COMPOUND

• Main Authors: ROB FALCONER, LAURENCE PATTERSON, JENNIFER ATKINSON, JASON GILL, MIKE BIBBY, LOADMAN PAUL
• Format: Patent
• Language: English; Japanese
• Published: 16.10.2014
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide a compound activated in vivo to a compound relatively having biological activity from a compound relatively having no biological activity, a so-called "prodrug", and a target therapy of cancer using the compound.SOLUTION: A peptide comprises an amino acid sequence -Arg-Ser-Cit-Gly-Hof-Tyr-Leu-, and has, at N-terminal or C-terminal of the peptide, a capping group c selected from fluorescein, a fluorescein derivative, monosaccharide, D-amino acid or proline imino acid. A compound binds to the peptide and has biological activity. A prodrug comprises an anti-cancer agent or a vascular disrupting agent. 【課題】相対的に生物活性をもたない化合物、いわゆる「プロドラッグ」から相対的に生物活性をもつ化合物に生体内で活性化される化合物及び前記化合物を使用する癌の標的治療方法の提供。【解決手段】アミノ酸配列−Ａｒｇ−Ｓｅｒ−Ｃｉｔ−Ｇｌｙ−Ｈｏｆ−Ｔｙｒ−Ｌｅｕ−を含み、かつペプチドのＮ末端またはＣ末端にキャップ形成基ｃ、フルオレセイン、フルオレセイン誘導体、単糖、Ｄ−アミノ酸、又はプロリンイミノ酸から選択、を有するペプチド及び前記ペプチドと結合している、生物活性をもつ化合物、抗癌剤又は血管破壊剤、を含むプロドラッグ。【選択図】なし