GRPR-targeted SPECT imaging using a novel bombesin-based peptide for colorectal cancer detection

Liu, Peifei; Tu, Yuanbiao; Ji, Tao; Liu, Zicun; Wang, Fang; Ma, Yi; Li, Zhaolun; Han, Zhihao; Gu, Yueqing

doi:10.1039/d0bm01432j

Cited by 11 publications

(8 citation statements)

References 31 publications

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“…To validate the results from the in vivo fluorescence imaging, we evaluated the capacity of radioactive conjugates for in vivo-targeted detection of HepG2 tumor using small animal SPECT-CT imaging. First, [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II was radiolabeled with [ 99m Tc ]NaTcO 4 as previously described. , Details of [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II are shown in Supporting Information. Radiochemical purity was >99%, with immediate specific activities >1.67 mCi/nmol after radiolabeling and a 18.7-min retention time for [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II (Figure S21).…”

Section: Resultsmentioning

confidence: 99%

“…First, [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II was radiolabeled with [ 99m Tc ]NaTcO 4 as previously described. 22,23 Details of [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II are shown in Supporting Information. Radiochemical purity was >99%, with immediate specific activities >1.67 mCi/nmol after radiolabeling and a 18.7-min retention time for [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II (Figure S21).…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…The radiosynthesis of [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II was done as we previously described. , The typical radio-HPLC chromatogram of [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II is shown in Figure S21. The lipophilicity of [ 99m Tc]Tc-HYNIC-PEG 4 -Ang II was evaluated by previously described …”

Section: Methodsmentioning

confidence: 99%

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AT1R-Specific Ligand Angiotensin II as a Novel SPECT Agent for Hepatocellular Carcinoma Diagnosis

Liu

Wang

et al. 2020

ACS Sens.

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Hepatocellular carcinoma (HCC) is characterized by a high mortality and early diagnosis and treatment are critically needed. Ang II type 1 receptor (AT1R) has recently emerged as a potential molecular target for cancer diagnosis and intervention. Here, we labeled angiotensin II (Ang II), an AT1R ligand that is overexpressed in various solid cancers, with the near-infrared fluorescent dye, MPA, and radionuclide technetium-99m, and evaluated its capacity for HCC detection. These analyses were done in vitro using HepG2 (AT1R-positive) and BxPC3 (AT1R-negative) cell lines, and in vivo using a subcutaneous and orthotopic xenograft mouse model by fluorescence and SPECT imaging. Both Ang II-PEG4-MPA- and [99mTc]Tc-HYNIC-PEG4-Ang II-bound AT1R exhibited a high affinity in vitro and [99mTc]Tc-HYNIC-PEG4-Ang II displayed an acceptable level of in vitro stability in rat plasma and whole blood. In vivo imaging revealed excellent specific tumor-targeting in HepG2 mouse xenografts models. In vitro and in vivo competition experiments revealed specific Ang II-PEG4-MPA and [99mTc]Tc-HYNIC-PEG4-Ang II uptake by HepG2 cells and tumors. Altogether, AT1R-positive tumors were successfully detected via fluorescence and SPECT imaging using Ang II-PEG4-MPA and [99mTc]Tc-HYNIC-PEG4-Ang II, respectively. Given their superior targeting capacity, Ang II-PEG4-MPA and [99mTc]Tc-HYNIC-PEG4-Ang II are promising tools for HCC detection and warrant clinical translation.

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Section: Resultsmentioning

confidence: 99%

Section: ■ Results and Discussionmentioning

confidence: 99%

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AT1R-Specific Ligand Angiotensin II as a Novel SPECT Agent for Hepatocellular Carcinoma Diagnosis

Liu

Wang

et al. 2020

ACS Sens.

