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    Maurotoxin, PI1 and HSTX1 derivatives
    2.
    发明申请
    Maurotoxin, PI1 and HSTX1 derivatives 有权
    毛毒素，PI1和HSTX1衍生物

    公开(公告)号：US20090062198A1

    公开(公告)日：2009-03-05

    申请号：US12009675

    申请日：2008-01-22

    申请人： Jean-Marc Sabatier ,  Kamel Mabrouk ,  Herve Rochat

    发明人： Jean-Marc Sabatier ,  Kamel Mabrouk ,  Herve Rochat

    IPC分类号： A61K38/17 ,  C07K14/435 ,  C12N5/06 ,  A61P25/28 ,  A61P37/00

    CPC分类号： C07K14/43522 ,  A61K38/00

    摘要： Derivatives of Maurotoxin (MTX) in which the native disulfide bridge pattern (Cys3-Cys24, Cys9-Cys29, Cys19, Cys31-Cys34) has been disrupted are useful for the treatment of pathologies associated with dysfunctioning and/or activation of Ca2+-activated and/or voltage-gated K+ channel subtypes, such as IKCa1 or Kv1.2. One preferred group of derivatives is that in which one or more of the Cys residues have been replaced with α-aminobutyrate (Abu) residues, thus breaking one or more of the four disulphide bridges. Within this group, the preferred derivative is that in which the Cys residues at position 9, 19, 29 and 34 have been replaced with a α-aminobutyrate residues. However, the derivative in which the Cys residues at positions 19 and 34 have been replaced with (Abu) residues is excluded Another preferred group of derivatives is that in which one or two of the amino acid residues of maurotoxin have been replaced by different amino acid residues resulting in the disulfide bridge pattern being changed to Cys3-Cys24, Cys9-Cys29, Cys13-Cys31, Cys19-Cys34. Within this group, the preferred compounds are that which the Arg residue at position 14 has been replaced by a Gln residue, that in which the Lys residue at position 15 has been replaced by a Gln residue, that in which the Arg residue at position 14 and Lys residue at position 15 have both been replaced by Gin residues, those in which neither of the residues at positions 32 and 33 is a Gly or Pro residue, and that in which the Gly residue at position 33 has been replaced by an Ala residue. Pi1 and HsTx1 derivatives with disrupted native disulfide bridge patterns are similarly useful.

    摘要翻译： 其中天然二硫桥型（Cys3-Cys24，Cys9-Cys29，Cys19，Cys31-Cys34）被破坏的Maurotoxin（MTX）的衍生物可用于治疗与功能障碍和/或激活Ca 2+激活相关的病理学 /或电压门控K +通道亚型，如IKCa1或Kv1.2。 一组优选的衍生物是其中一个或多个Cys残基被α-氨基丁酸（Abu）残基替代，从而破坏了四个二硫键中的一个或多个。 在该组内，优选的衍生物是其中9,19,29和34位的Cys残基被α-氨基丁酸残基替代。 然而，其中位于第19和34位的Cys残基已经被（Abu）残基所取代的衍生物被排除。另外一组优选的衍生物是其中一个或两个母体毒素的氨基酸残基被不同的氨基酸替代 导致二硫键图案的残基变为Cys3-Cys24，Cys9-Cys29，Cys13-Cys31，Cys19-Cys34。 在该组中，优选的化合物是第14位的Arg残基被Gln残基取代，其中第15位的Lys残基被Gln残基替代，其中第14位的Arg残基 和位置15处的Lys残基都被Gin残基取代，其中32位和33位的残基都不是Gly或Pro残基，其中第33位的Gly残基被Ala残基所取代 。 具有破坏的天然二硫键图案的Pi1和HsTx1衍生物同样有用。

    Multiple branch peptide construction
    3.
    发明授权
    Multiple branch peptide construction 失效
    多分支肽结构

    公开(公告)号：US06379679B1

    公开(公告)日：2002-04-30

    申请号：US09342847

    申请日：1999-06-29

    申请人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    发明人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    IPC分类号： A61K4500

    CPC分类号： C07K14/005 ,  A61K38/00 ,  C12N2740/16122

    摘要： Multiple branch peptide constructions formed from peptides derived from the envelope transmembrane glycoprotein gp41 of HIV, and including the consensus sequence RQGY preceded by 0 to 4 amino acid residues and succeeded by 2 to 4 amino acid residues, most preferably RQGYSPL, show increased receptor affinity and prevent cell-to-cell fusion. They have a direct virostatic effect. Because they present the same peptide sequence several times, these MBPCs are able to neutralize in vitro the different steps of virus envelope/cell membrane fusion, and infected cell membrane/uninfected cell membrane fusion of several strains of HIV-1 and HIV-2. These results open a potential use in treatment of HIV infection.

    摘要翻译： 由衍生自HIV的包膜跨膜糖蛋白gp41的肽形成的多分支肽结构，并且包括在0至4个氨基酸残基之前的共有序列RQGY，并且继续存在2至4个氨基酸残基，最优选RQGYSPL，表现出增加的受体亲和力 防止细胞间细胞融合。 它们具有直接的静电作用。 由于它们呈现相同的肽序列多次，所以这些MBPC能够在体外中和病毒包膜/细胞膜融合的不同步骤，以及几种HIV-1和HIV-2菌株的感染细胞膜/未感染的细胞膜融合。 这些结果揭示了治疗艾滋病毒感染的潜在用途。

    Multiple branch peptide construction
    4.
    发明授权
    Multiple branch peptide construction 失效
    多分支肽结构

    公开(公告)号：US07285621B2

    公开(公告)日：2007-10-23

    申请号：US10126915

    申请日：2002-04-19

    申请人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    发明人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    IPC分类号： A61K38/04 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K14/005 ,  A61K9/127 ,  A61K38/162 ,  C12N2740/16122

    摘要： Multiple branch peptide constructions formed from peptide-branches derived from the envelope transmembrane glycoprotein gp41 of HIV, and including the consensus sequence RQGY preceded by 0 to 4 amino acid residues and succeeded by 0 to 4 amino acid residues, most preferably RQGYS, show increased receptor affinity and prevent cell-to-cell fusion. They have a direct virostatic effect. Because they present the same peptide sequence several times, these MBPCs are able to neutralize in vitro the different steps of virus envelope/cell membrane fusion, and infected cell membrane/uninfected cell membrane fusion of several strains of HIV-1 and HIV-2. These results open a potential use in treatment of HIV infection.

