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    • 3. 发明公开
    • MOLECULAR PROBE PRECURSOR FOR IMAGING OF PANCREATIC ISLET, AND USE THEREOF
    • 麦克卢瑟尔SONDENVORLÄUFERZUR BILDGEBUNG DER LANGERHANS-INSELN UND VERFAHRENDAFÜR
    • EP2335739A1
    • 2011-06-22
    • EP09814677.2
    • 2009-09-18
    • Kyoto UniversityARKRAY, Inc.
    • INAGAKI, NobuyaSAJI, HideoTOYODA, KentaroKIMURA, HiroyukiHIRAO, KonomuNAGAKAWA, Kenji
    • A61K49/00C07K14/00
    • A precursor of a molecular probe for imaging of pancreatic islets is provided. The precursor includes a polypeptide represented by any one of the following formulae (1) to (12), or a polypeptide having a homology with the foregoing polypeptide:
      *-DLSKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (1)
      *-LSKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (2)
      *-SKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (3)
      *-KQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (4)
      *-DLSK* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (5)
      *-LSW QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (6)
      *-SK* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (7)
      *-K* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (8)
      DLSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (9)
      LSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (10)
      SK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (11)
      K* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH 2 (12)
    • 提供了用于胰岛成像的分子探针的前体。 前体包括由下式(1)至(12)中的任一个表示的多肽或与前述多肽具有同源性的多肽:* -DLSKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(1)* -LSKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(2)* -SKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(3)* -KQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(4)* -DLSK * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2(5)* -LSW QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2(6)* -SK * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2(7)* -K * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2(8)DLSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(9)LSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(10)SK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2 11)K * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH 2(12)
    • 7. 发明公开
    • MOLECULAR PROBE FOR IMAGING ISLETS OF LANGERHANS, AND USE THEREFORE
    • MOLEKULARE SONDE ZUR BILDGEBUNG DER LANGERHANS-INSELN UND IHRE VERWENDUNG
    • EP2474326A1
    • 2012-07-11
    • EP10813687.0
    • 2010-08-31
    • Kyoto UniversityArkray, Inc.
    • INAGAKI, NobuyaSAJI, HideoTOYODA, KentaroKIMURA, HiroyukiOGAWA, YuHIRAO, KonomuNAGAKAWA, Kenji
    • A61K49/00C07K14/00
    • 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-NH 2 (1)
      Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH 2 (5)
      B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (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,

      where A represents either an aromatic hydrocarbon group or an aromatic heterocyclic group, R 1 represents a substituent that contains radioactive iodine, R 2 represents either a hydrogen atom or a substituent different from that represented by R 1 , and R 3 represents any one of a bond, a methylene group, and an oxymethylene group.
    • 提供胰岛成像的分子探针。 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-NH 2(1)Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH 2(5)B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2(9)其中式(1)和(5)中的X和B - 在式(9)中表示氨基被具有芳环的式(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,R 2表示氢原子或与R 1表示的不同的取代基,R 3表示键,亚甲基和氧亚甲基中的任一个。