利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

9 条记录 (耗时 0.032 秒)

    Heparin- and sulfatide binding peptides from the type I repeats of human thrombospondin and conjugates thereof
    7.
    发明授权
    Heparin- and sulfatide binding peptides from the type I repeats of human thrombospondin and conjugates thereof 失效
    来自人类血小板反应素的I型重复序列的肝素和硫酸肽结合肽及其缀合物

    公开(公告)号：US5770563A

    公开(公告)日：1998-06-23

    申请号：US487568

    申请日：1995-06-07

    申请人： David D. Roberts ,  Philip J. Browning ,  Joseph L. Bryant ,  John K. Inman ,  Henry C. Krutzsch ,  Nenghua Guo

    发明人： David D. Roberts ,  Philip J. Browning ,  Joseph L. Bryant ,  John K. Inman ,  Henry C. Krutzsch ,  Nenghua Guo

    IPC分类号： A61K38/00 ,  C07K7/00 ,  C07K14/78 ,  C07K17/10 ,  A61K38/04 ,  C07K5/00

    CPC分类号： C07K17/10 ,  C07K14/78 ,  A61K38/00 ,  C12N2533/50 ,  Y10S514/908

    摘要： This invention identifies a biologically active group of peptide sequences from Type I repeat units of the extracellular matrix protein, human thrombospondin-1, identical or homologous to the sequence, KRFKQDGGWSHWSPWSSC (SEQ ID NO:30). The biological activities residing with the full sequences, portions thereof, and variants of the full or partial sequences are disclosed. The invention describes how biological activity may be enhanced by covalently linking these peptides to suitable carriers, preferably a branched, water-soluble polymer of low (or absent) toxicity and immunogenicity, such as polysucrose (Ficoll.TM.). The invention describes (1) a method for preparing such conjugates, (2) the use of the defined peptides or their conjugates in blocking or modifying the action on cellular processes of heparin (e.g., proliferation, adhesion, motility, extravasation and neovascularization), sulfatides, related sulfated glycoconjugates, fibronectin, and basic fibroblast growth factor, involving malignant cell lines and normal endothelial cells. Use of the defined peptides, analogs or peptidomimetics and their conjugates for treatment of metastatic tumors, breast carcinomas, melanomas, Kaposi's sarcomas, hemangiomas, diabetic retinopathies, and various pathological conditions dependent upon neovascularization is also disclosed.

    摘要翻译： 本发明鉴定了与序列KRFKQDGGWSHWSPWSSC（SEQ ID NO：30）相同或同源的细胞外基质蛋白I型重复单元的人类血小板反应蛋白-1的生物活性肽序列。 公开了其完整序列，部分和全部或部分序列的变体的生物活性。 本发明描述如何通过将这些肽共价连接到合适的载体，优选具有低（或不存在）毒性和免疫原性的支链水溶性聚合物如聚蔗糖（Ficoll TM）来增强生物活性。 本发明描述了（1）制备这种缀合物的方法，（2）使用所定义的肽或其缀合物来阻断或改变对肝素细胞过程的作用（例如增殖，粘附，运动，外渗和新生血管形成） 硫酸盐，相关的硫酸化糖缀合物，纤连蛋白和碱性成纤维细胞生长因子，涉及恶性细胞系和正常内皮细胞。 还公开了定义的肽，类似物或肽模拟物及其缀合物用于治疗转移性肿瘤，乳腺癌，黑素瘤，卡波西氏肉瘤，血管瘤，糖尿病视网膜病变以及依赖于新血管形成的各种病理状况的用途。

    Amino acid derivative and bromoacetyl modified peptides for the preparation of synthetic peptide polymers, conjugated peptides, and cyclic peptides
    8.
    发明授权
    Amino acid derivative and bromoacetyl modified peptides for the preparation of synthetic peptide polymers, conjugated peptides, and cyclic peptides 失效
    用于制备合成肽聚合物，缀合肽和环肽的氨基酸衍生物和溴乙酰基修饰的肽

