Pilot Study of a Novel 18F-labeled FSHR Probe for Tumor Imaging

Xu, Yuping; Pan, Donghui; Zhu, Chen; Xu, Qing; Wang, Lizhen; Chen, Fei; Yang, Ronghua; Luo, Songyuan; Yang, Min; Yan, Yongjun

doi:10.1007/s11307-013-0712-1

Cited by 32 publications

(65 citation statements)

References 26 publications

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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%

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%

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

Xu¹,

Bai²,

Huang³

et al. 2017

J. Cancer

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“…In the previous study, NOTA-MAL-FSH was designed and labeled with 18 F. 18 F-Al-NOTA-MAL-FSH was preliminarily evaluated in FSHR-positive PC3 prostate tumor by microPET image. Interrelated analyses concluded that the 18 F-Al-NOTA-MAL-FSH 33-53 had fast clearance rate, high specificity, excellent tissue penetration, and low immunogenicity, and may be a suitable radiotracer for the non-invasive visualization of FSHR positive tumor in vivo [24]. Based on these results, FSH 33-53 was used to connect Lytic peptide.…”

Section: Discussionmentioning

confidence: 99%

“…Preparation of NOTA-MAL-FSH 33-53 -Lytic FSH 33-53 -Lytic was conjugated with NOTA-MAL as described previously [24]. Briefly, a solution of 6 lmol FSH 33-53 -Lytic was mixed with 8 lmol NOTA-MAL in 0.2 M ammonium acetate solution.…”

Section: Methodsmentioning

confidence: 99%

“…FSH peptide has high affinity to FSHR [22,23]. Xu, et al [24,25], prepared new positron emission tomography (PET) probes such as 18 F-Al-NOTA-MAL-FSH 33-53 and 68 Ga-Al-NOTA-MAL-FSH , then evaluated the imaging performance in PC3 human prostate tumor xenograft by microPET image. Both these tracers had specific FSHR targeting,which was important for accurately diagnose of prostate cancer.…”

Section: Introductionmentioning

confidence: 99%

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An investigation on the anti-tumor properties of FSH33-53-Lytic

Liu

Yang

Pan

et al. 2015

J Radioanal Nucl Chem

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A new designed hybrid peptide FSH 33-53 -Lytic was synthesized and expected to combine the follicle stimulating hormone receptor (FSHR) targeting and tumor cell membranes disintegration. Through in vitro and vivo study, no significant enhancement on anti-tumor activity was shown compared with Lytic peptide only. We also prepared 18 F-Al-NOTA-MAL-FSH 33-53 -Lytic and use microPET image to observe the FSHR targeting of FSH 33-53 -Lytic. No accumulation in the tumor may explain the failure of FSH 33-53 -Lytic on cancer therapy. In summary, microPET image can provide more accurate and visible information for screening new anti-tumor agents.

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“…Radiolabelled receptor-binding peptides have become important radiopharmaceuticals for diagnosis and therapy in tumor [57][58][59][60][61] .…”

Section: Radiolabeled Peptides For Pc Imagingmentioning

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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Pilot Study of a Novel 18F-labeled FSHR Probe for Tumor Imaging

Abstract: NOTA-MAL-FSH1 could be labeled rapidly and efficiently with (18)F using one step method. Favorable preclinical data suggest that (18)F-Al-NOTA-MAL-FSH1 may be a suitable radiotracer for the non-invasive visualization of FSHR positive tumor in vivo.

Cited by 32 publications

References 26 publications

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

An investigation on the anti-tumor properties of FSH33-53-Lytic

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

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Pilot Study of a Novel 18F-labeled FSHR Probe for Tumor Imaging

Abstract: NOTA-MAL-FSH1 could be labeled rapidly and efficiently with (18)F using one step method. Favorable preclinical data suggest that (18)F-Al-NOTA-MAL-FSH1 may be a suitable radiotracer for the non-invasive visualization of FSHR positive tumor in vivo.

Cited by 32 publications

References 26 publications

PET of HER2 Expression with a Novel 18FAl Labeled Affibody

PET of HER2 Expression with a Novel 18FAl Labeled Affibody

An investigation on the anti-tumor properties of FSH33-53-Lytic

Advancement in treatment and diagnosis of pancreatic cancer with radiopharmaceuticals

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Product

Resources

About

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody

PET of HER2 Expression with a Novel ¹⁸FAl Labeled Affibody