123/125I-labelled 2-iodo-L-phenylalanine and 2-iodo-D-phenylalanine: comparative uptake in various tumour types and biodistribution in mice

Kersemans, Veerle; Cornelissen, Bart; Kersemans, Ken; Bauwens, Matthias; Dierckx, Rudi; Spiegeleer, Bart De; Mertens, John; Slegers, Guido

doi:10.1007/s00259-005-0043-9

Cited by 27 publications

(20 citation statements)

References 10 publications

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“…[35] Some cancer cells such as C6 rat glioma, HeLa cervix carcinoma cells and R1M rhabdomyosarcoma have high expression of LAT1 but showed no upregulation of LAT2. [36, 37] In such cancer cells lack of expression of LAT2, FEP ([ 18 F] 2 ) might have advantage over FET ([ 18 F] 1 ). Further investigations are needed to identify the amino acid transport systems involved in the uptake process.…”

Section: Resultsmentioning

confidence: 99%

Synthesis, uptake mechanism characterization and biological evaluation of 18F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents

Wang

Qü

Lieberman

et al. 2011

Nuclear Medicine and Biology

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Introduction Amino acids based tracers represent a promising class of tumor metabolic imaging agents with successful clinical applications. Two new phenylalanine derivatives, p-(2-[18F]fluoroethyl)-L-phenylalanine (FEP, [18F]2) and p-(3-[18F]fluoropropyl)-L-phenylalanine (FPP, [18F]3) were synthesized and evaluated in comparison to clinically utilized O-(2-[18F]fluoroethyl)-L-tyrosine (FET, [18F]1). Methods FEP ([18F]2) and FPP ([18F]3) were successfully synthesized by a rapid and efficient two-step nucleophilic fluorination of tosylate precursors and deprotection reaction. In vitro cell uptake studies were carried out in 9L glioma cells. In vivo studies, 9L tumor xenografts were implanted in Fisher 344 rats. Results FEP ([18F]2) and FPP ([18F]3) could be efficiently labeled within 90 min with good enantiomeric purity (>95%), good yield (11–37%) and high specific activity (21–69 GBq/μmol). Cell uptake studies showed FEP had higher uptake than FPP as well as reference ligand FET ([18F]1). Uptake mechanism studies suggested that FEP is a selective substrate for system L and prefers its subtype LAT1. In vivo biodistribution studies demonstrated FEP had specific accumulation in tumor cells and tumor to background ratio reached 1.45 at 60 min. Small animal PET imaging studies showed FEP was comparable to FET for imaging rats bearing 9L tumor model. FEP had high uptake in 9L tumor compared to surrounding tissue and was quickly excreted through urinary tract. Conclusion Biological evaluations indicate that FEP ([18F]2) is a potential useful tracer for tumor imaging with PET.

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Section: Resultsmentioning

confidence: 99%

Synthesis, uptake mechanism characterization and biological evaluation of 18F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents

Wang

Qü

Lieberman

et al. 2011

Nuclear Medicine and Biology

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“…Studies in animal tumor models using the L-and [72,73]. Studies comparing radioiodinated 2-iodo-L-phenylalanine and 2-iodo-D-phenylalanine in tumorbearing animals demonstrated that the D-enantiomer uptake was lower than with the L-enantiomer in normal tissues but that the D-and L-enantiomer showed similar levels of tumor uptake [74]. Human studies with the D-and L-enantiomers of 2-iodo-phenylalanine also demonstrated lower uptake and faster clearance of the D-enantiomer [75].…”

Section: Amino Acid Transportmentioning

confidence: 98%

Non-natural amino acids for tumor imaging using positron emission tomography and single photon emission computed tomography

McConathy

Goodman

2008

Cancer Metastasis Rev

109

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Amino acids are required nutrients for proliferating tumor cells, and amino acid transport is upregulated in many tumor types. Studies of radiolabeled amino acids in animals and humans demonstrate that amino acid based tracers have advantageous characteristics relative to 2-[(18)F]fluoro-2-deoxyglucose in certain tumors, particularly brain gliomas. Non-natural amino acids for tumor imaging generally have greater metabolic stability and can be labeled with longer-lived radionuclides for positron emission tomography and single photon emission computed tomography such as fluorine-18 and iodine-123. Amino acids enter cells via amino acid transport with varying selectivity based on their chemical structure. This review focuses on the rationale, biological basis, current status and future prospects of radiolabeled non-natural amino acids for tumor imaging and discusses various classes of these compounds including aromatic, alicyclic and alpha,alpha-dialkyl amino acids.

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“…Decreasing these two metabolites may inhibit tumor growth [6]. Myo-inositol as a growth factor influenced the tumor growth rate.…”

Section: Page 13 Of 27mentioning

confidence: 99%

Turmeric enhancing anti-tumor effect of Rhizoma paridis saponins by influencing their metabolic profiling in tumors of H22 hepatocarcinoma mice

Man

Chai

Qiu

et al. 2015

Pathology - Research and Practice

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123/125I-labelled 2-iodo-L-phenylalanine and 2-iodo-D-phenylalanine: comparative uptake in various tumour types and biodistribution in mice

Cited by 27 publications

References 10 publications

Synthesis, uptake mechanism characterization and biological evaluation of 18F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents

Synthesis, uptake mechanism characterization and biological evaluation of 18F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents

Non-natural amino acids for tumor imaging using positron emission tomography and single photon emission computed tomography

Turmeric enhancing anti-tumor effect of Rhizoma paridis saponins by influencing their metabolic profiling in tumors of H22 hepatocarcinoma mice

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