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論文

Medical application of radiohalogenated peptides; Synthesis and ${it in vitro}$ evaluation of F(${it p}$-$$^{131}$$I)KCCYSL for targeting HER2

佐々木 一郎; 渡辺 茂樹; 大島 康宏; 須郷 由美; 山田 圭一*; 花岡 宏史*; 石岡 典子

Peptide Science 2015, p.243 - 246, 2016/03

Radioisotope labeled peptides 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. Radiohalogens such as $$^{131}$$I and $$^{211}$$At are useful for clinical imaging and therapeutic applications, and it can be introduced at the ${it para}$ position of phenylalanine residue via electrophilic destannylation. KCCYSL (Lys$$^{1}$$-Cys$$^{2}$$-Cys$$^{3}$$-Tyr$$^{4}$$-Ser$$^{5}$$-Leu$$^{6}$$) is a hexapeptide containing disulfide bond. Previous study revealed that KCCYSL has potential as tumor imaging and therapeutic agent targeting tumor cells overexpressing the human epidermal growth factor receptor type 2 (HER2). In this study, we report synthesis and ${it in vitro}$ evaluation of radiohalogenated KCCYSL derivatives. Precursor peptides, Boc-F(${it p}$-SnBu$$_{3}$$)K(Boc)C(Trt)C(Trt)Y($$^{t}$$Bu)S($$^{t}$$Bu)L-OH and Boc-F(${it p}$-SnBu$$_{3}$$)GS($$^{t}$$Bu)GK(Boc)C(Trt)C(Trt)Y($$^{t}$$Bu)S($$^{t}$$Bu)L-OH, were synthesized by the Fmoc solid phase peptide synthesis. Then, precursor peptides were radioiodinated via electrophilic destannylation, and they were deprotected to obtain F(${it p}$-$$^{131}$$I)KCCYSL and F(${it p}$-$$^{131}$$I)GSGKCCYSL in radiochemical yield 15% and 17%, respectively. ${it In vitro}$ assays of the radioiodinated peptides for HER2 and stability in serum are being undertaken.

論文

Simultaneous analysis of silicon and boron dissolved in water by combination of electrodialytic salt removal and ion-exclusion chromatography with corona charged aerosol detection

森 勝伸*; 佐柄 克哉*; 新井 香織*; 中谷 暢丈*; 大平 慎一*; 戸田 敬*; 板橋 英之*; 小崎 大輔*; 須郷 由美; 渡辺 茂樹; et al.

Journal of Chromatography A, 1431, p.131 - 137, 2016/01

 被引用回数:7 パーセンタイル:52.67(Biochemical Research Methods)

Selective separation and sensitive detection of dissolved silicon and boron (DSi and DB) in aqueous solution was achieved by connecting an electrodialytic ion isolation device (EID), an ion-exclusion chromatography (IEC) column, and a corona charged aerosol detector (CCAD) in sequence. They were separated by IEC using pure water eluent. Detection of DSi and DB by the CCAD was effective for much greater sensitivity than by conductimetric detection. The EID removed salt from the sample prior to the IEC-CCAD. The combination of EID, IEC and CCAD successfully separated and determined DSi and DB in artificial seawater and hot-spring water samples by eluting pure water.

論文

Preparation and evaluation of an astatine-211-labeled sigma receptor ligand for $$alpha$$ radionuclide therapy

小川 数馬*; 水野 覚瑛*; 鷲山 幸信*; 柴 和弘*; 高橋 成人*; 小阪 孝史*; 渡辺 茂樹; 篠原 厚*; 小谷 明*

Nuclear Medicine and Biology, 42(11), p.875 - 879, 2015/11

 被引用回数:13 パーセンタイル:34.92(Radiology, Nuclear Medicine & Medical Imaging)

