Preliminary evaluation of [<sup>18</sup>F]AlF-NOTA-MAL-Cys<sup>39</sup>-exendin-4 in insulinoma with PET

Xu, Qing; Zhu, Chen; Xu, Yuping; Pan, Donghui; Liu, Ping; Yang, Ronghua; Wang, Lizhen; Chen, Fei; Sun, Xinchen; Luo, Songyuan; Yang, Min

doi:10.3109/1061186x.2015.1020808

Cited by 32 publications

(39 citation statements)

References 30 publications

(47 reference statements)

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“…No-carrier-added [ 18 F]fluoride was obtained from an in-house cyclotron (HM67, Sumitomo Heavy Industries, Ltd.) Analytic and preparative high-performance liquid chromatography (HPLC) were performed according to the previous literatures. 30,31…”

Section: Methodsmentioning

confidence: 99%

“…Cys-MZHER 2:342 were conjugated with MAL-NOTA under standard reaction conditions as previously described 30,31. Briefly, a solution of 6μmol Cys-MZHER 2:342 was mixed with 8μmol MAL-NOTA in 0.2N ammonium acetate solution.…”

Section: Methodsmentioning

confidence: 99%

“…NOTA-MAL-MZHER 2:342 was radiolabeled with 18 F following procedures 30,31 A solution of NOTA-MAL-MZHER 2:342 Affibody molecule (300μg, 38nmol) in sodium acetate buffer (20μL, pH4, 0.2M) was added to a solution of AlCl 3 (6μL, 2mM in sodium acetate buffer, pH4, 0.5M) and 18 F-fluoride (~3700MBq) in 100μl target water. This mixture was heated for 15min at 100℃.…”

Section: Methodsmentioning

confidence: 99%

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PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

Xu¹,

Bai²,

Huang³

et al. 2017

J. Cancer

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Background: Human epidermal growth factor receptor type 2 (HER2) is abundant in a wide variety of tumors and associated with the poor prognosis. Radiolabeled affibodies are potential candidates for detecting HER2-positive lesions. However, laborious multiple-step synthetic procedure and high abdomen background may hinder the widespread use. Herein, cysteinylated ZHER2:342 modified with a new hydrophilic linker (denoted as MZHER2:342) was designed and labeled using 18FAl-NOTA strategies. The biologic efficacy of the novel tracer and its feasibilities for in vivo monitoring HER2 levels were also investigated in xenograft models with different HER2 expressions.Method: MZHER2:342 was conjugated with MAL-NOTA under standard reaction conditions. The affibody molecule was then radiolabeled with 18FAl complex. The binding specificity of the tracer, 18FAl-NOTA-MAL-MZHER2:342, with HER2 was primarily characterized via in vitro studies. MicroPET imaging were performed in nude mice bearing tumors (SKOV-3, JIMT-1 and MCF-7) after injection. The HER2 levels of xenografts were determined using Western blotting analysis.Results: 18FAl-NOTA-MAL-MZHER2:342 can be efficiently produced within 30 min with a non-decaycorrected yield of about 10% and a radiochemical purity of more than 95%. In vitro experiments revealed that the modified affibody retained the specific affinity to HER2. PET imaging showed that SKOV-3 and JIMT-1 xenografts were clearly visualized with excellent contrast and low abdomen backgrounds. On the contrary, the signals of MCF-7 tumor were difficult to visualize. The ROI values ranged from16.54±2.69% ID/g for SKOV-3 to 8.42±1.20 %ID/g for JIMT-1 tumors at 1h postinjection respectively. Poor uptake was observed from MCF-7 tumors with 1.71±0.34% ID/g at the same time point. Besides, a significant linear correlation between % ID/g values and relative HER2 expression levels was also found.Conclusions: 18FAl-NOTA-MAL-MZHER2:342 is a promising tracer for in vivo detecting HER2 status with the advantages of facile synthesis and favorable pharmacokinetics. It may be useful in differential diagnosis, molecularly targeted therapy and prognosis of the cancers.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

Xu¹,

Bai²,

Huang³

et al. 2017

J. Cancer

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“…Despite the encouraging results, the tedious radiosynthesis would hinder the tracer to widespread use. Recently, a one-step simple procedure for preparing 18 F-labeled peptides via chelating 18 FAl with NOTA has been reported [84] . Xu et al [84] conjugated Cys 39 -exendin-4 with NOTA-MAL and obtained NOTA-MALCys 39 -exendin-4.…”

mentioning

confidence: 99%

“…Recently, a one-step simple procedure for preparing 18 F-labeled peptides via chelating 18 FAl with NOTA has been reported [84] . Xu et al [84] conjugated Cys 39 -exendin-4 with NOTA-MAL and obtained NOTA-MALCys 39 -exendin-4. The compound was simply radiolabeled with 18 FAl complex by one step in 30 min [85] .…”

mentioning

confidence: 99%

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

Xu¹

2016

WJGO

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Pancreatic cancer (PC) is a major health problem. Conventional imaging modalities show limited accuracy for reliable assessment of the tumor. Recent researches suggest that molecular imaging techniques with tracers provide more biologically relevant information and are benefit for the diagnosis of the cancer. In addition, radiopharmaceuticals also play more important roles in treatment of the disease. This review summaries the advancement of the radiolabeled compounds in the theranostics of PC.

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Multivalent γ‐PGA‐Exendin‐4 Conjugates to Target Pancreatic β‐Cells

Rossi

Kerekes²,

Kovács-Kocsi³

et al. 2022

ChemBioChem

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Targeting of glucagon-like peptide 1 receptor (GLP-1R), expressed on the surface of pancreatic β-cells, is of great interest for the development of advanced therapies for diabetes and diagnostics for insulinoma. We report the conjugation of exendin-4 (Ex-4), an approved drug to treat type 2 diabetes, to poly-γ-glutamic acid (γ-PGA) to obtain more stable and effective GLP-1R ligands. Exendin-4 modified at Lysine-27 with PEG4-maleimide was conjugated to γ-PGA functionalized with furan, in different molar ratios, exploiting a chemoselective Diels-Alder cycloaddition. The γ-PGA presenting the highest number of conjugated Ex-4 molecules (average 120 per polymeric chain) showed a double affinity towards GLP-1R with respect to exendin per se, paving the way to improved therapeutic and diagnostic applications.

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Preliminary evaluation of [¹⁸F]AlF-NOTA-MAL-Cys³⁹-exendin-4 in insulinoma with PET

Abstract: [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4 shows favorable characteristics for insulinoma imaging and may be translated to clinical studies.

Cited by 32 publications

References 30 publications

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

Multivalent γ‐PGA‐Exendin‐4 Conjugates to Target Pancreatic β‐Cells

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Preliminary evaluation of [18F]AlF-NOTA-MAL-Cys39-exendin-4 in insulinoma with PET

Abstract: [(18)F]AlF-NOTA-MAL-Cys(39)-exendin-4 shows favorable characteristics for insulinoma imaging and may be translated to clinical studies.

Cited by 32 publications

References 30 publications

PET of HER2 Expression with a Novel 18FAl Labeled Affibody

PET of HER2 Expression with a Novel 18FAl Labeled Affibody

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

Multivalent γ‐PGA‐Exendin‐4 Conjugates to Target Pancreatic β‐Cells

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Product

Resources

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Preliminary evaluation of [¹⁸F]AlF-NOTA-MAL-Cys³⁹-exendin-4 in insulinoma with PET

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody