Radiofluorinated probe for PET imaging of fatty acid binding protein 4 in cancer

Temma, Takashi; Nishigori, Kantaro; Onoe, Satoru; Sampei, Sotaro; Kimura, Ikuo; Ono, Masahiro; Saji, Hideo

doi:10.1016/j.nucmedbio.2014.10.006

Cited by 5 publications

(4 citation statements)

References 18 publications

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“…Clinically, down-regulation of these proteins has been found in non-motile, abnormal headed, infertile spermatozoa [ 18 , 34 ]. Additionally, the functional affiliation of these proteins also has been reported to prostatic carcinoma and metastatic melanoma of the testis [ 35 , 36 ]. In contrast, the up-regulated proteins were peroxisomal membrane protein 20 (PMP20) and isoaspartyl peptidase/L-asparaginase (ASRGL1) (Table 1 ); interestingly, neither of them had been previously described in spermatozoa.…”

Section: Discussionmentioning

confidence: 99%

A novel approach to assessing bisphenol-A hazards using an in vitro model system

et al. 2016

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BackgroundAlthough the toxicological impacts of the xenoestrogen bisphenol-A (BPA) have been studied extensively, but the mechanism of action is poorly understood. Eventually, no standard method exists for evaluating the possible health hazards of BPA exposure. Considering mice spermatozoa as a potential in vitro model, we investigated the effects of BPA exposure (0.0001, 0.01, 1, and 100 μM for 6 h) on spermatozoa and the related mechanisms of action. The same doses were also employed to evaluate protein profiles of spermatozoa as a means to monitor their functional affiliation to diseases.ResultsOur results demonstrated that high concentrations of BPA negatively affect sperm motility, viability, mitochondrial functions, and intracellular ATP levels by activating the mitogen-activated protein kinase, phosphatidylinositol 3-kinase, and protein kinase-A pathways. Moreover, short-term exposure of spermatozoa to high concentrations of BPA induced differential expressions of 24 proteins. These effects appeared to be caused by protein degradation and phosphorylation in spermatozoa. Proteins differentially expressed in spermatozoa from BPA treatment groups are putatively involved in the pathogenesis of several diseases, mainly cancer, carcinoma, neoplasm, and infertility.ConclusionsBased on these results, we propose that BPA adversely affects sperm function by the activation of several kinase pathways in spermatozoa. In addition, BPA-induced changes in the sperm proteome might be partly responsible for the observed effects in spermatozoa, subsequently involve in the pathogenesis of many diseases. Therefore, we anticipated that current strategy might broadly consider for the health hazards assessment of other toxicological agents.Electronic supplementary materialThe online version of this article (doi:10.1186/s12864-016-2979-5) contains supplementary material, which is available to authorized users.

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Section: Discussionmentioning

confidence: 99%

A novel approach to assessing bisphenol-A hazards using an in vitro model system

et al. 2016

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“…It was found to be elevated at the boundary between tumor cells and CAAs. Temma et al [194] developed FABP4-targeting TAP1 and radiolabeled it with 125 I and 18 F for SPECT and PET imaging, respectively. [ 18 F]F-TAP1 showed a tumor uptake of 3.86 ± 0.39%ID/g, and an uptake in the blood of 10.38 ± 0.56%ID/g (3 h p.i.…”

Section: Cancer-associated Adipocytesmentioning

confidence: 99%

“…Partly due to the lack in (radio)biological understanding, most of the investigated TME-targeting radioligands are researched for imaging, and not (yet) for therapy. As Preclinical Preclinical [194][195][196] FASN Acetate Preclinical [198] inhibitors for identifying patients suitable for treatment with the corresponding PD1/PDL1 immune checkpoint inhibition therapy [200]. This multidisciplinary theranostic strategy allows for quick redirection and adjustment of treatment schedules when necessary, which is especially relevant for TME markers of which expression is highly variable between patients.…”

Section: Future Perspectives For Tme-targeting Radionuclide Intervent...mentioning

confidence: 99%

Radionuclide imaging and therapy directed towards the tumor microenvironment: a multi-cancer approach for personalized medicine

