摘要:
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.
摘要:
A molecular probe for imaging of pancreatic islets is provided. The molecular probe includes a polypeptide represented by the following formula (1), or a polypeptide that has a homology with the foregoing polypeptide. (SEQ ID NO. 1) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2 (1) Wherein “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a group represented by the following chemical formula (I), wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group; R1 represents a substituent that contains 11C, 13N, 15O, 18F, 64Cu, 67Ga, 68Ga, 75Br, 76Br, 77Br, 99mTc, 111In, 123I, 124I, 125I, or 131I; R2 represents either a hydrogen atom, or a substituent different from that represented by R1; and R3 represents any one of a bond, an alkylene group having 1 to 6 carbon atoms, and an oxyalkylene group having 1 to 6 carbon atoms.
摘要翻译:提供了用于胰岛成像的分子探针。 分子探针包括由下式(1)表示的多肽,或与前述多肽具有同源性的多肽。 (SEQ ID NO.1)Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2(1)其中,“X”表示赖氨酸残基,赖氨酸残基的侧链的氨基用下述化学式(I)表示的基团标记, 其中A表示芳族烃基或芳族杂环基; R1表示含有11C,13N,150C,18F,64Cu,67Ga,68Ga,75Br,76Br,77Br,99mTc,111In,123I,124I,125I或131I的取代基; R2表示氢原子或与R1表示的取代基不同的取代基; R3表示碳原子数1〜6的亚烷基,碳原子数1〜6的氧亚烷基。
摘要:
A precursor of molecular probe for imaging of pancreatic islets is provided. A polypeptide represented by any one of the following formulae (1) to (4), or a polypeptide having a homology with the foregoing polypeptide. *-DLSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(1) *-LSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(2) *-SK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(3) *-K* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2,(4) wherein *- indicates that an α-amino group at an N-terminus is protected by a protecting group or modified with a modifying group having no electric charge; K* indicates that an amino group of a side chain of a lysine is protected by a protecting group; and —NH2 indicates that a carboxyl group at a C-terminus is amidated.
摘要:
A molecular probe for imaging of pancreatic islets is provided. The molecular probe includes a polypeptide represented by the following formula (1), or a polypeptide that has a homology with the foregoing polypeptide. (SEQ ID NO. 1) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2 (1) Wherein “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a group represented by the following chemical formula (I), wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group; R1 represents a substituent that contains 11C, 13N, 15O, 18F, 64Cu, 67Ga, 68Ga, 75Br, 76Br, 77Br, 99mTc, 111In, 123I, 124I, 125I, or 131I; R2 represents either a hydrogen atom, or a substituent different from that represented by R1; and R3 represents any one of a bond, an alkylene group having 1 to 6 carbon atoms, and an oxyalkylene group having 1 to 6 carbon atoms.
摘要翻译:提供了用于胰岛成像的分子探针。 分子探针包括由下式(1)表示的多肽,或与前述多肽具有同源性的多肽。 (SEQ ID NO.1)Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2(1)其中,“X”表示赖氨酸残基,赖氨酸残基的侧链的氨基用下述化学式(I)表示的基团标记, 其中A表示芳族烃基或芳族杂环基; R1表示含有11C,13N,150C,18F,64Cu,67Ga,68Ga,75Br,76Br,77Br,99mTc,111In,123I,124I,125I或131I的取代基; R2表示氢原子或与R1表示的取代基不同的取代基; R3表示碳原子数1〜6的亚烷基,碳原子数1〜6的氧亚烷基。
摘要:
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.
摘要翻译: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。
摘要:
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.
摘要翻译: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。
摘要:
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.
摘要:
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-NH2 (1) *-LSKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (2) *-SKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (3) *-KQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (4) *-DLSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (5) *-LSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (6) *-SK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (7) *-K*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (8) DLSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (9) LSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (10) SK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (11) K*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (12)
摘要:
A precursor of a molecular probe for imaging of pancreatic islets is a compound expressed as the following formula (I): wherein -V-X represents a substituent on a benzene ring, V represents a bond, R1, of OR1, R1 represents a C1-C6 alkylene group, R2 represents H (hydrogen atom), a C1-C6 alkyl group, a C7-C10 aralkyl group, or a protecting group, X represents a OMs group, a OTs group, a OTf group, Br (bromine atom), or I (iodine atom), and carbon marked with * is an asymmetric carbon atom.
摘要:
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-NH2 (1) *-LSKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (2) *-SKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (3) *-KQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (4) *-DLSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (5) *-LSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (6) *-SK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (7) *-K*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (8) DLSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (9) LSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (10) SK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (11) K*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (12)