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“…Bombesin shares a C-terminal amino acid sequence with GRPr’s native ligand, gastrin-releasing peptide, and is known to have a high affinity and specificity towards GRPr [ 83 , 84 , 88 ]. Therefore, bombesin derivatives have been labeled with applicable radionuclides for PET and SPECT imaging [ 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 ]. As with other SiFA peptides, the latest generation of analogues utilize polar auxiliaries to counterbalance the increase in lipophilicity [ 91 ].…”

Section: Peptidesmentioning

confidence: 99%

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

et al. 2021

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The incorporation of silicon fluoride acceptor (SiFA) moieties into a variety of molecules, such as peptides, proteins and biologically relevant small molecules, has improved the generation of 18F-radiopharmaceuticals for medical imaging. The efficient isotopic exchange radiofluorination process, in combination with the enhanced [18F]SiFA in vivo stability, make it a suitable strategy for fluorine-18 incorporation. This review will highlight the clinical applicability of [18F]SiFA-labeled compounds and discuss the significant radiotracers currently in clinical use.

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“…Gastrin-releasing peptide receptor (GRPR) has been shown to be overexpressed on many tumors, such as human breast cancer, prostate cancer, colon cancer, and cervical cancer (32)(33)(34)(35)(36)(37). Lango et al demonstrated that GRPR is overexpressed in squamous cell carcinoma of the head and neck (HNSCC), and GRPR was further used as a biomarker for surgical margin prediction in a murine orthotopic model of oral cancer (38).…”

Section: Introductionmentioning

confidence: 99%

pH-responsive graphene oxide loaded with targeted peptide and anticancer drug for OSCC therapy

Gao

Zhao

et al. 2022

Front. Oncol.

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Oral squamous cell carcinoma (OSCC) is the most common type of cancer occurring in the oral and maxillofacial regions. Despite of the advances in the diagnosis and treatment, the overall 5-year survival rate has remained about 40%–50% in the past decades. Various nanotechnology-based carrier systems have been investigated for their potentials in the OSCC treatment. However, because of the lack of active targeting of tumors, their application is limited. Studies have shown that gastrin-releasing peptide receptors (GRPRs) are overexpressed on many human cancers, including head and neck squamous cell carcinoma. Herein, we aimed to develop a GRPR-targeted nano-graphene oxide (NGO) nanoprobe drug delivery system for OSCC therapy. DOX@NGO-BBN-AF750 was synthesized by the non-covalent bonding method to couple carboxylated NGO with BBN-AF750 (bombesin antagonist peptides conjugated to Alexa Fluor 750) and DOX (doxorubicin) through π-π and hydrogen bonding. Internalization and antitumor activities were carried out in human HSC-3 cancer cells. The tumor pH microenvironment was simulated to study the release of antitumor drug DOX from the DOX@NGO-ant BBN-AF750 complex under different pH conditions. DOX@NGO-BBN-AF750 showed internalization into HSC-3 cells. The IC50 (50% inhibitory concentration) was 5 µg/ml for DOX@NGO-BBN-AF750 in HSC-3 cells. Furthermore, DOX@NGO-BBN-AF750 showed a pH-sensitive drug release rate, and a dose-dependent and pH-responsive cytotoxicity in HSC-3 cells. DOX@NGO-BBN-AF750 presents the characteristics ensuring a slow release of DOX from the nanoprobe, thereby protecting the drug from degradation and prolonging the half-life of the drug. This report provides a versatile strategy to achieving targeted and imaging-guided therapy of OSCC.

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GRPR-targeted SPECT imaging using a novel bombesin-based peptide for colorectal cancer detection

Abstract: Colorectal cancer (CRC) is the third most common cancer worldwide, and the prognosis of CRC is better with an earlier diagnosis. The presence of the gastrin-releasing peptide receptor (GRPR) has...

Cited by 11 publications

References 31 publications

AT1R-Specific Ligand Angiotensin II as a Novel SPECT Agent for Hepatocellular Carcinoma Diagnosis

AT1R-Specific Ligand Angiotensin II as a Novel SPECT Agent for Hepatocellular Carcinoma Diagnosis

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

pH-responsive graphene oxide loaded with targeted peptide and anticancer drug for OSCC therapy

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