Sigma receptors are overexpressed in a variety of human tumors, making them potential targets for radionuclide receptor therapy. We have previously synthesized and evaluated $$^{131}$$I-labeled (+)-2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-[$$^{131}$$I]pIV], which has a high affinity for sigma receptors. Therefore, (+)-[$$^{131}$$I]pIV significantly inhibited tumor cell proliferation in tumor-bearing mice. In the present study, we report the synthesis and the in vitro and in vivo characterization of (+)-[$$^{211}$$At]pAtV, an $$^{211}$$At-labeled sigma receptor ligand, that has potential use in $$alpha$$-radionuclide receptor therapy. The lipophilicity of (+)-[$$^{211}$$At]pAtV was similar to that of (+)-[$$^{125}$$I]-pIV. Uptake of DU-145, prostate cancer cell lines, and the biodistribution patterns in DU-145 tumor-bearing mice at 1 h post-injection were also similar between (+)-[$$^{211}$$At]pAtV and (+)-[$$^{125}$$I]-pIV. Namely, (+)-[$$^{211}$$At]pAtV demonstrated high uptake and retention in tumor via binding to sigma receptors.

論文

Nucleoside diphosphate kinase from psychrophilic ${it Pseudoalteromonas}$ sp. AS-131 isolated from Antarctic Ocean

米澤 悌*; 永山 あい子*; 徳永 廣子*; 石橋 松二郎*; 新井 栄揮; 黒木 良太; 渡邉 啓一*; 荒川 力*; 徳永 正雄*

Protein Journal, 34(4), p.275 - 283, 2015/08

 被引用回数:2 パーセンタイル:91.6(Biochemistry & Molecular Biology)

好冷菌${it Pseudoalteromonas}$ sp. AS-131由来ヌクレオシド二リン酸キナーゼ(ASNDK)の大腸菌による発現、および、精製に成功した。通常細菌由来ヌクレオシド二リン酸キナーゼと比較して、ASNDKは、(1)37$$^{circ}$$Cの大腸菌発現では変性した不溶性の状態で発現する。(2)活性の至適温度は30$$^{circ}$$C低い。など、熱的に不安定な特徴を有していた。また、ASNDKは、中度好塩菌由来ヌクレオシド二リン酸キナーゼのような二量体構造を形成することが示唆された。

論文

ワシントン大学(シアトル)留学記

渡辺 茂樹

放射線と産業, (138), p.52 - 54, 2015/06

本稿は、2013年3月から1年間アメリカ合衆国ワシントン州シアトルにあるワシントン大学へ留学中の研究成果と生活を報告したものである。

論文

Production and separation of astatine isotopes in the $$^7$$Li + $$^{nat}$$Pb reaction

西中 一朗; 横山 明彦*; 鷲山 幸信*; 前田 英太*; 渡辺 茂樹; 橋本 和幸; 石岡 典子; 牧井 宏之; 豊嶋 厚史; 山田 記大*; et al.

Journal of Radioanalytical and Nuclear Chemistry, 304(3), p.1077 - 1083, 2015/06

 被引用回数:7 パーセンタイル:38.07(Chemistry, Analytical)

29-57MeVの$$^7$$Liビームと$$^{nat}$$Pb標的核の反応においてアスタチン同位体$$^{207-211}$$Atの生成断面積を$$alpha$$線, $$gamma$$線スペクトルメトリーで測定した。生成断面積の励起関数を統計模型モデル計算と比較することで、$$^7$$Li + $$^{nat}$$Pbの反応機構を調べた。44MeVより大きい入射エネルギーでの$$^{210}$$Atと$$^{209}$$Atの生成断面積が理論値よりも小さいことから、分解反応が存在することを明らかにした。照射した鉛標的からのアスタチンの化学分離を乾式蒸留法に基づいて調べ、アスタチン製造の相補的な手法を開発した。

論文

Development of a widely usable amino acid tracer; $$^{76}$$Br-$$alpha$$-methyl-phenylalanine for tumor PET imaging

花岡 宏史*; 大島 康宏; 鈴木 結利花*; 山口 藍子*; 渡辺 茂樹; 上原 知也*; 永森 收志*; 金井 好克*; 石岡 典子; 対馬 義人*; et al.

Journal of Nuclear Medicine, 56(5), p.791 - 797, 2015/05

 被引用回数:12 パーセンタイル:34.92(Radiology, Nuclear Medicine & Medical Imaging)

Radiolabeled amino acids are superior PET tracers for imaging of malignant tumors, and amino acids labeled with $$^{76}$$Br, an attractive positron emitter due to its relatively long half-life (t$$_{1/2}$$=16.2 h), could potentially be widely usable tumor imaging tracer. In this study, in consideration of stability and tumor specificity, 2-$$^{76}$$Br-bromo-$$alpha$$-methyl-L-phenylalanine (2-$$^{76}$$Br-BAMP) and 4-$$^{76}$$Br-bromo-$$alpha$$-methyl-L-phenylalanine (4-$$^{76}$$Br-BAMP) were designed and their potential as a tumor imaging agent was evaluated. No-carrier-added $$^{76}$$Br and $$^{77}$$Br, the latter of which is suitable radiobromine for basic studies due to its longer half-life (t$$_{1/2}$$ = 57.1 h), were produced. Both $$^{77}$$Br-BAMPs were stable in the plasma and in the murine body. In biodistribution studies, 2-$$^{77}$$Br-BAMP showed more rapid blood clearance and lower renal accumulation than did 4-$$^{77}$$Br-BAMP. More than 90% of injected radioactivity was excreted in the urine by 6 h post-injection of 2-$$^{77}$$Br-BAMP. High tumor accumulation of 2-$$^{77}$$Br-BAMP was observed in tumor-bearing mice and PET imaging with 2-$$^{76}$$Br-BAMP enabled clear visualization of the tumor. These findings suggest that 2-$$^{76}$$Br-BAMP would constitute a potential new PET tracer for tumor imaging and may eventually enable the wider use of amino acid tracers.

論文

Stabilization of a high-order harmonic generation seeded extreme ultraviolet free electron laser by time-synchronization control with electro-optic sampling

冨澤 宏光*; 佐藤 尭洋*; 小川 奏*; 渡川 和晃*; 田中 隆次*; 原 徹*; 矢橋 牧名*; 田中 均*; 石川 哲也*; 富樫 格*; et al.

High Power Laser Science and Engineering, 3, p.e14_1 - e14_10, 2015/04

 被引用回数:2 パーセンタイル:81.74(Optics)

自由電子レーザー(FEL)は、共振器を使用しない自己増幅自発放射(SASE)方式を用いている。この方式では、自然放射光を種光としてレーザー発振・増幅するため、発振したレーザー光のスペクトルや時間波形がスパイク状構造になる欠点がある。この問題点を解決するために、短波長光源である高次高調波をFELにインジェクションし、スペクトルや時間波形にスパイク構造のないフルコヒーレント化された極端紫外領域(波長61.2nm)のシードFEL光の発生に成功した。しかしながら、外部からのコヒーレント光をシード光として用いる場合、電子バンチとシード光のタイミングドリフトにより、シードFEL光の出力ゆらぎが大きくなり、発生頻度も減少する問題がある。この問題点を解決するために、電気光学(Electro-Optic: EO)効果を利用したタイミングモニターを開発し、FEL装置の診断セクションに導入した。これにより、シードFEL光(波長61.2nm)の発生頻度が約0.3%から約25%に向上し、最大出力20$$mu$$Jが得られた。また、検討中の水の窓領域でのシードFELについても報告する。

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

JAEA-Review 2014-050, JAEA Takasaki Annual Report 2013, P. 100, 2015/03

MARSGL peptide (H-Met-Ala-Arg-Ser-Gly-Leu-OH) has high affinity to the human epidermal growth factor receptor 2 (HER2) overexpressing in various tumor cells. Copper-64 ($$^{64}$$Cu) is a useful radionuclide in nuclear medicine, and can be produced by the cyclotron. In this study, we designed and synthesized $$^{64}$$Cu-labeled MARSGL peptide conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) as a novel positron emission tomography (PET) imaging probe for HER2 overexpressing tumors. The formation of $$^{64}$$Cu-DOTA-MARSGL was determined by TLC and HPLC compared with a non-radioactive preparation. It was confirmed that $$^{64}$$Cu-DOTA-MARSGL was obtained in high radiochemical yield more than 94%. We also examined a stability of $$^{64}$$Cu-DOTA-MARSGL ${it in vitro}$. The chromatogram was not changed after incubation in physiological saline at 37$$^{circ}$$C overnight. In order to evaluate the usefulness as a PET imaging probe, further ${it in vitro}$ studies on the stability in human or mice plasma and the cellular uptake are in progress.

