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Journal Articles

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

Hanaoka, Hirofumi*; Ohshima, Yasuhiro; Suzuki, Yurika*; Yamaguchi, Aiko*; Watanabe, Shigeki; Uehara, Tomoya*; Nagamori, Shushi*; Kanai, Yoshikatsu*; Ishioka, Noriko; Tsushima, Yoshito*; et al.

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

https://doi.org/10.2967/jnumed.114.152215
 Times Cited Count：18 Percentile：62.62(Radiology, Nuclear Medicine & Medical Imaging)

Journal Articles

Design, synthesis, and evaluation of [$$^{188}$$Re]Organorhenium-labeled antibody fragments with renal enzyme-cleavable linkage for low renal radioactivity levels

Uehara, Tomoya*; Koike, Miho*; Nakata, Hideo*; Hanaoka, Hirofumi*; Iida, Yasuhiko*; Hashimoto, Kazuyuki; Akizawa, Hiromichi*; Endo, Keigo*; Arano, Yasushi*

Bioconjugate Chemistry, 18(1), p.190 - 198, 2007/01

https://doi.org/10.1021/bc0602329
 Times Cited Count：20 Percentile：55.24(Biochemical Research Methods)

Renal localization of radiolabeled antibody fragments constitutes a problem in targeted imaging and radiotherapy. To estimate the applicability of the molecular design to metallic radionuclides, [$$^{188}$$Re]tricarbonyl(cyclopentadienylcarbonate)rhenium ([$$^{188}$$Re]CpTR-COOH) was conjugated with maleoyl-glycyl-lysine to prepare [$$^{188}$$Re]CpTR-GK. The cleavage of the glycyl-lysine linkage of the compound generates a glycine conjugate of [$$^{188}$$Re]CpTR-Gly. [$$^{188}$$Re]CpTR-GK was conjugated to thiolated Fab fragments to prepare [$$^{188}$$Re]CpTR-GK-Fab. The biodistribution of radioactivity after injection of [$$^{188}$$Re]CpTR-GK-Fab was compared with that of [$$^{188}$$Re]CpTR-Fab. [$$^{188}$$Re]CpTR-GK-Fab exhibited significantly lower renal radioactivity levels than did [$$^{188}$$Re]CpTR-Fab. The analysis of urine samples collected for 6 h postinjection of [$$^{188}$$Re]CpTR-GK-Fab showed that [$$^{188}$$Re]CpTR-Gly was the major radiometabolite. In tumor-bearing mice, [$$^{188}$$Re]CpTR-GK-Fab significantly reduced renal radioactivity levels without impairing the radioactivity levels in tumor. These findings indicate that the molecular design of radioparmaceuticals labeled with metallic radionuclides can be useful by using a radiometal chelate of high inertness and by designing a radiometabolite of high urinary excretion when released from antibody fragments following cleavage of a glycyl-lysine linkage. This study also indicates that a change in chemical structure of a radiolabel attached to a glycyl-lysine linkage significantly affected enzymes involved in the hydrolysis reaction.

Journal Articles

Assessment of $$^{186}$$Re chelate-conjugated bisphosphonate for the development of new radiopharmaceuticals for bones

Uehara, Tomoya*; Jin, Z. L.*; Ogawa, Kazuma*; Akizawa, Hiromichi*; Hashimoto, Kazuyuki; Nakayama, Morio*; Arano, Yasushi*

Nuclear Medicine and Biology, 34(1), p.79 - 87, 2007/01

https://doi.org/10.1016/j.nucmedbio.2006.10.001
 Times Cited Count：23 Percentile：56.61(Radiology, Nuclear Medicine & Medical Imaging)

In this study, a key factor affecting the pharmacokinetics of a chelate-conjugated BP was investigated to estimate the validity and the applicability of molecular design. Chemically inert and well-characterized [$$^{186}$$Re]CpTR-Gly was conjugated with 3-amino-1-hydroxypropylidene-1,1-bisphosphonate and purified by HPLC to prepare [$$^{186}$$Re]CpTR-Gly-APD. Plasma stability, plasma protein binding, hydroxyapatite (HA) binding and the pharmacokinetics of [$$^{186}$$Re]CpTR-Gly-APD were compared with those of $$^{186}$$Re 1-hydroxyethylidene-1,1-diphosphonate (HEDP). The HPLC-purified [$$^{186}$$Re]CpTR-Gly-APD showed higher plasma stability, higher HA binding, higher bone accumulation and lower plasma protein binding than did $$^{186}$$Re -HEDP. Although $$^{186}$$Re -HEDP possessed HA binding and bone accumulation similar to those of [$$^{186}$$Re]CpTR-Gly-APD, the specific activity of $$^{186}$$Re -labeled BPs was found to play a crucial role in bone accumulation and blood clearance. Thus, the molecular design of chelate-conjugated BP would be useful for the development of bone-seeking radiopharmaceuticals with a variety of radionuclides by selecting chelating molecules that provide high specific activities.

