The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice

Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<s...
Ausführliche Beschreibung

Gespeichert in:

Autor*in:	Yiding Zhang [verfasserIn] Katsushi Kumata [verfasserIn] Lin Xie [verfasserIn] Yusuke Kurihara [verfasserIn] Masanao Ogawa [verfasserIn] Tomomi Kokufuta [verfasserIn] Nobuki Nengaki [verfasserIn] Ming-Rong Zhang [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2023

Schlagwörter:	[ PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [

Übergeordnetes Werk:	In: Pharmaceuticals - MDPI AG, 2005, 16(2023), 7, p 963
Übergeordnetes Werk:	volume:16 ; year:2023 ; number:7, p 963

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/ph16070963

Katalog-ID:	DOAJ09384431X

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520			\|a Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice.
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allfields	10.3390/ph16070963 doi (DE-627)DOAJ09384431X (DE-599)DOAJ19e9d20f8c2740e48bc14481b8ce8245 DE-627 ger DE-627 rakwb eng RS1-441 Yiding Zhang verfasserin aut The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica Katsushi Kumata verfasserin aut Lin Xie verfasserin aut Yusuke Kurihara verfasserin aut Masanao Ogawa verfasserin aut Tomomi Kokufuta verfasserin aut Nobuki Nengaki verfasserin aut Ming-Rong Zhang verfasserin aut In Pharmaceuticals MDPI AG, 2005 16(2023), 7, p 963 (DE-627)491437528 (DE-600)2193542-7 14248247 nnns volume:16 year:2023 number:7, p 963 https://doi.org/10.3390/ph16070963 kostenfrei https://doaj.org/article/19e9d20f8c2740e48bc14481b8ce8245 kostenfrei https://www.mdpi.com/1424-8247/16/7/963 kostenfrei https://doaj.org/toc/1424-8247 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_73 GBV_ILN_74 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_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 16 2023 7, p 963
spelling	10.3390/ph16070963 doi (DE-627)DOAJ09384431X (DE-599)DOAJ19e9d20f8c2740e48bc14481b8ce8245 DE-627 ger DE-627 rakwb eng RS1-441 Yiding Zhang verfasserin aut The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica Katsushi Kumata verfasserin aut Lin Xie verfasserin aut Yusuke Kurihara verfasserin aut Masanao Ogawa verfasserin aut Tomomi Kokufuta verfasserin aut Nobuki Nengaki verfasserin aut Ming-Rong Zhang verfasserin aut In Pharmaceuticals MDPI AG, 2005 16(2023), 7, p 963 (DE-627)491437528 (DE-600)2193542-7 14248247 nnns volume:16 year:2023 number:7, p 963 https://doi.org/10.3390/ph16070963 kostenfrei https://doaj.org/article/19e9d20f8c2740e48bc14481b8ce8245 kostenfrei https://www.mdpi.com/1424-8247/16/7/963 kostenfrei https://doaj.org/toc/1424-8247 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_73 GBV_ILN_74 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_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 16 2023 7, p 963
allfields_unstemmed	10.3390/ph16070963 doi (DE-627)DOAJ09384431X (DE-599)DOAJ19e9d20f8c2740e48bc14481b8ce8245 DE-627 ger DE-627 rakwb eng RS1-441 Yiding Zhang verfasserin aut The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica Katsushi Kumata verfasserin aut Lin Xie verfasserin aut Yusuke Kurihara verfasserin aut Masanao Ogawa verfasserin aut Tomomi Kokufuta verfasserin aut Nobuki Nengaki verfasserin aut Ming-Rong Zhang verfasserin aut In Pharmaceuticals MDPI AG, 2005 16(2023), 7, p 963 (DE-627)491437528 (DE-600)2193542-7 14248247 nnns volume:16 year:2023 number:7, p 963 https://doi.org/10.3390/ph16070963 kostenfrei https://doaj.org/article/19e9d20f8c2740e48bc14481b8ce8245 kostenfrei https://www.mdpi.com/1424-8247/16/7/963 kostenfrei https://doaj.org/toc/1424-8247 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_73 GBV_ILN_74 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_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 16 2023 7, p 963
allfieldsGer	10.3390/ph16070963 doi (DE-627)DOAJ09384431X (DE-599)DOAJ19e9d20f8c2740e48bc14481b8ce8245 DE-627 ger DE-627 rakwb eng RS1-441 Yiding Zhang verfasserin aut The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica Katsushi Kumata verfasserin aut Lin Xie verfasserin aut Yusuke Kurihara verfasserin aut Masanao Ogawa verfasserin aut Tomomi Kokufuta verfasserin aut Nobuki Nengaki verfasserin aut Ming-Rong Zhang verfasserin aut In Pharmaceuticals MDPI AG, 2005 16(2023), 7, p 963 (DE-627)491437528 (DE-600)2193542-7 14248247 nnns volume:16 year:2023 number:7, p 963 https://doi.org/10.3390/ph16070963 kostenfrei https://doaj.org/article/19e9d20f8c2740e48bc14481b8ce8245 kostenfrei https://www.mdpi.com/1424-8247/16/7/963 kostenfrei https://doaj.org/toc/1424-8247 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_73 GBV_ILN_74 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_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 16 2023 7, p 963
