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論文

Synthesis and ${it in vitro}$ Evaluation of $$^{64}$$Cu-labeled peptide for tumor imaging

須郷 由美; 佐々木 一郎; 渡辺 茂樹; 大島 康宏; 石岡 典子

Peptide Science 2013, p.355 - 358, 2014/03

HER2 is a member of the epidermal growth factor receptor family, which is overexpressed on the surface of tumor cells. H-Met-Ala-Arg-Ser-Gly-Leu-OH (MARSGL) is a linear peptide having high affinity to HER2 overexpressing in various cancer cells. In the previous study, we have synthesized a novel radioiodinated MARSGL via electrophilic destannylation in high radiochemical yield. $$^{64}$$Cu is an attractive radionuclide for positron emission tomography imaging as well as radiotherapy due to its half-life of 12.7 h and decay characteristics of both $$beta$$$$^{+}$$ and $$beta$$$$^{-}$$. 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) is a macrocyclic ligand for various metal ions. In this study, we designed and synthesized $$^{64}$$Cu-labeled MARSGL peptide conjugated with DOTA as an imaging probe for HER2 overexpressing tumors. In order to evaluate the usefulness of $$^{64}$$Cu-DOTA-MARSGL peptide as a PET imaging probe,${it in vitro}$ studies were also performed.

論文

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

佐々木 一郎; 山田 圭一*; 渡邉 茂樹; 花岡 宏史*; 須郷 由美; 奥 浩之*; 石岡 典子

Peptide Science 2013, p.157 - 160, 2013/03

Radioisotope (RI)-labeled peptides which have the high affinity to receptors on surface of the tumor cell are promising for diagnostic radiography (PET and SPECT) and radiotherapy. MARSGL (H-Met$$^{1}$$-Ala$$^{2}$$-Arg$$^{3}$$-Ser$$^{4}$$-Gly$$^{5}$$-Leu$$^{6}$$-OH), a linear hexapeptide consisting of six amino acids, has the high affinity to HER2/neu receptor overexpressing in various cancer cells. Thus, radiolabeled MARSGL has potential for the above mentioned purposes. Radiohalogens have various useful radionuclides, which could be introduced to aromatic compounds via tin-halogen exchange reaction. In this study, stannylated peptide Boc-F(${it p}$-SnBu$$_{3}$$)MAR(Pbf)S($$^{t}$$Bu)GL-OH was synthesized to prepare radiohalogen ($$^{76}$$Br or $$^{131}$$I)-labeled FMARSGL derivatives. First, Boc-Phe(${it p}$-SnBu$$_{3}$$)-OH was prepared from Boc-Phe(${it p}$-I)-OMe via Pd(0)-catalyzed coupling reaction with (Bu$$_{3}$$Sn)$$_{2}$$ and was successfully introduced into ${it N}$-terminal of H-MARSGL-Trt(2-Cl) resin synthesized from H-Leu-Trt(2-Cl) resin by Fmoc-SPPS. After cleavage reaction of Boc-F(${it p}$-SnBu$$_{3}$$)MAR(Pbf)S($$^{t}$$Bu)GL-Trt(2-Cl) resin with 25% 1,1,1,3,3,3-hexafluoro-2-propanol in CH$$_{2}$$Cl$$_{2}$$, Boc-F(${it p}$-SnBu$$_{3}$$)MAR(Pbf)S($$^{t}$$Bu)GL-OH was obtained and identified by using ESI-MS and NMR. Synthesis of $$^{131}$$I-labeled FMARSGL is due to report in this presentation.

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