Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography

To develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[ N -(3-aminopropyl)methacrylamide] [poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetonedimethylsulfoxide using N,N ‘-azobis(isobutyronitril...

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Main Authors: Jianchao Yuan, Yezi You, Xin Lu, Otto Muzik, David Oupicky, Fangyu Peng
Format: Article
Language:English
Published: SAGE Publishing 2007-01-01
Series:Molecular Imaging
Online Access:https://doi.org/10.2310/7290.2006.00030
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author Jianchao Yuan
Yezi You
Xin Lu
Otto Muzik
David Oupicky
Fangyu Peng
author_facet Jianchao Yuan
Yezi You
Xin Lu
Otto Muzik
David Oupicky
Fangyu Peng
author_sort Jianchao Yuan
collection DOAJ
description To develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[ N -(3-aminopropyl)methacrylamide] [poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetonedimethylsulfoxide using N,N ‘-azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering ( M n 5 2.40 × 10 4 , M w / M n = 1.87). Subsequently, poly[APMA] was coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as an activator, followed by conjugation with 64 Cu radionuclide. Prolonged retention of poly[APMA]-DOTA- 64 Cu conjugates within the tumor tissues was demonstrated by micro–positron emission tomography at 24 hours following intra-tumoral injection of the conjugates to human prostate xenografts in mice. The data suggest that the poly[APMA]-DOTA- 64 Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.
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spelling doaj-art-02e074b8cfa84664a887dce13ed4dd032025-01-02T22:37:02ZengSAGE PublishingMolecular Imaging1536-01212007-01-01610.2310/7290.2006.0003010.2310_7290.2006.00030Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission TomographyJianchao YuanYezi YouXin LuOtto MuzikDavid OupickyFangyu PengTo develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[ N -(3-aminopropyl)methacrylamide] [poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetonedimethylsulfoxide using N,N ‘-azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering ( M n 5 2.40 × 10 4 , M w / M n = 1.87). Subsequently, poly[APMA] was coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as an activator, followed by conjugation with 64 Cu radionuclide. Prolonged retention of poly[APMA]-DOTA- 64 Cu conjugates within the tumor tissues was demonstrated by micro–positron emission tomography at 24 hours following intra-tumoral injection of the conjugates to human prostate xenografts in mice. The data suggest that the poly[APMA]-DOTA- 64 Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.https://doi.org/10.2310/7290.2006.00030
spellingShingle Jianchao Yuan
Yezi You
Xin Lu
Otto Muzik
David Oupicky
Fangyu Peng
Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
Molecular Imaging
title Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
title_full Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
title_fullStr Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
title_full_unstemmed Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
title_short Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
title_sort synthesis of poly apma dota cu conjugates for interventional radionuclide therapy of prostate cancer assessment of intratumoral retention by micro positron emission tomography
url https://doi.org/10.2310/7290.2006.00030
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