Pharmacokinetics of 3-[125I]iodo-α-methyl-l-tyrosine, a tumor imaging agent, after probenecid loading in mice implanted with colon cancer DLD-1 cells

Nakajima, Syuichi; Shikano, Naoto; Kotani, Takashi; Ogura, Masato; Nishii, Ryuichi; Yoshimoto, Mitsuyoshi; Yamaguchi, Naoto; Iwamura, Yukio; Kubota, Nobuo; Ishikawa, Nobuyoshi; Kawai, Keiichi

doi:10.1016/j.nucmedbio.2007.06.017

Cited by 13 publications

(6 citation statements)

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“…The relative contributions of amino acid transport systems A, L, and, ASC/other to the uptake of [23] and Nakajima et al [24] and the results are shown in Table 1. Although the dominant uptake mechanism for [ 3 H]MET in human carcinomas was through system L amino acid transport, system A, ASC, or other Na + -dependent system(s) also played a role.…”

Section: Uptake Of [mentioning

confidence: 96%

“…BCH was used as a system L inhibitor and MeAIB was used as a system A inhibitor. To calculate the relative contributions of amino acid transporter systems, we used the methods reported by Shikano et al [23] and Nakajima et al [24]. In brief, uptake of mRNA levels of neutral amino acid transporters were determined by conducting qRT-PCR assays.…”

Section: C]met Has Been As Widely Used In Brain Tumor Imaging As O-(2mentioning

confidence: 99%

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Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Kagawa

Nishii

Higashi³

et al. 2017

Nuclear Medicine and Biology

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Results and Conclusion: [ 14 C]MeAIB uptake occurred principally via a Na + -dependent A type mechanism whereas [ 3 H]MET uptake, which occurred predominantly via a Na + -independent L type mechanism although other transporters were also utilized depending on cell type. There was no correlation between [ 3 H]MET uptake and total system L amino acid transporter (LAT) expression. In contrast, [ 14 C]MeAIB uptake strongly correlated with total system A amino acid transporter (SNAT) expression and proliferative activity in this preliminary study using four human carcinoma cell lines. Carcinoma proliferative activity also correlated with total SNAT expression.

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Section: Uptake Of [mentioning

confidence: 96%

Section: C]met Has Been As Widely Used In Brain Tumor Imaging As O-(2mentioning

confidence: 99%

Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Kagawa

Nishii

Higashi³

et al. 2017

Nuclear Medicine and Biology

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“…Since 2- 211 At-AAMP is excreted in urine in an intact form [ 13 ], preventing its renal uptake could increase and maintain its accumulation level in tumors by delaying clearance from the blood. A previous study demonstrated that preloading of probenecid, an organic anion transporter (OAT) inhibitor, markedly delayed the clearance of radioiodine-labeled α-methyltyrosine (IMT; Figure 1 a) from the blood and increased its accumulation in tumors by reducing renal uptake [ 15 ]. Considering the common target molecule (LAT1) and structural similarity between 2- 211 At-AAMP and IMT ( Figure 1 ), we speculated that the probenecid loading strategy should work on 2- 211 At-AAMP.…”

Section: Introductionmentioning

confidence: 99%

Enhancing the Therapeutic Effect of 2-211At-astato-α-methyl-L-phenylalanine with Probenecid Loading

Hanaoka

Ohshima

Suzuki

et al. 2021

Cancers

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L-type amino acid transporter 1 (LAT1) might be a useful target for tumor therapy since it is highly expressed in various types of cancers. We previously developed an astatine-211 (211At)-labeled amino acid derivative, 2-211At-astato-α-methyl-L-phenylalanine (2-211At-AAMP), and demonstrated its therapeutic potential for LAT1-positive cancers. However, the therapeutic effect of 2-211At-AAMP was insufficient, probably due to its low tumor retention. The preloading of probenecid, an organic anion transporter inhibitor, can delay the clearance of some amino acid tracers from the blood and consequently increase their accumulation in tumors. In this study, we evaluated the effect of probenecid preloading on the biodistribution and therapeutic effect of 2-211At-AAMP in mice. In biodistribution studies, the blood radioactivity of 2-211At-AAMP significantly increased with probenecid preloading. Consequently, the accumulation of 2-211At-AAMP in tumors was significantly higher with probenecid than without probenecid loading. In a therapeutic study, tumor growth was suppressed by 2-211At-AAMP with probenecid, and the tumor volume was significantly lower in the treatment group than in the untreated control group from day 2 to day 30 (end of the follow-up period) after treatment. These results indicate that probenecid loading could improve the therapeutic effect of 2-211At-AAMP by increasing its accumulation in tumors.

