Design and radio-synthesis of somatostatin receptors targeted 68Ga-DOTA-Benereotide for non-invasive PET imaging

Liu, Fei; Zhu, Hua; Li, Chuangui; Lin, Xinfeng; Xiong, Chiyi; Li, Chun; Liu, Yang

doi:10.1007/s10967-015-4241-z

Cited by 2 publications

(3 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…68 Ga-DOTA−PA1 was stable in PBS, NaOAc buffered solution (pH = 5.5), and 5% HSA for at least 2 h, according to previously reported procedures. 26 In Vitro Studies of 68 Ga-DOTA−PA1 in Cell Lines. The expression level of SSTR 1 , SSTR 2 , SSTR 3 , and SSTR 5 in human lung squamous carcinoma cell line (A549), human colorectal cancer cell lines (HT-29), human pulmonary giant cell carcinoma cell line (PG), and human gastric cancer cells (BGC823) was measured by Western blotting (Figure 1C and Figure S4), with β-actin protein as the internal standard.…”

Section: ■ Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Liu

et al. 2018

Mol. Pharmaceutics

Self Cite

View full text Add to dashboard Cite

Most of the radiolabeled somatostatin analogues (SSAs) are specific for subtype somatostatin receptor 2 (SSTR). Lack of ligands targeting other subtypes of SSTRs, especially SSTR SSTR, and SSTR, limited their applications in tumors of low SSTR expression, including lung tumor. In this study, we aimed to design and synthesize a positron emission tomography (PET) radiotracer targeting multi-subtypes of SSTRs for PET imaging. PA1 peptide and its conjugate with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator or fluorescein isothiocyanate (FITC) at the N-terminal of the lysine position were synthesized. Ga was chelated to DOTA-PA1 to obtainGa-DOTA-PA1 radiotracer. The stability, lipophilicity, binding affinity, and binding specificity of Ga-DOTA-PA1 and FITC-PA1 were evaluated by various in vitro experiments. Micro-PET imaging ofGa-DOTA-PA1 was performed in nude mice bearing A549 lung adenocarcinoma, as compared with Ga-DOTA-(Tyr3)-octreotate (Ga-DOTA-TATE). Histological analysis of SSTR expression in A549 tumor tissues and human tumor tissues was conducted using immunofluorescence staining and immunohistochemical assay. Ga-DOTA-PA1 had high radiochemical yield and radiochemical purity of over 95% and 99%, respectively. The radiotracer was stable in vitro in different buffers over a 2 h incubation period. Cell uptake ofGa-DOTA-PA1 was 1.31-, 1.33-, and 1.90-fold that of Ga-DOTA-TATE, which has high binding affinity only for SSTR, after 2 h incubation in H520, PG, and A549 lung cancer cell lines, respectively. Micro-PET images of Ga-DOTA-PA1 showed that the PET imaging signal correlated with the total expression of SSTRs, instead of SSTR only, which was measured by Western blotting and immunofluorescence analysis in mice bearing A549 tumors. In summary, a novel PET radiotracer, Ga-DOTA-PA1, targeting multi-subtypes of SSTRs, was successfully synthesized and was confirmed to be useful for PET imaging. It may have potential as a noninvasive PET radiotracer for imaging SSTR-positive tumors.

show abstract

Section: ■ Resultsmentioning

confidence: 99%

“…The log P value of 68 Ga-DOTA–PA1 was determined to be 0.18 ± 0.02, while that of 68 Ga-DOTA-TATE was −3.12 ± 0.16. 68 Ga-DOTA–PA1 was stable in PBS, NaOAc buffered solution (pH = 5.5), and 5% HSA for at least 2 h, according to previously reported procedures …”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Liu

et al. 2018

Mol. Pharmaceutics

Self Cite

View full text Add to dashboard Cite

show abstract

“…In addition, the structure of PA1 is simpler and the synthesis is more convenient than that of PA. Moreover, PA1 has similar binding affinity for SSTRs as PA, which shows higher affinity for multiple SSTRs and more effective effect on the diagnosis of SSTRs positive expressing tumors. , Here, we further investigated the potential of 64 Cu-labeled PA1 for the diagnosis of multiple SSTRs expressing tumors.…”

mentioning

confidence: 99%

Evaluation of Pan-SSTRs Targeted Radioligand [⁶⁴Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice

Liu

Guo

Liu

et al. 2020

ACS Med. Chem. Lett.

Self Cite

View full text Add to dashboard Cite

64Cu-labeled new pan-somatostatin receptors (pan-SSTRs) probe PA1 was synthesized, characterized, and evaluated by in vitro and in vivo experiments. [64Cu]NOTA-PA1 was obtained with high specific activity, high radiochemical purity, and good stability. Cell uptake of [64Cu]NOTA-PA1 was higher than that of [64Cu]DOTA-TATE in MCF-7, A549, BGC823, and HT-29 cell lines. [64Cu]NOTA-PA1 showed high binding affinity for SSTRs expressed in A549 cells. The in vivo biodistribution and micropositron emission tomography (micro-PET) imaging studies of [64Cu]NOTA-PA1 revealed good detection ability in MCF-7 and A549 xenografted nude mice. The radiosynthesis, quality control, and preliminary biological evaluation of [64Cu]NOTA-PA1 have broaden the application of radiolabeled octreotide for SSTRs imaging, which could act as a potential multisubtypes targeted radiotracer for imaging SSTRs-positive tumors.

show abstract

Design and radio-synthesis of somatostatin receptors targeted 68Ga-DOTA-Benereotide for non-invasive PET imaging

Cited by 2 publications

References 19 publications

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Evaluation of Pan-SSTRs Targeted Radioligand [⁶⁴Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice

Contact Info

Product

Resources

About

Design and radio-synthesis of somatostatin receptors targeted 68Ga-DOTA-Benereotide for non-invasive PET imaging

Cited by 2 publications

References 19 publications

Design, Synthesis, and Biological Evaluation of 68Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Design, Synthesis, and Biological Evaluation of 68Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Evaluation of Pan-SSTRs Targeted Radioligand [64Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice

Contact Info

Product

Resources

About

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Design, Synthesis, and Biological Evaluation of ⁶⁸Ga-DOTA–PA1 for Lung Cancer: A Novel PET Tracer for Multiple Somatostatin Receptor Imaging

Evaluation of Pan-SSTRs Targeted Radioligand [⁶⁴Cu]NOTA-PA1 Using Micro-PET Imaging in Xenografted Mice