Angiopeptin

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Angiopeptin
• 英文别名: (2S)-6-amino-N-[(2S)-1-[[(2R)-1-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanamide
• 化学式: C₅₄H₇₁N₁₁O₁₀S₂
• 分子量: 1098.3
• InChiKey: UGVPPRZHXAMSJP-SCTWWAJVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  77
• 可旋转键数：
  29
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  357
• 氢给体数：
  15
• 氢受体数：
  14

文献信息

• A drug for the treatment of cancer
  申请人：National Institute of Immunology

  公开号：EP0835662A2

  公开（公告）日：1998-04-15

  A pharmaceutical composition useful for killing or inhibiting multiplication of cancer cells. It is expected that the pharmaceutical composition will be useful in preventing, inhibiting, or modulating the hypersecretion of VIP, somatostatin, bombesin, Substance P, or a combination of VIP, somatostatin, bombesin, or Substance P. The composition may suitably comprise, consist of, or consist essentially of a therapeutically effective combination of peptide analogs of somatostatin, VIP, bombesin, and Substance P. Also provided is a method of treatment for humans or other animals suffering from cancer, the method comprising administering a therapeutically effective dose of the pharmaceutical composition so as to kill or inhibit the multiplication of cancer cells. The method of treatment may be particularly useful in the treatment of cancers of the colon and rectum. Also provided is a method of treatment for humans or animals having hypersecretion or modulation of VIP, somatostatin, bombesin, Substance P, or a combination of VIP, somatostatin, bombesin, or Substance P.

  一种用于杀死或抑制癌细胞繁殖的药物组合物。预计该药物组合物将有助于预防、抑制或调节 VIP、somatostatin、bombesin、Substance P 或 VIP、somatostatin、bombesin 或 Substance P 的组合物的高分泌。该组合物可适当地包括、由或主要由治疗有效的 somatostatin、VIP、bombesin 和 Substance P 肽类似物组合组成。还提供了一种治疗人类或其他动物癌症的方法，该方法包括施用治疗有效剂量的药物组合物，以杀死或抑制癌细胞的繁殖。该治疗方法尤其适用于结肠癌和直肠癌的治疗。还提供了一种治疗方法，适用于VIP、体生长抑素、蚕豆素、物质P或VIP、体生长抑素、蚕豆素或物质P组合分泌过多或调节过多的人类或动物。
• Neuropeptide receptor and uses thereof
  申请人：Pfizer Limited

  公开号：EP1340979A2

  公开（公告）日：2003-09-03

  This invention relates to the identification of an orphan G-protein coupled receptor MRGX2 (and variants thereof) as a receptor of neuropeptides such as but not limited to cortistatin, somatostatin, Bam 13-22, α-MSH, neuropeptide FF, dynorphin A and substance P, and the use of such neuropeptides (and structurally related molecules) as modulators for MRGX2. It also relates to screening methods to identify agonists and antagonists for this neuropeptide receptor.

  本发明涉及一种孤儿 G 蛋白偶联受体 MRGX2（及其变体）作为神经肽受体的鉴定，这些神经肽包括但不限于可体司他汀、体生长抑素、Bam 13-22、α-MSH、神经肽 FF、达诺啡 A 和 P 物质，以及使用这些神经肽（和结构相关的分子）作为 MRGX2 的调节剂。它还涉及鉴定这种神经肽受体的激动剂和拮抗剂的筛选方法。
• [EN] PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF SYNDROME X OF REAVEN<br/>[FR] COMPOSITION PHARMACEUTIQUE POUR LE TRAITEMENT DU SYNDROME X DE REAVEN
  申请人：——

  公开号：WO1998010786A2

  公开（公告）日：1998-03-19

  [EN] The present invention relates to a pharmaceutical composition comprising as active ingredient a compound selected among somatostatin or one of its analogs, diazoxide or one of its analogs, cyclothiazide or one of its analogs and metformin, for the treatment of syndrome X of Reaven (also called "Hyper Insulinemia syndrome" or "The Deadly Quartet").
  [FR] L'invention concerne une composition pharmaceutique comprenant, en tant que principe actif, un composé choisi parmi la somatostatine ou un de ses analogues, le diazoxyde ou un de ses analogues, le cyclothiazidéor ou un de ses analogues et la metformine, pour le traitement du syndrome X de Raeven (également appelé syndrome d'hyperinsulinémie ou "quartet meurtrier").