本发明还涉及利用LTRPC2结合的方法，以及调节方法 LTRPC2活性和测量LTRPC2渗透性的方法。本发明还涉及调节LTRPC2表达的方法。

6. 发明授权

US07452675B2 Methods of screening for TRPM4b modulators 有权
标题翻译：筛选TRPM4b调节剂的方法
公开(公告)号：US07452675B2
公开(公告)日：2008-11-18
申请号：US10142649
申请日：2002-05-08
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： G01N33/53 , C12P21/02
CPC分类号： G01N33/6872 , C40B30/06 , G01N2500/00
摘要： The invention relates, in part, to methods useful in identifying molecules, that bind TRPM4b, which modulate TRPM4b ion channel activity, and/or which alter expression of TRPM4b within cells. The TRPM4b channels as described herein contain TRPM4b polypeptides, which are in turn encoded by TRPM4b nucleic acids. The ion channels described herein are preferably formed in HEK-293 cells from one or more novel TRPM4b polypeptides, which exhibit one or more of the unique TRPM4b properties described herein.
摘要翻译：本发明部分地涉及可用于鉴定结合调节TRPM4b离子通道活性的TRPM4b和/或改变TRPM4b在细胞内的表达的分子的分子。如本文所述的TRPM4b通道包含TRPM4b多肽，其又由TRPM4b核酸编码。本文所述的离子通道优选在来自一种或多种新的TRPM4b多肽的HEK-293细胞中形成，其表现出本文所述的一种或多种独特的TRPM4b性质。

7. 发明申请

US20080096227A1 CRAC modulators and use of same for drug discovery 审中-公开
标题翻译： CRAC调节剂并用于药物发现
公开(公告)号：US20080096227A1
公开(公告)日：2008-04-24
申请号：US11733640
申请日：2007-04-10
申请人： Reinhold Penner , Andrea Fleig , Jean-Pierre Kinet
发明人： Reinhold Penner , Andrea Fleig , Jean-Pierre Kinet
IPC分类号： C12N5/02 , G01N33/53
CPC分类号： G01N33/6872 , C12N15/113 , C12N2310/11 , C12N2310/14 , G01N33/5038
摘要： The invention relates to use of a calcium release activated Ca+2 (CRAC) channel (CRACM) such as CRACM1 and CRACM2 to identify bioactive agents which can modulate store operated calcium entry and CRAC channel activity. The invention further relates to the use of recombinant nucleic acids that encode CRACM. One aspect of the invention includes methods of determining binding of candidate bioactive agents to a CRACM polypeptide and for determining modulation of CRACM polypeptide activity as it affects CRAC channel permeability. The invention further relates to methods and compositions modulating the cellular expression of the nucleic acids that encode CRACM.
摘要翻译：本发明涉及钙释放活化的Ca 2+（CRAC）通道（CRACM）如CRACM1和CRACM2的用途，以鉴定可调节储存操作的钙进入和CRAC通道活性的生物活性剂。本发明还涉及编码CRACM的重组核酸的用途。本发明的一个方面包括确定候选生物活性剂与CRACM多肽的结合并确定CRACM多肽活性的调节的方法，因为它影响CRAC通道通透性。本发明还涉及调节编码CRACM的核酸的细胞表达的方法和组合物。

8. 发明授权

US08580525B2 Methods of screening for LTRPC7 modulators 有权
标题翻译：筛选LTRPC7调节剂的方法
公开(公告)号：US08580525B2
公开(公告)日：2013-11-12
申请号：US12128471
申请日：2008-05-28
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： G01N33/567 , C12N5/22
CPC分类号： G01N33/6872 , C07K14/705 , G01N2500/04
摘要： The present invention relates to the identification and isolation of a novel family of ATP regulated calcium transmembrane channel polypeptides designated herein as “LTRPC7” (Long Transient Receptor Potential Channel). Channels comprising these polypeptides close in response to concentrations of cytoplasmic ATP in the millimolar range, are subject to inhibition by high intracellular levels of calcium and/or magnesium, and do not respond to depletion or reduction in intracellular calcium stores. The invention further relates to the methods of utilizing LTRPC7 for binding, and the methods for modulating LTRPC7 activity and for measuring LTRPC2 permeability. The invention further relates to the methods of modulating expression of LTRPC7.
摘要翻译：本发明涉及鉴定和分离本文称为“LTRPC7”（长瞬态受体电位通道）的ATP调节的钙跨膜通道多肽的新家族。包含这些多肽的通道在毫微克范围内响应细胞质ATP的浓度而接近的细胞受到钙和/或镁的高细胞内水平的抑制，并且不对细胞内钙储存物的消耗或减少作出反应。本发明还涉及使用LTRPC7进行结合的方法，以及调节LTRPC7活性和测量LTRPC2渗透性的方法。本发明还涉及调节LTRPC7表达的方法。

9. 发明授权

US07960129B2 Assays and methods for determining STIM2 activity 有权
标题翻译：确定STIM2活性的方法和方法
公开(公告)号：US07960129B2
公开(公告)日：2011-06-14
申请号：US12053329
申请日：2008-03-21
申请人： Reinhold Penner , Andrea Fleig
发明人： Reinhold Penner , Andrea Fleig
IPC分类号： G01N33/53 , C12Q1/02
CPC分类号： G01N33/6872 , G01N2500/02 , G01N2800/28
摘要： The present invention provides assays and methods for determining levels of STIM2 activity, thus providing tools for the characterization and study of the regulation of intracellular calcium levels.
摘要翻译：本发明提供了用于确定STIM2活性水平的测定和方法，从而提供用于表征和研究细胞内钙水平的调节的工具。

10. 发明申请

US20050148633A1 Method for modulating calcium ion-release-activated calcium ion channels 审中-公开
标题翻译：钙离子释放活化钙离子通道调节方法
公开(公告)号：US20050148633A1
公开(公告)日：2005-07-07
申请号：US10897682
申请日：2004-07-22
申请人： Yu Xie , Mats Holmqvist , Jerome Mahiou , Mitsunori Ono , Lijun Sun , Shoujun Chen , Shijie Zhang , Jun Jiang , Dinesh Chimmanamada , Andrea Fleig , Chih-Yi Yu
发明人： Yu Xie , Mats Holmqvist , Jerome Mahiou , Mitsunori Ono , Lijun Sun , Shoujun Chen , Shijie Zhang , Jun Jiang , Dinesh Chimmanamada , Andrea Fleig , Chih-Yi Yu
IPC分类号： A61K31/35 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4196 , A61K31/42 , A61K31/4439 , A61K31/444 , A61K31/535 , A61K31/724 , A61P20060101 , A61P27/00 , C07D20060101
CPC分类号： C07C233/66 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/535 , C07C237/42 , C07D213/81 , C07D231/14 , C07D239/28 , C07D263/34 , C07D277/56 , C07D285/06 , C07D333/38 , Y02A50/422
摘要： The invention relates to a method for modulating Ca2+-release-activated Ca2+ channels (CRAC) in a cell by administering to the cell a compound of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein.
摘要翻译：本发明涉及一种通过向细胞施用式（I（I））化合物来调节细胞中的Ca 2+ - 释放激活的Ca 2+ 2 +通道（CRAC）的方法）或其药学上可接受的盐，溶剂化物，包合物或前药，其中X，Y，A，Z，L和n如本文所定义。

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