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Non-mammalian GnRH analogs and uses thereof in the regulation of the immune system

机译:非哺乳动物GnRH类似物及其在调节免疫系统中的用途

摘要

Specially designed non-mammalian GnRH, its analogs, or biometics resistant to degradation by peptidase, are disclosed. The GnRH analogs are further defined as analogs of GnRH II or salmon GnRH. These non-mammalian analogs incorporate D-arginine, D-leucine, D-tBu-Serine, D-Trp or other active D amino acids at position 6 and ethylamide, aza-Gly-amide or other Gly amide at position 10. The D-Arg (6) - GnRH II - ethylamide, D-Arg (6) - GnRH II-aza-Gly (10)-amide, the D-Arg (6) - salmon GnRH ethylamide, and D-Arg (6) - salmon GnRH-aza-Gly (10)-amide analogs are also provided, and demonstrate preferential binding to immune system non-mammalian GnRH receptors. These non-mammalian GnRH or its analogs, or long-acting preparation, biometics or their antibodies may be used in pharmaceutical preparation, and specifically in treatment of various immune system disorders. The non-mammalian GnRH or its analogs are also provided in pharmaceutical preparations that may be used clinically for treating immune system disorders when used in very low doses and administered in pulsatile fashion. The aza-Gly (10) amide non-mammalian analogs are yet other embodiments of the non-mammalian GnRH or its analogs provided as a part of the invention. The use of agents that regulate the production or antibodies or In addition, the detection of non-mammalian GnRH or GnRH II or the non-mammalian GnRH receptors may be used as a diagnostic tool.
机译:公开了专门设计的非哺乳动物GnRH,其类似物或对肽酶降解具有抗性的生物仿制药。 GnRH类似物进一步定义为GnRH II或鲑鱼GnRH的类似物。这些非哺乳动物类似物在位置6引入D-精氨酸,D-亮氨酸,D-tBu-丝氨酸,D-Trp或其他活性D氨基酸,在位置10引入乙酰胺,氮杂-Gly-酰胺或其他Gly酰胺。 -Arg(6)-GnRH II-乙酰胺,D-Arg(6)-GnRH II-氮杂-Gly(10)-酰胺,D-Arg(6)-鲑鱼GnRH乙酰胺和D-Arg(6)-还提供了鲑鱼GnRH-氮杂-Gly(10)-酰胺类似物,并证明了与免疫系统非哺乳动物GnRH受体的优先结合。这些非哺乳动物GnRH或其类似物,或长效制剂,生物仿制药或其抗体可用于药物制剂,特别是用于治疗各种免疫系统疾病。非哺乳动物GnRH或其类似物也以药物制剂的形式提供,当以非常低的剂量使用并以脉动方式给药时,可在临床上用于治疗免疫系统疾病。氮杂-Gly(10)酰胺非哺乳动物类似物是作为本发明一部分提供的非哺乳动物GnRH或其类似物的其他实施方案。使用调节产量的试剂或抗体,或此外,非哺乳动物GnRH或GnRH II或非哺乳动物GnRH受体的检测可以用作诊断工具。

著录项

  • 公开/公告号EP1626055A2

    专利类型

  • 公开/公告日2006-02-15

    原文格式PDF

  • 申请/专利权人 SILER-KHODR THERESA M.;

    申请/专利号EP20050017405

  • 发明设计人 SILER-KHODR THERESA M.;

    申请日2005-08-10

  • 分类号C07K7/06;C07K7/23;A61K38/09;C07K16/26;C12N15/00;

  • 国家 EP

  • 入库时间 2022-08-21 21:28:56

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