論文

Exploring of peptides with affinity to HER2 from random peptide libraries using radioisotope; Random hexapeptide libraries with fixed amino acid sequence at 1 and 2 positions

佐々木 一郎; 花岡 宏史*; 山田 圭一*; 渡辺 茂樹; 須郷 由美; 大島 康宏; 鈴木 博元; 石岡 典子

Peptide Science 2014, p.257 - 260, 2015/03

We have sought to establish drug discovery system using radioisotope (RI) labeled peptides which have high affinity to target proteins overexpressed in cancers. Of the target proteins, we chose the human epidermal growth factor receptor type 2 (HER2), a membrane protein overexpressed in various cancers to evaluate the drug discovery system. Three series of random hexapeptide libraries introduced a radioiodinated D-tyrosine (y(3-$$^{131}$$I)) to $$N$$-terminal were designed and binding assay with HER2-expressed cell lines were conducted in this study. First, we synthesized a series of random hexapeptide libraries with fixed amino acid sequence at 1 and 2 positions, y(3-$$^{131}$$I)X$$^{1}$$X$$^{2}$$X$$^{3}$$X$$^{4}$$X$$^{5}$$X$$^{6}$$. Non-radioactive random peptide libraries, yXXXXXX, were prepared by Fmoc-SPPS with an automatic peptide synthesizer. Radioiodinated y(3-$$^{131}$$I)XXXXXX were subsequently synthesized in 30-50% radiochemical yield. Binding assay using HER2-overexpressed cell line showed that high affinity (38-50% dose, n=6) was obtained with yIIXXXX, while other random peptide libraries were yielded low affinity (approximately 1% dose), which indicated that the system using RI labeled random peptide libraries have potential to discover peptide drug for cancer therapy. Preparation of other random hexapeptide libraries are being undertaken.

論文

Production of highly purified no-carrier-added $$^{177}$$Lu for radioimmunotherapy

渡辺 智; 橋本 和幸; 渡辺 茂樹; 飯田 靖彦*; 花岡 宏史*; 遠藤 啓吾*; 石岡 典子

Journal of Radioanalytical and Nuclear Chemistry, 303(1), p.935 - 940, 2015/01

 被引用回数:6 パーセンタイル:38.07(Chemistry, Analytical)

No-carrier-added $$^{177}$$Lu produced via the $$^{176}$$Yb(n, $$gamma$$) $$^{177}$$Yb $$rightarrow$$$$^{177}$$Lu process was separated from the macroscopic amounts of the Yb target using reversed-phase ion-pair liquid chromatography. To produce a highly purified $$^{177}$$Lu solution capable of labeling antibodies, the metallic impurities were removed using cation, chelating ion, and anion exchange columns. After the elimination of metallic impurities, the concentrations of Ca, Fe, and Zn were reduced from 87, 340, and 77 ppb to 13, 18, and 9 ppb, respectively. Consequently, the labeling yield of the $$^{177}$$Lu -labeled antibody increased from less than 5% to 88%.

論文

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

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

JAEA-Review 2013-059, JAEA Takasaki Annual Report 2012, P. 96, 2014/03

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.

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

Evaluation of a wet chemistry method for isolation of cyclotron produced [$$^{211}$$At] astatine

Balkin, E. R.*; Hamlin, D. K.*; Gagnon, K.*; Chyan, M.-K.*; Pal, S.*; 渡辺 茂樹; Wilbur, D. S.*

Applied Sciences (Internet), 3(3), p.636 - 655, 2013/09

 被引用回数:20 パーセンタイル:17.25(Chemistry, Multidisciplinary)