Heide

Dalm

2022

Eur J Nucl Med Mol Imaging

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Targeted radionuclide theranostics is becoming more and more prominent in clinical oncology. Currently, most nuclear medicine compounds researched for cancer theranostics are directed towards targets expressed in only a small subset of cancer types, limiting clinical applicability. The identification of cancer-specific targets that are (more) universally expressed will allow more cancer patients to benefit from these personalized nuclear medicine–based interventions. A tumor is not merely a collection of cancer cells, it also comprises supporting stromal cells embedded in an altered extracellular matrix (ECM), together forming the tumor microenvironment (TME). Since the TME is less genetically unstable than cancer cells, and TME phenotypes can be shared between cancer types, it offers targets that are more universally expressed. The TME is characterized by the presence of altered processes such as hypoxia, acidity, and increased metabolism. Next to the ECM, the TME consists of cancer-associated fibroblasts (CAFs), macrophages, endothelial cells forming the neo-vasculature, immune cells, and cancer-associated adipocytes (CAAs). Radioligands directed at the altered processes, the ECM, and the cellular components of the TME have been developed and evaluated in preclinical and clinical studies for targeted radionuclide imaging and/or therapy. In this review, we provide an overview of the TME targets and their corresponding radioligands. In addition, we discuss what developments are needed to further explore the TME as a target for radionuclide theranostics, with the hopes of stimulating the development of novel TME radioligands with multi-cancer, or in some cases even pan-cancer, application.

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“…PET imaging targeting lipid metabolism Several PET radiotracers targeting lipid synthesis [51,52], fatty acid binding [53], or fatty acid uptake [54] have been developed, although their implications in predicting or monitoring breast cancer therapeutic response still need more investigation. As an essential nutrient required for cellular methyl group metabolism, choline uptake reflects membrane lipid synthesis and the proliferation activity of cells.…”

Section: Open Accessmentioning

confidence: 99%

Integrating metabolic reprogramming and metabolic imaging to predict breast cancer therapeutic responses

Liu

Zhou

Song

2021

Trends in Endocrinology & Metabolism

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Metabolic reprogramming is not only an emerging hallmark of cancer, but also an essential regulator of cancer cell adaptation to the microenvironment. Metabolic imaging targeting metabolic signatures has been widely used for breast cancer diagnosis. However, limited implications have been explored for monitoring breast cancer therapy response, although metabolic plasticity is notably associated with therapy resistance. In this review, we focus on the metabolic alterations upon breast cancer therapy and their potential for evaluating breast cancer therapeutic responses. We summarize the metabolic network and regulatory changes upon breast cancer therapy in terms of cancer pathological and genetic differences and discuss the implications of metabolic imaging with various probes in selecting target beneficiaries for precision treatment. Key metabolic reprogramming of breast cancer in response to therapyReprogramming of glucose metabolism upon breast cancer therapy Drug-resistant breast cancer cells are able to reprogram glucose metabolism to adapt to the stress induced by drug treatment (Figure 1). For example, breast cancer cells resistant to lapatinib, a dual inhibitor of dermal growth factor receptor (EGFR) and HER2, recover the Highlights Reprogramming of metabolic pathways is pivotal for the adaptation and resistance to antitumor treatments in breast cancer.Metabolic changes upon treatment are superior to single timepoint metabolic signals in monitoring breast cancer therapeutic response.Cancer genetic and metabolic heterogeneity need to be fully integrated to precisely predict breast cancer response to different treatments.Metabolic imaging guided usage of anticancer drugs is critical for precise treatment in breast cancer.

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Radiofluorinated probe for PET imaging of fatty acid binding protein 4 in cancer

Abstract: [(18)F]FTAP1 is a promising PET probe to target FABP4.

Cited by 5 publications

References 18 publications

A novel approach to assessing bisphenol-A hazards using an in vitro model system

A novel approach to assessing bisphenol-A hazards using an in vitro model system

Radionuclide imaging and therapy directed towards the tumor microenvironment: a multi-cancer approach for personalized medicine

Integrating metabolic reprogramming and metabolic imaging to predict breast cancer therapeutic responses

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