    摘要翻译： 由衍生自HIV的包膜跨膜糖蛋白gp41的肽分支形成的多个分支肽结构，并且包括在0至4个氨基酸残基之前的共有序列RQGY，并且随后的0至4个氨基酸残基，最优选RQGYS显示增加的受体 亲和力并防止细胞间细胞融合。 它们具有直接的静电作用。 由于它们呈现相同的肽序列多次，所以这些MBPC能够在体外中和病毒包膜/细胞膜融合的不同步骤，以及几种HIV-1和HIV-2菌株的感染细胞膜/未感染的细胞膜融合。 这些结果揭示了治疗艾滋病毒感染的潜在用途。

    Maurotoxin, PI1 and HSTX1 derivatives
    5.
    发明授权
    Maurotoxin, PI1 and HSTX1 derivatives 有权
    毛毒素，PI1和HSTX1衍生物

    公开(公告)号：US07829666B2

    公开(公告)日：2010-11-09

    申请号：US12009675

    申请日：2008-01-22

    申请人： Jean-Marc Sabatier ,  Kamel Mabrouk ,  Herve Rochat

    发明人： Jean-Marc Sabatier ,  Kamel Mabrouk ,  Herve Rochat

    IPC分类号： A61K38/12

    CPC分类号： C07K14/43522 ,  A61K38/00

    摘要： Derivatives of Maurotoxin (MTX) in which the native disulfide bridge pattern (Cys3-Cys24, Cys9-Cys29, Cys19, Cys31-Cys34) has been disrupted are useful for the treatment of pathologies associated with dysfunctioning and/or activation of Ca2+-activated and/or voltage-gated K+ channel subtypes, such as IKCa1 or Kv1.2. In one group of derivatives, one or two of the amino acid residues of maurotoxin have been replaced by different amino acid residues resulting in the disulfide bridge pattern being changed to Cys3-Cys24, Cys9-Cys29, Cys13-Cys31, Cys19-Cys34. Exemplary substitutions include the Arg residue at position 14 and/or the Lys residue at position 15 replaced by a Gln residue and the Gly residue at position 33 replaced by an Ala residue. Pi1 and HsTx1 derivatives with disrupted native disulfide bridge patterns are similarly useful.

    摘要翻译： 其中天然二硫桥型（Cys3-Cys24，Cys9-Cys29，Cys19，Cys31-Cys34）被破坏的Maurotoxin（MTX）的衍生物可用于治疗与功能障碍和/或激活Ca 2+激活相关的病理学 /或电压门控K +通道亚型，如IKCa1或Kv1.2。 在一组衍生物中，一个或两个母体毒素的氨基酸残基被不同的氨基酸残基取代，导致二硫键形式改变为Cys3-Cys24，Cys9-Cys29，Cys13-Cys31，Cys19-Cys34。 示例性的取代包括位置14处的Arg残基和/或在位置15处的Lys残基被Gln残基取代，而33位的Gly残基被Ala残基取代。 具有破坏的天然二硫键图案的Pi1和HsTx1衍生物同样有用。

    Multiple branch peptide construction
    6.
    发明申请
    Multiple branch peptide construction 失效
    多分支肽结构

    公开(公告)号：US20060155108A1

    公开(公告)日：2006-07-13

    申请号：US10126915

    申请日：2002-04-19

    申请人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    发明人： Kamel Mabrouk ,  Jean-Marc Sabatier ,  Herve Rochat ,  Jurphaas Van Rietschoten

    IPC分类号： C07K14/47

    CPC分类号： C07K14/005 ,  A61K9/127 ,  A61K38/162 ,  C12N2740/16122

    摘要： Multiple branch peptide constructions formed from peptide-branches derived from the envelope transmembrane glycoprotein gp41 of HIV, and including the consensus sequence RQGY preceded by 0 to 4 amino acid residues and succeeded by 0 to 4 amino acid residues, most preferably RQGYS, show increased receptor affinity and prevent cell-to-cell fusion. They have a direct virostatic effect. Because they present the same peptide sequence several times, these MBPCs are able to neutralize in vitro the different steps of virus envelope/cell membrane fusion, and infected cell membrane/uninfected cell membrane fusion of several strains of HIV-1 and HIV-2. These results open a potential use in treatment of HIV infection.

    摘要翻译： 由衍生自HIV的包膜跨膜糖蛋白gp41的肽分支形成的多个分支肽结构，并且包括在0至4个氨基酸残基之前的共有序列RQGY，并且随后的0至4个氨基酸残基，最优选RQGYS显示增加的受体 亲和力并防止细胞间细胞融合。 它们具有直接的静电作用。 由于它们呈现相同的肽序列多次，所以这些MBPC能够在体外中和病毒包膜/细胞膜融合的不同步骤，以及几种HIV-1和HIV-2菌株的感染细胞膜/未感染的细胞膜融合。 这些结果揭示了治疗艾滋病毒感染的潜在用途。