    公开(公告)号：US5286846A

    公开(公告)日：1994-02-15

    申请号：US715650

    申请日：1991-06-14

    申请人： John K. Inman ,  Frank A. Robey

    发明人： John K. Inman ,  Frank A. Robey

    IPC分类号： A61K47/48 ,  C07C271/22 ,  C07K1/00 ,  C07K1/04 ,  C07K1/107 ,  A61K37/02 ,  C08G63/48

    CPC分类号： A61K47/48238 ,  C07C271/22 ,  C07K1/006 ,  C07K1/04 ,  C07K1/1077

    摘要： A new amino derivative, N.sup..alpha. -tert-butoxycarbonyl-N.sup..epsilon. -(N-bromoacetyl-.beta.-alanyl)-L-lysine (BBAL), has been synthesized as a reagent to be used in solid-phase peptide synthesis for introducing a side-chain bromoacetyl group at any desired position in a peptide sequence. The bromoacetyl group subsequently serves as a sulfhydryl-selective cross-linking function for the preparation of cyclic peptides, peptide conjugates and polymers. BBAL residues are stable to final HF deprotection/cleavage. BBAL peptides can be directly coupled to other molecules or surfaces which possess free sulfhydryl groups by forming stable thioether linkages. Peptides containing both BBAL and cysteine residues can be self-coupled to produce either cyclic molecules or linear peptide polymers. Such peptide derivatives are useful in preparing potential peptide immunogens, vaccines and therapeutics, and for substances such as peptides linked to polymers, plastics, enamels and ceramics.

    摘要翻译： 已经合成了一种新的氨基酸衍生物，N - 叔丁氧羰基-Nε-（N-溴乙酰基-β-丙氨酰基）-L-赖氨酸（BBAL）作为固相中的试剂 用于在肽序列中的任何所需位置引入侧链溴乙酰基的肽合成。 随后溴乙酰基用作制备环肽，肽缀合物和聚合物的巯基选择性交联功能。 BBAL残基对最终的HF去保护/切割是稳定的。 BBAL肽可以通过形成稳定的硫醚键直接偶联到具有游离巯基的其它分子或表面。 含有BBAL和半胱氨酸残基的肽可以是自偶联的，以产生环状分子或线性肽聚合物。 这样的肽衍生物可用于制备潜在的肽免疫原，疫苗和治疗剂，以及用于物质如与聚合物，塑料，搪瓷和陶瓷连接的肽。

    Amino acid derivative and bromoacetyl modified peptides for the preparation of synthetic peptide polymers, conjugated peptides, and cyclic peptides
    9.
    发明授权
    Amino acid derivative and bromoacetyl modified peptides for the preparation of synthetic peptide polymers, conjugated peptides, and cyclic peptides 失效
    用于制备合成肽聚合物，缀合肽和环肽的氨基酸衍生物和溴乙酰基修饰的肽

    公开(公告)号：US5444150A

    公开(公告)日：1995-08-22

    申请号：US154786

    申请日：1993-11-19

    申请人： John K. Inman ,  Frank A. Robey

    发明人： John K. Inman ,  Frank A. Robey

    IPC分类号： A61K47/48 ,  C07C271/22 ,  C07K1/00 ,  C07K1/04 ,  C07K1/107 ,  A61K38/00 ,  C08G63/48

    CPC分类号： A61K47/48238 ,  C07C271/22 ,  C07K1/006 ,  C07K1/04 ,  C07K1/1077

    摘要： A new amino acid derivative, N.sup..alpha. -tert-butoxycarbonyl-N.sup.e -(N-bromoacetyl-.beta.-alanyl)-L-lysine (BBAL), has been synthesized as a reagent to be used in solid-phase peptide synthesis for introducing a side-chain bromoacetyl group at any desired position in a peptide sequence. The bromoacetyl group subsequently serves as a sulfhydryl-selective cross-linking function for the preparation of cyclic peptides, peptide conjugates and polymers. BBAL residues are stable to final HF deprotection/cleavage. BBAL peptides can be directly coupled to other molecules or surfaces which possess free sulfhydryl groups by forming stable thioether linkages. Peptides containing both BBAL and cysteine residues can be self-coupled to produce either cyclic molecules or linear peptide polymers. Such peptide derivatives are useful in preparing potential peptide immunogens, vaccines and therapeutics, and for substances such as peptides linked to polymers, plastics, enamels and ceramics.

    摘要翻译： 已经合成了新的氨基酸衍生物，Nα-叔丁氧基羰基-Ne-（N-溴乙酰基-β-丙氨酰基）-L-赖氨酸（BBAL）作为用于固相肽合成的试剂，用于引入 侧链溴乙酰基在肽序列中的任何所需位置。 随后溴乙酰基用作制备环肽，肽缀合物和聚合物的巯基选择性交联功能。 BBAL残基对最终的HF去保护/切割是稳定的。 BBAL肽可以通过形成稳定的硫醚键直接偶联到具有游离巯基的其它分子或表面。 含有BBAL和半胱氨酸残基的肽可以是自偶联的，以产生环状分子或线性肽聚合物。 这样的肽衍生物可用于制备潜在的肽免疫原，疫苗和治疗剂，以及用于诸如与聚合物，塑料，搪瓷和陶瓷连接的肽的物质。