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

Gespeichert in:

Autor*in:	Di Xiao [verfasserIn] Xiaojiang Duan [verfasserIn] Qianqian Gan [verfasserIn] Xuran Zhang [verfasserIn] Junbo Zhang [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2020

Schlagwörter:	PSMA isonitrile prostate cancer SPECT imaging

Übergeordnetes Werk:	In: Molecules - MDPI AG, 2003, 25(2020), 23, p 5548
Übergeordnetes Werk:	volume:25 ; year:2020 ; number:23, p 5548

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/molecules25235548

Katalog-ID:	DOAJ078207665

Internformat


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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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allfields	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
spelling	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
allfields_unstemmed	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
allfieldsSound	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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callnumber-first	Q - Science
author	Di Xiao
spellingShingle	Di Xiao misc QD241-441 misc <sup<99m</sup<Tc misc PSMA misc isonitrile misc prostate cancer misc SPECT imaging misc Organic chemistry 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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topic_title	QD241-441 Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer <sup<99m</sup<Tc PSMA isonitrile prostate cancer SPECT imaging
topic	misc QD241-441 misc <sup<99m</sup<Tc misc PSMA misc isonitrile misc prostate cancer misc SPECT imaging misc Organic chemistry
topic_unstemmed	misc QD241-441 misc <sup<99m</sup<Tc misc PSMA misc isonitrile misc prostate cancer misc SPECT imaging misc Organic chemistry
topic_browse	misc QD241-441 misc <sup<99m</sup<Tc misc PSMA misc isonitrile misc prostate cancer misc SPECT imaging misc Organic chemistry
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title	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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title_full	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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author_browse	Di Xiao Xiaojiang Duan Qianqian Gan Xuran Zhang Junbo Zhang
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title_sort	preparation and biological evaluation of [<sup<99m</sup<tc]tc-cngu as a psma-targeted radiotracer for the imaging of prostate cancer
callnumber	QD241-441
title_auth	Preparation and Biological Evaluation of [<sup<99m</sup<Tc]Tc-CNGU as a PSMA-Targeted Radiotracer for the Imaging of Prostate Cancer
abstract	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.
abstract_unstemmed	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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title_short	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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up_date	2024-07-03T16:35:21.289Z
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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. 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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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