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    • 6. 发明授权
    • Molecular probe for imaging of pancreatic islets and use of the same
    • 胰岛成像用分子探针及其用途
    • US08642008B2
    • 2014-02-04
    • US12872837
    • 2010-08-31
    • Nobuya InagakiHideo SajiKentaro ToyodaHiroyuki KimuraYu OgawaKonomu HiraoKenji NagakawaHirokazu Matsuda
    • Nobuya InagakiHideo SajiKentaro ToyodaHiroyuki KimuraYu OgawaKonomu HiraoKenji NagakawaHirokazu Matsuda
    • A61K51/08
    • A61K51/088
    • To provide a molecular probe for imaging of pancreatic islets. A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe includes any one of the following polypeptides: polypeptides represented by the following formulae (1), (5), and (9); and polypeptides having homology with the foregoing polypeptides: Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (5) B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (9) where X in the formulae (1) and (5) and B- in the formula (9) indicate that an amino group is labeled with a group represented by the formula (I) below having an aromatic ring, wherein A represents either an aromatic hydrocarbon group or an aromatic heterocyclic group, R1 represents a substituent that contains radioactive iodine, R2 represents either a hydrogen atom or a substituent different from that represented by R1, and R3 represents any one of a bond, a methylene group, and an oxymethylene group.
    • 为胰岛成像提供分子探针。 提供了一种用于胰岛成像的分子探针。 分子探针包括以下多肽之一:由下式(1),(5)和(9)表示的多肽。 和与前述多肽具有同源性的多肽:Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2(1)Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2(5)B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2(9)其中式(1)和(5)中的X和 式(9)表示氨基用具有芳环的下式(I)表示的基团标记,其中A表示芳香族烃基或芳香族杂环基,R 1表示含有放射性碘的取代基, R2表示氢原子或与R1表示的不同的取代基,R3表示键,亚甲基和氧亚甲基中的任一个。
    • 10. 发明授权
    • Molecular probe for imaging of pancreatic islets and use of the same
    • 胰岛成像用分子探针及其用途
    • US08980220B2
    • 2015-03-17
    • US12964486
    • 2010-12-09
    • Hideo SajiNobuya InagakiKentaro ToyodaHiroyuki KimuraKonomu HiraoKenji NagakawaHirokazu Matsuda
    • Hideo SajiNobuya InagakiKentaro ToyodaHiroyuki KimuraKonomu HiraoKenji NagakawaHirokazu Matsuda
    • C07K14/605G01N33/74A61K51/08
    • G01N33/74A61K51/088C07K14/605
    • A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide, (SEQ ID NO. 1) Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) (SEQ ID NO. 2) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (2) (SEQ ID NO. 3) B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (3) where, in the formulae (1) and (2), “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a radioactive nuclide, and “Z—” indicates that an α-amino group at an N-terminus is not modified, or is modified with a modifying group having no electric charge; in the formula (3), “B—” indicates that an α-amino group at an N-terminus is labeled with a radioactive nuclide; and in the formulae (1), (2), and (3), “—NH2” indicates that a carboxyl group at a C-terminus is amidated.
    • 提供了一种用于胰岛成像的分子探针。 分子探针包含由下式(1),(2)或(3)表示的多肽,或与前述多肽具有同源性的多肽(SEQ ID NO.1)Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2(1)( SEQ ID NO.2)Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2(2)(SEQ ID NO.3)B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2(3)其中,在式(1)和(2)中,“X”表示赖氨酸残基, 赖氨酸残基的侧链的氨基被放射性核素标记,“Z-”表示N末端的α-氨基未被修饰,或者是用不具有电荷的修饰基团修饰 ; 在式(3)中,“B-”表示N末端的α-氨基用放射性核素标记; 在式(1),(2)和(3)中,“-NH 2”表示C末端的羧基被酰胺化。