Journal Articles

Rhemium-186-monoaminemonoamidedithiol-conjugated bisphosphonate derivatives for bone pain palliation

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Otaka, Akira*; Ueda, Masashi*; Uehara, Tomoya*; Magata, Yasuhiro*; Hashimoto, Kazuyuki; Saji, Hideo*

Nuclear Medicine and Biology, 33(4), p.513 - 520, 2006/05

https://doi.org/10.1016/j.nucmedbio.2006.03.006
 Times Cited Count：54 Percentile：80.16(Radiology, Nuclear Medicine & Medical Imaging)

To develop a radiopharmaceutical for the palliation of painful bone metastases based on the concept of bifunctional radiopharmaceuticals, we synthesized a bisphosphonate derivative labeled with rhenium-186 ($$^{186}$$Re) that contains a hydroxyl group at the central carbon of its bisphosphonate structure and attached a stable $$^{186}$$Re-MAMA chelate to the amino group of a 4-amino-butylidene-bisphosphonate derivative, $$^{186}$$Re-MAMA-HBP, and investigated the effect of a hydroxyl group at the central carbon of its bisphosphonate structure on the affinity for hydroxyapatite and biodistribution by conducting a comparative study with $$^{186}$$Re-MAMA-BP. $$^{186}$$Re-MAMA-HBP was prepared by a reaction with $$^{186}$$ReO$$_{4}$$$$^{-}$$ and SnCl$$_{2}$$ in citrate buffer after the deprotection of trityl groups of Tr-MAMA-HBP. After reversed phase HPLC, $$^{186}$$Re-MAMA-HBP had a radiochemical purity of over 95 %. Compared with $$^{186}$$Re-MAMA-BP, $$^{186}$$Re-MAMA-HBP showed a greater affinity for hydroxyapatite beads in vitro and accumulated a significantly higher level in the femur in vivo. Thus, the introduction of a hydroxyl group into $$^{186}$$Re complex-conjugated bisphosphonates would be effective in enhancing accumulation in bone. These findings provide useful information on the design of bone-seeking therapeutic radiopharmaceuticals.

Journal Articles

Development of a Rhenium-186-labeled MAG3-conjugated bisphosphonate for the palliation of metastatic bone pain based on the concept of bifunctional radiopharmaceuticals

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Ono, Masahiro*; Hanaoka, Hirofumi*; Ishino, Seigo*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*

Bioconjugate Chemistry, 16(4), p.751 - 757, 2005/07

https://doi.org/10.1021/bc040249w
 Times Cited Count：61 Percentile：86.86(Biochemical Research Methods)

Rhenium-186-1-hydroxyethylidene-1,1-diphosphonate ($$^{186}$$Re-HEDP) has been used for the palliation of metastatic bone pain. Delayed blood clearance and high gastric uptake of radioactivity have been observed upon injection, due to the instability of $$^{186}$$Re-HEDP in vivo. In this study, on the basis of the concept of bifunctional radiopharmaceuticals, we designed a stable $$^{186}$$Re-mercaptoacetylglycylglycylglycine (MAG3) complex-conjugated bisphosphonate ($$^{186}$$Re-MAG3-HBP). After purification by HPLC, $$^{186}$$Re-MAG3-HBP was synthesized with a radiochemical purity of over 95%. In biodistribution experiments, the radioactivity level of$$^{186}$$Re-MAG3-HBP in bone was significantly higher than that of $$^{186}$$Re-HEDP. Blood clearance of $$^{186}$$Re-MAG3-HBP was faster than that of $$^{186}$$Re-HEDP. In addition, the gastric accumulation of $$^{186}$$Re-MAG3-HBP radioactivity was lower than that of $$^{186}$$Re-HEDP. In conclusion, $$^{186}$$Re-MAG3-HBP is expected to be a useful radiopharmaceutical for the palliation of metastatic bone pain.

