The potential use of the neurotensin high affinity receptor 1 as a biomarker for cancer progression and as a component of personalized medicine in selective cancers

Dupouy, Sandra; Mourra, Najat; Doan, Van Kien; Gompel, Anne; Alifano, Marco; Forgez, Patricia

doi:10.1016/j.biochi.2011.04.024

Cited by 80 publications

(96 citation statements)

References 105 publications

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“…Accumulating evidence suggests that NTRs play key roles in cancer growth and survival (20,23,24). In fact, NTRs have been proposed as a promising marker for human pancreatic carcinoma (25), breast cancer (26), head and neck carcinoma (27), prostate cancer (28), and non-small cell lung cancer (29).…”

Section: Discussionmentioning

confidence: 99%

Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Liu

et al. 2014

J Nucl Med

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Accumulating evidence suggests that neurotensin receptors (NTRs) play key roles in cancer growth and survival. In this study, we developed a simple and efficient method to radiolabel neurotensin peptide with 18 F for NTR-targeted imaging. Methods: The thiolreactive reagent 18 F-(2-(2-(2-fluoroethoxy)ethoxy)ethylsulfonyl)ethane ( 18 F-DEG-VS) was facilely prepared through 1-step radiofluorination. After high-pressure liquid chromatography purification, 18 F-DEG-VS was incubated with the c(RGDyC) and c(RGDyK) peptide mixture to evaluate its specificity toward the reactive thiol. Thiolated neurotensin peptide was then labeled with 18 F using this novel synthon, and the resulting imaging probe was subjected to receptor-binding assay and small-animal PET studies in a murine xenograft model. The imaging results and metabolic stability of 18 F-DEG-VS-NT were compared with the thiol-specific maleimide derivative N-[2-(4-18 F-fluorobenzamido) ethyl]maleimide-neurotensin ( 18 F-FBEM-NT). Results: 18 F-DEG-VS was obtained in high labeling yield. The reaction of 19 F-DEG-VS was highly specific for thiols at neutral pH, whereas the lysine of c(RGDyK) reacted at a pH greater than 8.5. 18 F-DEG-VS-c(RGDyC) was the preferred product when both c(RGDyK) and c(RGDyC) were incubated together with 18 F-DEG-VS. Thiolated neurotensin peptide (Cys-NT) efficiently reacted with 18 F-DEG-VS, with a 95% labeling yield (decay-corrected). The radiochemical purity of the 18 F-DEG-VS-NT was greater than 98%, and the specific activity was about 19.2 ± 4.3 TBq/mmol. Noninvasive small-animal PET demonstrated that 18 F-DEG-VS-NT had an NTR-specific tumor uptake in subcutaneous HT-29 xenografts. The tumor-to-muscle, tumor-to-liver, and tumor-to-kidney ratios reached 30.65 ± 22.31, 11.86 ± 1.98, and 1.91 ± 0.43 at 2 h after injection, respectively, based on the biodistribution study. Receptor specificity was demonstrated by blocking experiment. Compared with 18 F-FBEM-NT, 18 F-DEG-VS-NT was synthesized with fewer steps and provided significantly improved imaging quality in vivo. Conclusion: We have established a facile 18 F-labeling method for site-specific labeling of the Cys-NT. Using this method, we synthesized an NTR-targeted PET agent, which demonstrated high tumor-to-background contrast.

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Section: Discussionmentioning

confidence: 99%

Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Liu

et al. 2014

J Nucl Med

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“…The NTR subtype 1 (NTR1) has been associated with several oncogenic effects such as proliferation, survival, migration, invasion, and neoangiogenesis (3,4) and has been demonstrated to be overexpressed, inter alia, in ductal pancreatic cancer, Ewing's sarcoma, and small cell lung cancer (1). Hence, NTR1 imaging might be a promising tool for tumor diagnosis and staging.…”

mentioning

confidence: 99%

Comparative Evaluation of the Biodistribution Profiles of a Series of Nonpeptidic Neurotensin Receptor-1 Antagonists Reveals a Promising Candidate for Theranostic Applications

et al. 2016

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“…Neurotensin and neurotensin receptor 1 have been identified as factors promoting tumor growth and cancer metastasis. 107 The selective neurotensin receptor 1 (NTR-1) antagonist sensitized prostate cancer cells to radiation therapy. 108 Functionalization with neurotensin peptides significantly improved the ability of liposomes to deliver chemotherapeutics into CRC cells and resulted in a four fold increase in cytotoxicity.…”

Section: Active Targeting Liposomesmentioning

confidence: 99%

Application of liposomes in drug development – focus on gastroenterological targets

Zhang¹,

Wang²,

Mao³

et al. 2013

IJN

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Over the past decade, liposomes became a focal point in developing drug delivery systems. New liposomes, with novel lipid molecules or conjugates, and new formulations opened possibilities for safely and efficiently treating many diseases including cancers. New types of liposomes can prolong circulation time or specifically deliver drugs to therapeutic targets. This article concentrates on current developments in liposome based drug delivery systems for treating diseases of the gastrointestinal tract. We will review different types and uses of liposomes in the development of therapeutics for gastrointestinal diseases including inflammatory bowel diseases and colorectal cancer.

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The potential use of the neurotensin high affinity receptor 1 as a biomarker for cancer progression and as a component of personalized medicine in selective cancers

Cited by 80 publications

References 105 publications

Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Comparative Evaluation of the Biodistribution Profiles of a Series of Nonpeptidic Neurotensin Receptor-1 Antagonists Reveals a Promising Candidate for Theranostic Applications

Application of liposomes in drug development – focus on gastroenterological targets

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The potential use of the neurotensin high affinity receptor 1 as a biomarker for cancer progression and as a component of personalized medicine in selective cancers

Cited by 80 publications

References 105 publications

Facile Preparation of a Thiol-Reactive 18F-Labeling Agent and Synthesis of 18F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Facile Preparation of a Thiol-Reactive 18F-Labeling Agent and Synthesis of 18F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Comparative Evaluation of the Biodistribution Profiles of a Series of Nonpeptidic Neurotensin Receptor-1 Antagonists Reveals a Promising Candidate for Theranostic Applications

Application of liposomes in drug development &ndash; focus on gastroenterological targets

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Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Facile Preparation of a Thiol-Reactive ¹⁸F-Labeling Agent and Synthesis of ¹⁸F-DEG-VS-NT for PET Imaging of a Neurotensin Receptor–Positive Tumor

Application of liposomes in drug development – focus on gastroenterological targets