allfieldsSound	10.3390/ph16070963 doi (DE-627)DOAJ09384431X (DE-599)DOAJ19e9d20f8c2740e48bc14481b8ce8245 DE-627 ger DE-627 rakwb eng RS1-441 Yiding Zhang verfasserin aut The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice 2023 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice. [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica Katsushi Kumata verfasserin aut Lin Xie verfasserin aut Yusuke Kurihara verfasserin aut Masanao Ogawa verfasserin aut Tomomi Kokufuta verfasserin aut Nobuki Nengaki verfasserin aut Ming-Rong Zhang verfasserin aut In Pharmaceuticals MDPI AG, 2005 16(2023), 7, p 963 (DE-627)491437528 (DE-600)2193542-7 14248247 nnns volume:16 year:2023 number:7, p 963 https://doi.org/10.3390/ph16070963 kostenfrei https://doaj.org/article/19e9d20f8c2740e48bc14481b8ce8245 kostenfrei https://www.mdpi.com/1424-8247/16/7/963 kostenfrei https://doaj.org/toc/1424-8247 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_73 GBV_ILN_74 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_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 16 2023 7, p 963
language	English
source	In Pharmaceuticals 16(2023), 7, p 963 volume:16 year:2023 number:7, p 963
sourceStr	In Pharmaceuticals 16(2023), 7, p 963 volume:16 year:2023 number:7, p 963
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topic_facet	[<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation Medicine R Pharmacy and materia medica
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callnumber-first	R - Medicine
author	Yiding Zhang
spellingShingle	Yiding Zhang misc RS1-441 misc [<sup<11</sup<C-carbonyl]BPTES misc PET misc glutaminase-1 (GLS1) misc glutaminase-1 inhibitor misc senescence misc [<sup<11</sup<C]acylation misc Medicine misc R misc Pharmacy and materia medica The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice
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topic_title	RS1-441 The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice [<sup<11</sup<C-carbonyl]BPTES PET glutaminase-1 (GLS1) glutaminase-1 inhibitor senescence [<sup<11</sup<C]acylation
topic	misc RS1-441 misc [<sup<11</sup<C-carbonyl]BPTES misc PET misc glutaminase-1 (GLS1) misc glutaminase-1 inhibitor misc senescence misc [<sup<11</sup<C]acylation misc Medicine misc R misc Pharmacy and materia medica
topic_unstemmed	misc RS1-441 misc [<sup<11</sup<C-carbonyl]BPTES misc PET misc glutaminase-1 (GLS1) misc glutaminase-1 inhibitor misc senescence misc [<sup<11</sup<C]acylation misc Medicine misc R misc Pharmacy and materia medica
topic_browse	misc RS1-441 misc [<sup<11</sup<C-carbonyl]BPTES misc PET misc glutaminase-1 (GLS1) misc glutaminase-1 inhibitor misc senescence misc [<sup<11</sup<C]acylation misc Medicine misc R misc Pharmacy and materia medica
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title	The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice
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title_full	The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice
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title_sort	glutaminase-1 inhibitor [<sup<11</sup<c-carbony]bptes: synthesis and positron emission tomography study in mice
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title_auth	The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice
abstract	Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice.
abstractGer	Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice.
abstract_unstemmed	Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [<sup<11</sup<C-carbonyl]BPTES ([<sup<11</sup<C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [<sup<11</sup<C]BPTES was synthesized by the reaction of an amine precursor () with [<sup<11</sup<C-carbonyl]phenylacetyl acid anhydride ([<sup<11</sup<C]<b<2</b<), which was prepared from [<sup<11</sup<C]CO<sub<2</sub< and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [<sup<11</sup<C]BPTES was 9.5% (based on [<sup<11</sup<C]CO<sub<2</sub<) during a synthesis time of 40 min. A PET study with [<sup<11</sup<C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice.
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title_short	The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice
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The Glutaminase-1 Inhibitor [<sup<11</sup<C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice

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