Journal Articles

Design of a radiopharmaceutical for the palliation of painful bone metastases; Rhenium-186-labeled bisphosphonate derivative

Ogawa, Kazuma*; Mukai, Takahiro*; Arano, Yasushi*; Hanaoka, Hirofumi*; Hashimoto, Kazuyuki; Nishimura, Hiroshi*; Saji, Hideo*

Journal of Labelled Compounds and Radiopharmaceuticals, 47(11), p.753 - 761, 2004/11

https://doi.org/10.1002/jlcr.864
 Times Cited Count：28 Percentile：61.65(Biochemical Research Methods)

no abstracts in English

Journal Articles

In vivo recognition of Cyclopentadienyltricarbonylrhenium (CpTR) derivatives

Uehara, Tomoya*; Koike, Miho*; Nakata, Hideo*; Miyamoto, Shigehiko*; Motoishi, Shoji; Hashimoto, Kazuyuki; Oku, Naoto*; Nakayama, Morio*; Arano, Yasushi*

Nuclear Medicine and Biology, 30(3), p.327 - 334, 2003/04

https://doi.org/10.1016/S0969-8051(02)00437-7
 Times Cited Count：20 Percentile：50.16(Radiology, Nuclear Medicine & Medical Imaging)

no abstracts in English

Journal Articles

Synthesis and evaluation of bisphosphonate derivative labeled with Rhenium-186 using monoaminemonoamidedithiols as a chelating group

Mukai, Takahiro*; Ogawa, Kazuma*; Arano, Yasushi*; Ono, Masahiro*; Fujioka, Yasushi*; Izumo, Mishiroku; Konishi, Junji*; Saji, Hideo*

Journal of Labelled Compounds and Radiopharmaceuticals, 44(Suppl.1), p.S617 - S618, 2001/05

no abstracts in English

Journal Articles

Labeling with radioactive rhenium for the purpose of the pain relief of cancerous bone metastasis

Ogawa, Kazuma*; Ono, Masahiro*; Fujioka, Yasushi*; Saji, Hideo*; Mukai, Takahiro*; Konishi, Junji*; Uehara, Tomoya*; Arano, Yasushi*; Onoma, Katsuyuki

Kaku Igaku, 37(5), P. 577, 2000/09

no abstracts in English

Oral presentation

Design of bone-targeted labeled oligoaspartate with $$^{99m}$$Tc and $$^{186/188}$$Re

Kiyota, Sachiko*; Uehara, Tomoya*; Ishii, Daisuke*; Akizawa, Hiromichi*; Hashimoto, Kazuyuki; Arano, Yasushi*

no journal, , 

no abstracts in English

Oral presentation

Development of $$^{76}$$Br-labeled antibody fragments for reduction of non-target radioactivity

Hanaoka, Hirofumi*; Watanabe, Shigeki; Watanabe, Satoshi; Ohshima, Yasuhiro; Uehara, Tomoya*; Akizawa, Hiromichi*; Iida, Yasuhiko*; Ishioka, Noriko; Arano, Yasushi*; Endo, Keigo*

no journal, , 

no abstracts in English

Oral presentation

Development of a $$^{76}$$Br-labeled amino acid derivative for PET imaging of tumor

Hanaoka, Hirofumi*; Watanabe, Shigeki; Tominaga, Hideyuki*; Ohshima, Yasuhiro; Watanabe, Satoshi; Yamada, Keiichi*; Arano, Yasushi*; Ishioka, Noriko; Endo, Keigo*

no journal, , 

no abstracts in English

Oral presentation

Synthesis and ${it in vivo}$ evaluation of $$^{111}$$In labeled hippuric acid derivative with high urinary excretion

Suzuki, Hiroyuki; Kanai, Ayaka*; Uehara, Tomoya*; Hanaoka, Hirofumi*; Arano, Yasushi*

no journal, , 

Oral presentation

Development of 2-[$$^{211}$$At]astato-$$alpha$$-methyl-L-phenylalanine (2-AAMP) as a novel radiopharmaceutical for internal radiotherapy

Ohshima, Yasuhiro; Suzuki, Hiroyuki*; Hanaoka, Hirofumi*; Watanabe, Shigeki; Watanabe, Satoshi; Watanabe, Naoyuki*; Tsushima, Yoshito*; Endo, Keigo*; Arano, Yasushi*; Ishioka, Noriko

no journal, , 

Oral presentation

Development of 2-$$^{76}$$Br-bromo-$$alpha$$-methyl-L-phenylalanine as a novel $$^{76}$$Br-labeled PET tracer

Ohshima, Yasuhiro; Hanaoka, Hirofumi*; Suzuki, Yurika*; Yamaguchi, Aiko*; Watanabe, Shigeki; Uehara, Tomoya*; Nagamori, Shushi*; Kanai, Yoshikatsu*; Ishioka, Noriko; Tsushima, Yoshito*; et al.

no journal, , 

no abstracts in English

Oral presentation

Synthesis and evaluation of $$^{211}$$At labeled $$alpha$$-methyl-L-phenylalanine

Suzuki, Hiroyuki*; Ohshima, Yasuhiro; Hanaoka, Hirofumi*; Watanabe, Shigeki; Watanabe, Satoshi; Sasaki, Ichiro; Sakashita, Tetsuya; Arano, Yasushi*; Ishioka, Noriko

no journal, , 

no abstracts in English

16 (Records 1-16 displayed on this page)
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