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“…Tumor cells exhibit increased amino acid metabolism . To exploit this property, many tumor‐targeting amino acid positron emission tomography (PET) tracers have been developed and evaluated . Some of these amino acid PET tracers have a ring structure.…”

Section: Introductionmentioning

confidence: 99%

“…Some of these amino acid PET tracers have a ring structure. For example, tyrosine‐based amino acid derivatives have a hexagonal ring structure . In addition, hydroxyproline derivatives have pentagonal rings, and cyclobutane derivatives have tetragonal rings.…”

Section: Introductionmentioning

confidence: 99%

Biological evaluation of new [¹⁸F]F‐labeled synthetic amino acid derivatives as oncologic radiotracers

Kim

Lee

Yook

et al. 2016

Labelled Comp Radiopharmac

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The present study evaluated the tumoral uptake of the novel synthetic amino acid positron emission tomography (PET) tracers (S)-2-amino-3-(4-([(18) F]fluoromethyl)-1H-1,2,3-triazol-1-yl)propanoic acid (AMC-101), (S)-2-amino-4-(4-([(18) F]fluoromethyl)-1H-1,2,3-triazol-1-yl)butanoic acid (AMC-102), and (S)-2-amino-5-(4-([(18) F]fluoromethyl)-1H-1,2,3-triazol-1-yl)pentanoic acid (AMC-103), all of which are (S)-2-amino-(4-([(18) F]fluoromethyl)-1H-1,2,3-triazol-1-yl)alkyl acids. In vitro cellular uptake was investigated using the rat glioma cell lines 9L and C6. In vitro competitive inhibition tests were performed to identify the involvement of specific amino acid transporters. In vivo dynamic PET images of 9L xenograft tumor-bearing model mice were acquired over 2 h after AMC administration. [(18) F]FDOPA PET studies were performed with and without S-carbidopa pretreatment for comparison. All three AMCs exhibited good in vitro cell uptake through the L and alanine-serine-cysteine transporters and enabled clear tumor visualization on PET, leaving the brain devoid of the tracer. Thirty minutes after injection, the mean tumor standardized uptake values were 1.59 ± 0.05, 1.89 ± 0.27, and 1.74 ± 0.13 for AMC-101, AMC-102, and AMC-103, respectively. Although the tumor uptake values of AMCs were lower than that of [(18) F]FDOPA with S-carbidopa pretreatment, AMCs enabled higher contrast images with lower background activity compared with [(18) F]FDOPA with S-carbidopa pretreatment. Our results indicate the potential uses of these new synthetic amino acids as oncologic radiotracers.

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Pharmacokinetics of 3-[125I]iodo-α-methyl-l-tyrosine, a tumor imaging agent, after probenecid loading in mice implanted with colon cancer DLD-1 cells

Cited by 13 publications

References 13 publications

Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Enhancing the Therapeutic Effect of 2-211At-astato-α-methyl-L-phenylalanine with Probenecid Loading

Biological evaluation of new [¹⁸F]F‐labeled synthetic amino acid derivatives as oncologic radiotracers

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Pharmacokinetics of 3-[125I]iodo-α-methyl-l-tyrosine, a tumor imaging agent, after probenecid loading in mice implanted with colon cancer DLD-1 cells

Cited by 13 publications

References 13 publications

Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Relationship between [ 14 C]MeAIB uptake and amino acid transporter family gene expression levels or proliferative activity in a pilot study in human carcinoma cells: Comparison with [ 3 H]methionine uptake

Enhancing the Therapeutic Effect of 2-211At-astato-α-methyl-L-phenylalanine with Probenecid Loading

Biological evaluation of new [18F]F‐labeled synthetic amino acid derivatives as oncologic radiotracers

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Biological evaluation of new [¹⁸F]F‐labeled synthetic amino acid derivatives as oncologic radiotracers