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公开(公告)号：US6165732A
公开(公告)日：2000-12-26
申请号：US127048
申请日：1998-07-31
IPC分类号： G01N33/50 , A61K38/00 , A61K38/17 , A61K45/00 , A61K48/00 , A61P9/10 , A61P15/00 , A61P17/02 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07K14/47 , C12N5/06 , G01N33/15 , C07K2/00
CPC分类号： C07K14/4747 , A61K38/00
摘要： Methods for identifying apoptosis-modulating compounds using lipid bilayers are provided. One method involves contacting a compound of interest with a lipid bilayer which contains an ion-channel formed by an anti-apoptotic or pro-apoptotic polypeptide of the BCL-2 family and assaying for changes in the ion conductance properties of the channel, including ion selectivity, single channel conductance and rectification. A second method identifies compounds which can form ion channels in planar lipid bilayers and determines the ion selectivity and pH dependence of such channel formation, where apoptosis modulating activity is predicted based on comparing these channel forming characteristics with those of Bcl-2 family members.
摘要翻译： 提供了使用脂质双层鉴定凋亡调节化合物的方法。 一种方法包括使感兴趣的化合物与含有由BCL-2家族的抗凋亡或促凋亡多肽形成的离子通道的脂质双层接触并测定通道的离子电导性质（包括离子）的变化 选择性，单通道电导和整流。 第二种方法鉴定了可以在平面脂双层中形成离子通道的化合物，并确定了这种通道形成的离子选择性和pH依赖性，其中基于将这些通道形成特征与Bcl-2家族成员的这些通道形成特征进行比较来预测凋亡调节活性。
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公开(公告)号：US5821265A
公开(公告)日：1998-10-13
申请号：US872901
申请日：1997-06-11
IPC分类号： A61K31/198 , A61K31/28 , A61L24/02 , A61L27/02 , A61K31/555
CPC分类号： A61L27/025 , A61K31/198 , A61K31/28 , A61L24/02
摘要： The present invention provides a method for blocking a cellular proton pump that comprises contacting a cell with a cellular proton pump-blocking effective quantity of In-EDTA or Tl-EDTA. The present invention also provides a method of treating or preventing cell-mediated disorders in a vertebrate animal by administering In-EDTA or Tl-EDTA to the vertebrate animal, as well as a method for stopping the cellular proton pump-blocking effect of Group IIIa metals such as Ga, In, and Tl, through use of suitable chelating agents. Suitable compositions for use in the aforementioned methods are provided as well.
摘要翻译： 本发明提供了一种阻断细胞质子泵的方法，该方法包括使细胞与细胞质子泵阻断有效量的In-EDTA或T-EDTA接触。 本发明还提供了一种通过向脊椎动物施用In-EDTA或T1-EDTA来治疗或预防脊椎动物中的细胞介导的疾病的方法，以及用于停止IIIa组细胞质子泵阻断作用的方法 金属如Ga，In和Tl，通过使用合适的螯合剂。 也提供了用于上述方法的合适的组合物。
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公开(公告)号：US08617516B2
公开(公告)日：2013-12-31
申请号：US12910385
申请日：2010-10-22
CPC分类号： A61K9/5123 , A61K49/1806
摘要： The present invention provides a substantially non-lytic, non-cytotoxic anchor peptide that is capable of stably inserting into lipid membranes. In particular, the invention provides nanoparticles comprising stably inserted anchor peptides, which may be conjugated to a variety of different cargo complexes.
摘要翻译： 本发明提供了能够稳定地插入脂质膜中的基本上非裂解性的非细胞毒性锚定肽。 特别地，本发明提供包含稳定插入的锚定肽的纳米颗粒，其可以缀合到各种不同的货物配合物。
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公开(公告)号：US20110123438A1
公开(公告)日：2011-05-26
申请号：US12910385
申请日：2010-10-22
CPC分类号： A61K9/5123 , A61K49/1806
摘要： The present invention provides a substantially non-lytic, non-cytotoxic anchor peptide that is capable of stably inserting into lipid membranes. In particular, the invention provides nanoparticles comprising stably inserted anchor peptides, which may be conjugated to a variety of different cargo complexes.
摘要翻译： 本发明提供了能够稳定地插入脂质膜中的基本上非裂解性的非细胞毒性锚定肽。 特别地，本发明提供包含稳定插入的锚定肽的纳米颗粒，其可以缀合到各种不同的货物配合物。
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公开(公告)号：US5763480A
公开(公告)日：1998-06-09
申请号：US196293
申请日：1994-02-14
IPC分类号： A61K31/198 , A61K31/28 , A61L24/02 , A61L27/02
CPC分类号： A61L27/025 , A61K31/198 , A61K31/28 , A61L24/02
摘要： The present invention provides a method for blocking a cellular proton pump that comprises contacting a cell with a cellular proton pump-blocking effective quantity of In-EDTA or Tl-EDTA. The present invention also provides a method of treating or preventing cell-mediated disorders in a vertebrate animal by administering In-EDTA or Tl-EDTA to the vertebrate animal, as well as a method for stopping the cellular proton pump-blocking effect of Group IIIa metals such as Ga, In, and Tl, through use of suitable chelating agents. Suitable compositions for use in the aforementioned methods are provided as well.
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公开(公告)号：US07129208B2
公开(公告)日：2006-10-31
申请号：US10341960
申请日：2003-01-14
CPC分类号： C07K7/06 , A61K9/1272
摘要： The present invention relates to amphiphiles for the formation of a synthetic ion channel in a phospholipid bilayer or biomembrane. The synthetic channel selectively transports chloride ions across the phospholipid bilayer or the membrane. Said amphiphiles impart ion permeability to the phospholipid bilayers or biomembrane and also modulate cellular volume in mammalian cells in vitro.
摘要翻译： 本发明涉及用于在磷脂双层或生物膜中形成合成离子通道的两亲物。 合成通道选择性地将氯离子输送穿过磷脂双层或膜。 所述两亲物赋予磷脂双层或生物膜的离子渗透性，并且还在体外调节哺乳动物细胞中的细胞体积。
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