Carbon-11 labelled tyrosine to study tumor metabolism by positron emission tomography (PET)

Bolster, Jm; Vaalburg, W; Paans, Amj; Vandijk, Th; Elsinga, Philippus; Zijlstra, J.B.; Piers, Da; Mulder, Nanno; Woldring, Mg; Wynberg, Hans

doi:10.1007/bf00263811

Cited by 51 publications

(18 citation statements)

References 14 publications

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“…Radiochemically pure L-[1-11C]tyrosine was synthesized with a specific activity >3.7 GBq/gmol (100 Ci/mmol) (Bolster et al 1986). 18FDG was synthesized, no carrier added, with a radiochemical purity >98% (Hamacher etal.…”

Section: Methodsmentioning

confidence: 99%

PET studies with l-[1-11C]tyrosine, l-[methyl-11C]methionine and 18F-fluorodeoxyglucose in prolactinomas in relation to bromocryptine treatment

et al. 1991

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Aspects of metabolism in prolactinomas were investigated by positron emission tomography using L-[1-11C]tyrosine, L-[methyl-11C]methionine and 18F-fluorodeoxyglucose (18FDG). Using L-[1-11C]tyrosine, four patients were monitored prior to and 18 h after an injection of 50 mg bromocriptine. At 18 h after bromocriptine intervention, L-[1-11C]tyrosine uptake into tumour was reduced with 28% (P less than 0.07). A correlation analysis of the bromocriptine-induced decrease in L-[1-11C]tyrosine uptake and the reduction of serum prolactin levels indicated that the action of bromocriptine on prolactin synthesis and prolactin release is not coupled. In the untreated situation, the four patients were investigated with 18FDG as well, but the prolactinomas could not be visualized. Three untreated patients were studied with L-[methyl-11C]methionine. The tumour-imaging potential of L-[methyl-11C]methionine and L-[1-11C]tyrosine appeared to be nearly equivalent for prolactinomas. Unlike prolactinoma tissue, the salivary glands showed a pronounced preference for L-[1-11C]tyrosine as compared to L-[methyl-11C]methionine. L-[1-11C]tyrosine is a valuable tool to obtain information on the metabolism and treatment of prolactinomas.

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Section: Methodsmentioning

confidence: 99%

PET studies with l-[1-11C]tyrosine, l-[methyl-11C]methionine and 18F-fluorodeoxyglucose in prolactinomas in relation to bromocryptine treatment

et al. 1991

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“…Using this route, as described in Fig. 3a, a vast number of racemic [ 11 C]AAs have been described in literature, namely phenylalanine [26], ornithine and lysine [38], tyrosine [28,30], proline [39] and phenylglycine [26], and achiral glycine [25,26]. The [1][2][3][4][5][6][7][8][9][10][11] C]proline has been reported in 12-18 % RCY with a RCP of 9 95 % in total synthesis time of 45 min [39].…”

Section: Carbon-11 Amino Acid Labelingmentioning

confidence: 99%

“…On the other hand, C-11-labeled small peptides have received less attention until recently, where multiple independent papers described different methods for C-11 labeling of peptides, though clinical translation has thus far been inadequately examined [10,15,19]. With current achievements, the scope of C-11 labeling of peptides ranges from small proteins that have been successfully labeled with C-11 and used for applications such as blood flow permeability studies, as well as C-11-labeled peptides for inflammation and tumor imaging [25][26][27][28].…”

Section: Introductionmentioning

confidence: 99%

From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application

et al. 2018

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Radiolabeled amino acids, their derivatives and peptides have a broad scope of application and can be used as receptor ligands, as well as enzyme substrates for many different diseases as radiopharmaceutical tracers. Over the past few decades, the application of molecular imaging techniques such as positron emission tomography (PET) has gained considerable importance and significance in diagnosis in today's advanced health care. Next to that, the availability of cyclotrons and state-of-the-art radiochemistry facilities has progressed the production of imaging agents enabling the preparation of many versatile PET radiotracers. Due to many favorable characteristics of radiolabeled amino acids and peptides, they can be used for tumor staging and monitoring the progress of therapy success, while aromatic amino acids can be employed as PET tracer to study neurological disorders. This review provides a comprehensive overview of radiosynthetic and enzymatic approaches towards carbon-11 amino acids, their analogues and peptides, with focus on stereoselective reactions, and reflects upon their clinical application.

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“…The delineation of viable tumour extent has been demonstrated by several studies, using for example carbon-l l-labelled methionine (Bergstr6m et al 1983) and carbon-11-or fluorine-18-1abelled tyrosine (Bolster et al 1986;Wienhard et al 1991). Furthermore, experimental studies suggest the potential of such compounds to provide a rapid and sensitive indicator of response to therapy (Kubota et al 1991).…”

Section: Introductionmentioning

confidence: 99%

Uptake and distribution of L-3-[I-125] Iodo-?-methyl tyrosine in experimental rat tumours: comparison with blood flow and growth rate

et al. 1993

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Radiolabelled amino acids combined with positron emission tomography (PET) show promise for the accurate delineation of viable tumour extent and may also provide a rapid and sensitive indicator of response to therapy. We have investigated the potential use of the radioiodinated amino acid analogue L-3-iodo-alpha-methyl tyrosine (IMT) for these purposes using experimental tumours in hooded rats. Preliminary studies using HSN tumours and IMT labelled with iodine-125 demonstrated maximum tumour uptake at 15 min post injection although an improved tumour-to-brain ratio was seen at 24 h due to the relatively poor retention of IMT in normal brain. Brain uptake of IMT was also found to be substantially reduced by competition with another large neutral amino acid phenylalanine; however, relatively less effect was seen in tumour, and in skeletal muscle no change in IMT uptake was observed. Quantitative autoradiography revealed no sign of heterogeneity in tumour IMT uptake: good penetration was seen even in poorly vascularised regions as confirmed by endothelial immunohistochemistry. Similar levels of IMT uptake were found in the OES.HR1 tumour during growth supplemented by exogenous oestrogen. Following arrest of tumour growth by removal of the oestrogen stimulus, IMT uptake was seen to fall from 1.7% to 1.0% of the injected dose per gram: this was matched by a fall in tumour blood flow as estimated by technetium-99m hexamethylpropylene amine oxime distribution. It appears that IMT uptake is more strongly influenced by blood flow than cell proliferation and that intratumoural distribution of IMT is principally determined by diffusion.

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Carbon-11 labelled tyrosine to study tumor metabolism by positron emission tomography (PET)

Cited by 51 publications

References 14 publications

PET studies with l-[1-11C]tyrosine, l-[methyl-11C]methionine and 18F-fluorodeoxyglucose in prolactinomas in relation to bromocryptine treatment

PET studies with l-[1-11C]tyrosine, l-[methyl-11C]methionine and 18F-fluorodeoxyglucose in prolactinomas in relation to bromocryptine treatment

From Carbon-11-Labeled Amino Acids to Peptides in Positron Emission Tomography: the Synthesis and Clinical Application

Uptake and distribution of L-3-[I-125] Iodo-?-methyl tyrosine in experimental rat tumours: comparison with blood flow and growth rate

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