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Titolo:
Synthesis and evaluation of F-18-labeled choline as an oncologic tracer for positron emission tomography: Initial findings in prostate cancer
Autore:
DeGrado, TR; Coleman, RE; Wang, SY; Baldwin, SW; Orr, MD; Robertson, CN; Polascik, TJ; Price, DT;
Indirizzi:
Duke Univ, Med Ctr, Dept Radiol, Durham, NC 27710 USA Duke Univ Durham NCUSA 27710 Med Ctr, Dept Radiol, Durham, NC 27710 USA Duke Univ, Med Ctr, Dept Surg, Durham, NC 27710 USA Duke Univ Durham NC USA 27710 v, Med Ctr, Dept Surg, Durham, NC 27710 USA Duke Univ, Dept Chem, Durham, NC 27708 USA Duke Univ Durham NC USA 27708Duke Univ, Dept Chem, Durham, NC 27708 USA
Titolo Testata:
CANCER RESEARCH
fascicolo: 1, volume: 61, anno: 2001,
pagine: 110 - 117
SICI:
0008-5472(20010101)61:1<110:SAEOFC>2.0.ZU;2-S
Fonte:
ISI
Lingua:
ENG
Soggetto:
MAGNETIC-RESONANCE SPECTROSCOPY; BRAIN-TUMORS; KINASE-ACTIVITY; C-11 CHOLINE; SRC-FAMILY; FDG-PET; METABOLISM; PROTEIN; ACETYLCHOLINE; ACTIVATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
46
Recensione:
Indirizzi per estratti:
Indirizzo: DeGrado, TR Duke Univ, Med Ctr, Dept Radiol, Box 3949, Durham, NC 27710 USA Duke Univ Box 3949 Durham NC USA 27710 9, Durham, NC 27710 USA
Citazione:
T.R. DeGrado et al., "Synthesis and evaluation of F-18-labeled choline as an oncologic tracer for positron emission tomography: Initial findings in prostate cancer", CANCER RES, 61(1), 2001, pp. 110-117

Abstract

The up-regulation of rates of choline uptake and phosphorylation in certain malignancies has motivated the development of positron-labeled choline analogues for noninvasive detection of cancer using positron emission tomography (PET). The choline analogue, no-carrier-added [F-18]fluoromethyl-dimethyl-2-hydroxyethyl (FCH), was synthesized through the intermediate [F-18]fluorobromomethane. FCH was evaluated in relationship to 2-[F-18]fluoro-2-deoxyglucose (FDG) as an oncological probe in cultured PC-3 human prostate cancer cells, a murine PC-3 human prostate cancer xenograft model, and in PET imaging studies of patients with prostate cancer. FCH was synthesized in 20-40% radiochemical yield and >98% radiochemical purity. Accumulation of FCH and FDG were comparable in cultured prostate cancer cells, whereas only FCHwas inhibited (90%) by hemicholinium-3, a specific inhibitor of choline transport and phosphorylation. FCH showed similar biodistribution to [C-14]choline in the tumor-bearing mouse, with prominent renal and hepatic uptake. Tumor uptake of FCH was similar to choline and FDG in the mouse model, although tumor:blood ratios were moderately higher for FCH. Initial PET imagingstudies in prostate cancer patients showed high uptake of FCH in advanced prostate carcinoma and detection of osseous and soft tissue metastases. FCHuptake by tumors was markedly reduced in patients rescanned during androgen deprivation therapy. It is concluded that FCH closely mimics choline uptake by normal tissues and prostate cancer neoplasms. FCH is potentially useful as a PET tracer for detection and localization of prostate cancer and monitoring effects of therapy.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 01:57:43