A "wet chemistry" approach for isolation of $$^{211}$$At from an irradiated bismuth target is described. The approach involves five steps: (1) dissolution of bismuth target in conc. HNO$$_{3}$$; (2) removal of the HNO$$_{3}$$ by distillation; (3) dissolution of residue in 8 M HCl; (4) extraction of $$^{211}$$At from 8 M HCl into DIPE; and (5) extraction of $$^{211}$$At from DIPE into NaOH. Results from 55 "optimized" At isolation runs gave recovery yields of approximately 78% after decay and attenuation corrections. An attenuation-corrected average of 26$$pm$$3 mCi in the target provided isolated (actual) yields of 16$$pm$$3 mCi of $$^{211}$$At. A sixth step, used for purification of $$^{211}$$At from trace metals, was evaluated in seven runs. In those runs, isolated $$^{211}$$At was distilled under reductive conditions to provide an average 71$$pm$$8% recovery. RadioHPLC analyses of the isolated $$^{211}$$At solutions, both initial and after distillation, were obtained to examine the $$^{211}$$At species present. The primary species of $$^{211}$$At present was astatide, but astatate and unidentified species were also observed. Studies to determine the effect of bismuth attenuation on $$^{211}$$At were conducted to estimate and attenuation factor ($$sim$$1.33) for adjustment of $$^{211}$$At readings in the bismuth target.

論文

Full-coherent free electron laser seeded by 13th- and 15th-order harmonics of near-infrared femtosecond laser pulses

佐藤 尭洋*; 岩崎 純史*; 大和田 成起*; 山内 薫*; 高橋 栄治*; 緑川 克美*; 青山 誠; 山川 考一; 富樫 格*; 深見 健司*; et al.

Journal of Physics B; Atomic, Molecular and Optical Physics, 46(16), p.164006_1 - 164006_6, 2013/08

 被引用回数:3 パーセンタイル:76.7(Optics)

自由電子レーザー(FEL)は、自己増幅自発放射方式を用いているため、発振したレーザー光のスペクトルや時間波形がスパイク状構造になる欠点がある。この問題点を解決するために、短波長光源である高次高調波をFELにインジェクションし、スペクトルや時間波形にスパイク構造のない極端紫外領域のシード型FELの研究開発を進めている。高次高調波を発生させるドライブレーザーである高出力フェムト秒・チタンサファイアCPAレーザーシステムは、これまで原子力機構で培ったレーザー技術を設計に活かし、レーザーシステムの構築を行った。そして、このドライブレーザーをXeガス中に集光して得られる13次高調波(波長61.7nm)、15次高調波(波長53.4nm)をシード光としてFELへインジェクションし、極端紫外領域でシード型FEL(波長61.2nm)の発振に世界で初めて成功した。また、シードFEL光のコントラスト比についても検討した。この結果について発表する。

論文

Full-coherent HHG-seeded EUV-FEL locked by EOS timing feedback

小川 奏*; 佐藤 尭洋*; 松原 伸一*; 岡安 雄一*; 富樫 格*; 渡部 貴宏*; 高橋 栄治*; 緑川 克美*; 青山 誠; 山川 考一; et al.

Proceedings of 10th Conference on Lasers and Electro-Optics Pacific Rim and 18th OptoElectronics and Communications Conference and Photonics in Switching 2013 (CLEO-PR & OECC/PS 2013) (USB Flash Drive), 2 Pages, 2013/06

自由電子レーザー(FEL)は、共振器を使用しない自己増幅自発放射(SASE)方式を用いている。この方式では、自然放射光を種光としてレーザー発振・増幅するため、発振したレーザー光のスペクトルや時間波形がスパイク状構造になる欠点がある。この問題点を解決するために、短波長光源である高次高調波をFELにインジェクションし、スペクトルや時間波形にスパイク構造のないフルコヒーレント化された極端紫外領域(波長61.5nm)のシードFEL光の発生に成功した。しかしながら、外部からのコヒーレント光をシード光として用いる場合、電子バンチとシード光のタイミングドリフトにより、シードFEL光の出力ゆらぎが大きくなり、発生頻度も減少する問題がある。この問題点を解決するために、電気光学(Electro-Optic: EO)効果を利用したタイミングモニターを開発し、FEL装置の診断セクションに導入した。これにより、シードFEL光(波長61.2nm)の発生頻度が約0.3%から約24%に向上し、最大出力20$$mu$$Jが得られた。この結果について発表する。

論文

Three-dimensional and multienergy $$gamma$$-ray simultaneous imaging by using a Si/CdTe Compton camera

鈴木 義行*; 山口 充孝; 小高 裕和*; 島田 博文*; 吉田 由香里*; 鳥飼 幸太*; 佐藤 隆博; 荒川 和夫*; 河地 有木; 渡辺 茂樹; et al.

