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Report No.

Synthesis of radiohalogen-labeled peptide with high affinity to HER2/neu receptor

Sasaki, Ichiro; Yamada, Keiichi*; Watanabe, Shigeki; Hanaoka, Hirofumi*; Sugo, Yumi; Oku, Hiroyuki*; Ishioka, Noriko

Radioisotope (RI)-labeled peptide with high affinity to receptors overexpressing on the surface of tumor cells are promising for applications in nuclear medicine such as diagnostic radiography and radiotherapy. MARSGL (H-Met$$^{1}$$-Ala$$^{2}$$-Arg$$^{3}$$-Ser$$^{4}$$-Gly$$^{5}$$-Leu$$^{6}$$-OH), a linear peptide consisting of six amino acids, has high affinity to HER2/neu receptor overexpressing in various cancer cells. Radiohalogens (radionuclides) such as radioiodine and radiobromine are versatile for clinical imaging and therapeutic applications. Thus, radiohalogenated MARSGL may have potential for clinical applications to HER2 overexpressing tumors. In this study, in order to achieve the labeling of radiohalogen for MARSGL, we design a radioiodinated peptide, F(${it p}$-$$^{131}$$I)MARSGL, in which phenylalanine labeled with $$^{131}$$I (t$$_{1/2}$$ = 8.0 d) at the ${it para}$ position of the aromatic ring is introduced into the N-terminal of MARSGL and report a new technique to prepare radiohalogen of peptide via electrophilic destanylation.



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