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    • 1. 发明授权
    • Peralkylated oligopeptide mixtures
    • 过烷基化寡肽混合物
    • US5480971A
    • 1996-01-02
    • US257782
    • 1994-06-09
    • Richard A. HoughtenJohn M. OstreshSylvie Blondelle
    • Richard A. HoughtenJohn M. OstreshSylvie Blondelle
    • C07K1/04C07K1/12C12Q1/18C07K7/06A61K38/00
    • C07K1/04C07K1/12C12Q1/18
    • Linear C.sub.1 -C.sub.7 -alkyl peralkylated oligopeptide sets of molecules are specific peralkylated oligopeptides, disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a set contains the same number of two to about ten substituted C.sub.1 -C.sub.7 -alkyl peralkylated amino acid residues, and the member chains of a set are present in equimolar amounts. The chains of a set contain one or more predetermined peralkylated amino acid residues at one or more predetermined positions of the peralkylated oligopeptide chain. The set contains equimolar amounts of at least six different peralkylated amino acid residues at one or more of the same predetermined positions of the peralkylated oligopeptide chain. Libraries of such sets, processes for their use and solid support-linked peralkylated sets are also contemplated, as are specific permethylated oligopeptides such as those having 5-8 phenylalanine residues that have antimicrobial properties.
    • 线性C 1 -C 7烷基全烷基化寡肽组分子是特异性全烷基化寡肽,其公开在合成和在受体结合测定中使用的方法。 一组的每个分子或链含有相同数量的两个至约十个取代的C 1 -C 7烷基全烷基化氨基酸残基,并且一组的成员链以等摩尔量存在。 一组的链在全烷基化寡肽链的一个或多个预定位置含有一个或多个预定的全烷基化氨基酸残基。 该组在全烷基化寡肽链的一个或多个相同的预定位置含有等摩尔量的至少六个不同的烷基化氨基酸残基。 还考虑了这些组的文库,其使用方法和固体支持物连接的全烷基化组,特定的二甲基化寡肽如具有5-8个具有抗微生物性质的苯丙氨酸残基的寡肽。
    • 5. 发明授权
    • Amphiphilic peptide compositions and analogues thereof
    • 两亲肽组合物及其类似物
    • US5294605A
    • 1994-03-15
    • US725331
    • 1991-07-08
    • Richard A. HoughtenSylvie Blondelle
    • Richard A. HoughtenSylvie Blondelle
    • A61K38/00C07K7/08C07K14/46A61K37/02C07K7/10
    • C07K14/46C07K7/08A61K38/00
    • A process for inhibiting growth of a target cell comprising administering to a host or to a target cell or virus a biologically active peptide which includes one of the following basic structures; R.sub.1 -R.sub.1 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.2 -R.sub.2 ; R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.1 ; or R.sub.1 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1 -R.sub.1 -R.sub.2 -R.sub.2 -R.sub.1, wherein R.sub.1 is a hydrophobic amino acid, and R.sub.2 is a basic hydrophilic or neutral hydrophilic amino acid. A preferred peptide is of the structural formula:(SEQ ID NO:3).Substitution and deletion analogues of this peptide can be prepared that have increased biological activity. Such peptides can be employed as pharmaceuticals.
    • 一种抑制靶细胞生长的方法,包括向宿主或靶细胞或病毒施用包括以下基本结构之一的生物活性肽; R1-R1-R2-R1-R1-R2-R2-R1-R1-R2-R2-R1-R2-R2; R2-R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R2-R1-R1; 或R1-R2-R1-R1-R2-R2-R1-R1-R2-R2-R1-R2-R2-R1-R1-R2-R2-R1,其中R1是疏水性氨基酸,R2是碱性 亲水或中性亲水氨基酸。 优选的肽具有以下结构式:(SEQ ID NO:3)。 可以制备具有增加的生物活性的该肽的取代和缺失类似物。 这样的肽可以用作药物。
    • 7. 发明授权
    • Peralkylated oligopeptide mixtures
    • 过烷基化寡肽混合物
    • US5763193A
    • 1998-06-09
    • US577846
    • 1995-12-22
    • Richard A. HoughtenJohn M. OstreshSylvie Blondelle
    • Richard A. HoughtenJohn M. OstreshSylvie Blondelle
    • C07K1/04C07K1/12C12Q1/18G01N33/53
    • C07K1/04C07K1/12C12Q1/18
    • Linear C.sub.1 -C.sub.7 -alkyl peralkylated oligopeptide sets of molecules are disclosed, as are their methods of synthesis and use in acceptor binding assays. Each molecule or chain of a set contains the same number of two to about ten substituted C.sub.1 -C.sub.7 -alkyl peralkylated amino acid residues, and the member chains of a set are present in equimolar amounts. The chains of a set contain one or more predetermined peralkylated amino acid residues at one or more predetermined positions of the peralkylated oligopeptide chain. The set contains equimolar amounts of at least six different peralkylated amino acid residues at one or more of the same predetermined positions of the peralkylated oligopeptide chain. Libraries of such sets, processes for their use and solid support-linked peralkylated sets are also contemplated, as are specific permethylated oligopeptides.
    • 公开了线性C 1 -C 7烷基全烷基化寡肽组分子,以及其在受体结合测定中的合成和使用方法。 一组的每个分子或链含有相同数量的两个至约十个取代的C 1 -C 7烷基全烷基化氨基酸残基,并且一组的成员链以等摩尔量存在。 一组的链在全烷基化寡肽链的一个或多个预定位置含有一个或多个预定的全烷基化氨基酸残基。 该组在全烷基化寡肽链的一个或多个相同的预定位置含有等摩尔量的至少六个不同的烷基化氨基酸残基。 这些组的文库,它们的使用方法和固体支持物连接的烷基化组也被考虑,特定的甲基化寡肽也是如此。