Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer
Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer...
Ausführliche Beschreibung
Autor*in: |
Di Xiao [verfasserIn] Xiaojiang Duan [verfasserIn] Qianqian Gan [verfasserIn] Xuran Zhang [verfasserIn] Junbo Zhang [verfasserIn] |
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Format: |
E-Artikel |
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Sprache: |
Englisch |
Erschienen: |
2020 |
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Schlagwörter: |
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Übergeordnetes Werk: |
In: Molecules - MDPI AG, 2003, 25(2020), 23, p 5548 |
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Übergeordnetes Werk: |
volume:25 ; year:2020 ; number:23, p 5548 |
Links: |
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DOI / URN: |
10.3390/molecules25235548 |
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Katalog-ID: |
DOAJ078207665 |
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520 | |a Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. | ||
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10.3390/molecules25235548 doi (DE-627)DOAJ078207665 (DE-599)DOAJd3a690fb296d46ba8475b97988d0b4d7 DE-627 ger DE-627 rakwb eng QD241-441 Di Xiao verfasserin aut Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging Organic chemistry Xiaojiang Duan verfasserin aut Qianqian Gan verfasserin aut Xuran Zhang verfasserin aut Junbo Zhang verfasserin aut In Molecules MDPI AG, 2003 25(2020), 23, p 5548 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:23, p 5548 https://doi.org/10.3390/molecules25235548 kostenfrei https://doaj.org/article/d3a690fb296d46ba8475b97988d0b4d7 kostenfrei https://www.mdpi.com/1420-3049/25/23/5548 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 23, p 5548 |
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10.3390/molecules25235548 doi (DE-627)DOAJ078207665 (DE-599)DOAJd3a690fb296d46ba8475b97988d0b4d7 DE-627 ger DE-627 rakwb eng QD241-441 Di Xiao verfasserin aut Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging Organic chemistry Xiaojiang Duan verfasserin aut Qianqian Gan verfasserin aut Xuran Zhang verfasserin aut Junbo Zhang verfasserin aut In Molecules MDPI AG, 2003 25(2020), 23, p 5548 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:23, p 5548 https://doi.org/10.3390/molecules25235548 kostenfrei https://doaj.org/article/d3a690fb296d46ba8475b97988d0b4d7 kostenfrei https://www.mdpi.com/1420-3049/25/23/5548 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 23, p 5548 |
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10.3390/molecules25235548 doi (DE-627)DOAJ078207665 (DE-599)DOAJd3a690fb296d46ba8475b97988d0b4d7 DE-627 ger DE-627 rakwb eng QD241-441 Di Xiao verfasserin aut Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging Organic chemistry Xiaojiang Duan verfasserin aut Qianqian Gan verfasserin aut Xuran Zhang verfasserin aut Junbo Zhang verfasserin aut In Molecules MDPI AG, 2003 25(2020), 23, p 5548 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:23, p 5548 https://doi.org/10.3390/molecules25235548 kostenfrei https://doaj.org/article/d3a690fb296d46ba8475b97988d0b4d7 kostenfrei https://www.mdpi.com/1420-3049/25/23/5548 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 23, p 5548 |
allfieldsGer |
10.3390/molecules25235548 doi (DE-627)DOAJ078207665 (DE-599)DOAJd3a690fb296d46ba8475b97988d0b4d7 DE-627 ger DE-627 rakwb eng QD241-441 Di Xiao verfasserin aut Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging Organic chemistry Xiaojiang Duan verfasserin aut Qianqian Gan verfasserin aut Xuran Zhang verfasserin aut Junbo Zhang verfasserin aut In Molecules MDPI AG, 2003 25(2020), 23, p 5548 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:23, p 5548 https://doi.org/10.3390/molecules25235548 kostenfrei https://doaj.org/article/d3a690fb296d46ba8475b97988d0b4d7 kostenfrei https://www.mdpi.com/1420-3049/25/23/5548 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 23, p 5548 |
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10.3390/molecules25235548 doi (DE-627)DOAJ078207665 (DE-599)DOAJd3a690fb296d46ba8475b97988d0b4d7 DE-627 ger DE-627 rakwb eng QD241-441 Di Xiao verfasserin aut Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging Organic chemistry Xiaojiang Duan verfasserin aut Qianqian Gan verfasserin aut Xuran Zhang verfasserin aut Junbo Zhang verfasserin aut In Molecules MDPI AG, 2003 25(2020), 23, p 5548 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:25 year:2020 number:23, p 5548 https://doi.org/10.3390/molecules25235548 kostenfrei https://doaj.org/article/d3a690fb296d46ba8475b97988d0b4d7 kostenfrei https://www.mdpi.com/1420-3049/25/23/5548 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 25 2020 23, p 5548 |
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Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer |
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Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. |
abstractGer |
Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. |
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Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with <sup<99m</sup<Tc to prepare [<sup<99m</sup<Tc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (<i<K</i<<sub<i</sub< value is 8.79 nM) in LNCaP cells. The [<sup<99m</sup<Tc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log <i<P</i< = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer. |
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Micro-SPECT imaging demonstrated that the [<sup<99m</sup<Tc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [<sup<99m</sup<Tc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer.</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a"><sup<99m</sup<Tc</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a">PSMA</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a">isonitrile</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a">prostate cancer</subfield></datafield><datafield tag="650" ind1=" " ind2="4"><subfield code="a">SPECT imaging</subfield></datafield><datafield tag="653" ind1=" " ind2="0"><subfield code="a">Organic chemistry</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Xiaojiang Duan</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="700" ind1="0" ind2=" "><subfield code="a">Qianqian Gan</subfield><subfield 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