Radiology, 267(3), p.941 - 947, 2013/06

 被引用回数:10 パーセンタイル:53.1(Radiology, Nuclear Medicine & Medical Imaging)

Capabillity tests of 3D imaging for medical applications were performed by using a new Compton camera. $$^{18}$$F, $$^{131}$$I and $$^{67}$$Ga separately compacted into micro tubes were injected subcutaneously into a Wister rat and imaged after sacrifice of the rat (ex-vivo model). In a separate experiment $$^{111}$$In-chloride and $$^{131}$$I-Methylnorcholestenol were injected into a rat intravenously and $$^{64}$$Cu was injected into the stomach orally just before imaging (more physiological model). The Compton camera demonstrated its 3D multinuclear imaging capability by separating out the three nuclear distributions clearly in ex-vivo model. In the more physiological model, the distributions of $$^{131}$$I and $$^{64}$$Cu were clearly imaged although $$^{111}$$In was difficult to visualize due to blurring at low energy region of $$gamma$$-ray. In conclusion, our new Compton camera successfully demonstrated highly resolved multiplanar and multinuclear $$gamma$$-ray simultaneous imaging.

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.

論文

High intense full-coherent radiation of free electron laser seeded by high-order harmonics in extreme-ultraviolet region

富樫 格*; 高橋 栄治*; 緑川 克美*; 青山 誠; 山川 考一; 佐藤 尭洋*; 岩崎 純史*; 大和田 成起*; 山内 薫*; 原 徹*; et al.

Proceedings of Ultrafast Optics IX (CD-ROM), 2 Pages, 2013/03

自由電子レーザー(FEL)は、共振器を使用しない自己増幅自発放射(SASE)方式を用いている。この方式では、自然放射光を種光としてレーザー発振・増幅するため、発振したレーザー光のスペクトルや時間波形がスパイク状構造になる欠点がある。この問題点を解決するために、短波長光源である高次高調波をFELにインジェクションし、スペクトルや時間波形にスパイク構造のないフルコヒーレント化された極端紫外領域のシード型自由電子レーザーの研究開発を進めている。高次高調波を発生させるドライブレーザーである高出力フェムト秒・チタンサファイアCPAレーザーシステムは、これまで原子力機構で培ったレーザー技術を設計に活かし、レーザーシステムの構築を行った。そして、このドライブレーザーをXeガス中に集光して得られる13次高調波(波長61.2nm)をシード光としてFELへインジェクションし、極端紫外領域でシード型FEL(波長61.2nm)の発振に世界で初めて成功した。高次高調波のシーディングによりSASE方式特有のスパイク構造がなくなり、スムーズなスペクトルが得られた。

論文

Synthesis of radioiodinated antitumor cyclic peptide, [$$^{125}$$I]-sansalvamide A derivative

渡邉 茂樹; 山田 圭一*; 津久井 匠隆*; 花岡 宏史*; 大島 康宏; 山口 藍子*; 奥 浩之*; 石岡 典子

JAEA-Review 2012-046, JAEA Takasaki Annual Report 2011, P. 88, 2013/01

Sansalvamide A (SA), a penta cyclic peptide isolated marine fungus, is a lead compound of anti-cancer reagent because the peptide has cytotoxicity against various cancer cell lines. Halogenated SA derivatives (SA-X, X = Cl, Br, I) was prepared and remarkable cytotocity against malignant human breast cancer. In this study, a radiohalogenated SA derivative [$$^{125}$$I]SA-I was prepared to conduct in vivo evaluation of SA derivatives. Synthetic scheme of [$$^{125}$$I]SA-I are as follows: an iodinated linear peptide, Boc-F(p-I)LLVL-OMe, was prepared by the conventional solid phase peptide synthesis. After preparation of stannylated peptide, Boc-F(p-SnBu$$_{3}$$)LLVL-OMe, $$^{125}$$I was labeled with electrophilic destannylation in the presence of oxidizing reagent. After deprotection of N- and C-termius, [$$^{125}$$I]SA-I was obtained successfully by macrocyclization in liquid phase. Overall labeled yield was 7%. To our best knowledge, this report is the first on the synthesis of radiolabeled SA derivative. In vivo evaluation of the SA derivative using [$$^{125}$$I]SA-I is being undertaken.

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