PET imaging of VEGFR and integrins in glioma tumor xenografts using 89Zr labelled heterodimeric peptide

Liu, Weihao; Ma, Hongxia; Li, Feize; Cai, Huawei; Liang, Ranxi; Chen, Xijian; Lan, Tu; Yang, Jijun; Liao, Jiali; Yang, Yuanyou; Liu, Ning

doi:10.1016/j.bmc.2022.116677

Cited by 9 publications

(4 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Very recently, an example of 89 Zr radiolabelled heterodimeric peptide targeting VEGFR (vascular endothelial growth factor receptor) and integrin was also reported. Liu et al 121 combined iRGD (CRGDK(fmoc)GPDC, with high affinity to α v integrins) and D A7R (atwlppr, targeting VEGFR 2 and NRP-1) together, to obtain a specific carrier suitable for 89 Radiolabelling of iRGD and D A7R using 89 Zr was prepared according to the best labelling method: the solution pH was first adjusted with sodium carbonate and then kept in the range of pH 7-8 by the addition of a small amount of HEPES. As a result, high radiolabelling yield (88.7 ± 2.4%) was obtained.…”

Section: Rsc Medicinal Chemistry Accepted Manuscriptmentioning

confidence: 99%

“…Very recently, an example of 89 Zr radiolabelled heterodimeric peptide targeting VEGFR (vascular endothelial growth factor receptor) and integrin was also reported. Liu et al 121 combined iRGD (CRGDK(Fmoc)GPDC, with high affinity to α v integrins) and D A7R (atwlppr, targeting VEGFR 2 and NRP-1) together, to obtain a specific carrier suitable for 89 Zr-based immunoPET tumour imaging. They developed a new 89 Zr labelled radiopharmaceutical (Fmoc-iRGD-PEG 3 -(lys-[ 89 Zr]Zr-DFO)-PEG 3 -D A7R) and systematically investigated its cell binding affinity and tumour uptake in glioma-bearing mice.…”

Section: Dfo and Its Derivativesmentioning

confidence: 99%

See 1 more Smart Citation

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

2023

View full text Add to dashboard Cite

show abstract

Section: Rsc Medicinal Chemistry Accepted Manuscriptmentioning

confidence: 99%

“…Very recently, an example of 89 Zr radiolabelled heterodimeric peptide targeting VEGFR (vascular endothelial growth factor receptor) and integrin was also reported. Liu et al 121 combined iRGD (CRGDK(Fmoc)GPDC, with high affinity to α v integrins) and D A7R (atwlppr, targeting VEGFR 2 and NRP-1) together, to obtain a specific carrier suitable for 89 Zr-based immunoPET tumour imaging. They developed a new 89 Zr labelled radiopharmaceutical (Fmoc-iRGD-PEG 3 -(lys-[ 89 Zr]Zr-DFO)-PEG 3 -D A7R) and systematically investigated its cell binding affinity and tumour uptake in glioma-bearing mice.…”

Section: Dfo and Its Derivativesmentioning

confidence: 99%

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

2023

View full text Add to dashboard Cite

show abstract

“…As a result, adjacent tumor cells may be destroyed even if they do not possess the specific tumor-associated receptor, enzyme, or antigen . Moreover, the sensitivity of hypoxic cells to alpha ray is similar to that of normal oxygen cells, which avoids the tolerance of tumor heterogeneity to radiotherapy and overcomes the deficiency of traditional radiotherapy and chemotherapy. , Furthermore, systemically administered targeted internal irradiation therapy combines molecular-specific cell recognition with ionizing radiation’s antitumor properties, possibly eliminating the primary tumor site as well as cancer that has spread throughout the body, including populations of malignant cells that are not detectable with diagnostic imaging. − …”

Section: Introductionmentioning

confidence: 99%

Effective Treatment of SSTR2-Positive Small Cell Lung Cancer Using ²¹¹At-Containing Targeted α-Particle Therapy Agent Which Promotes Endogenous Antitumor Immune Response

Qin,

Yang,

Zhang

et al. 2023

Mol. Pharmaceutics

Self Cite

View full text Add to dashboard Cite

Small cell lung cancer (SCLC) is a neuroendocrine tumor with a high degree of malignancy. Due to limited treatment options, patients with SCLC have a poor prognosis. We have found, however, that intravenously administered octreotide (Oct) armed with astatine-211 ([ 211 At]SAB-Oct) is effective against a somatostatin receptor 2 (SSTR2)-positive SCLC tumor in SCLC tumor-bearing BALB/c nude mice. In biodistribution analysis, [ 211 At]SAB-Oct achieved the highest concentration in the SCLC tumors up to 3 h after injection as time proceeded. A single intravenous injection of [ 211 At]SAB-Oct (370 kBq) was sufficient to suppress SSTR2-positive SCLC tumor growth in treated mice by inducing DNA double-strand breaks. Additionally, a multitreatment course (370 kBq followed by twice doses of 370 kBq for a total of 1110 kBq) inhibited the growth of the tumor compared to the untreated control group without significant off-target toxicity. Surprisingly, we found that [ 211 At]SAB-Oct could up-regulate the expressions of calreticulin and major histocompatibility complex I (MHC-I) on the tumor cell membrane surface, suggesting that αparticle internal irradiation may activate an endogenous antitumor immune response through the regulation of immune cells in the tumor microenvironment, which could synergically enhance the efficacy of immunotherapy. We conclude that [ 211 At]SAB-Oct is a potential new therapeutic option for SSTR2-positive SCLC.

show abstract

“…However, the success of these therapies depends on the accurate detection and monitoring of cancer cells, which can be challenging when using conventional imaging techniques. One such strategy is the use of 89 Zr-oxalate for the labeling of small molecules, peptides, and other biomolecules [ 6 , 7 ].…”

Section: Introductionmentioning

confidence: 99%

Exploring the Potential of Zirconium-89 in Diagnostic Radiopharmaceutical Applications: An Analytical Investigation

et al. 2023

View full text Add to dashboard Cite

This study highlights the use of 89Zr-oxalate in diagnostic applications with the help of WinAct and IDAC2.1 software. It presents the biodistribution of the drug in various organs and tissues, including bone, blood, muscle, liver, lung, spleen, kidneys, inflammations, and tumors, and analyzes the maximum amount of nuclear transformation per Bq intake for each organ. The retention time of the maximum nuclear transformation and the absorbed doses of the drug in various organs and tissues are also examined. Data from clinical and laboratory studies on radiopharmaceuticals are used to estimate the coefficients of transition. The accumulation and excretion of the radiopharmaceutical in the organs is assumed to follow an exponential law. The coefficients of transition from the organs to the blood and vice versa are estimated using a combination of statistical programs and digitized data from the literature. WinAct and IDAC 2.1 software are used to calculate the distribution of the radiopharmaceutical in the human body and to estimate the absorbed doses in organs and tissues. The results of this study can provide valuable information for the biokinetic modeling of wide-spectrum diagnostic radiopharmaceuticals. The results show that 89Zr-oxalate has a high affinity for bones and a relatively low impact on healthy organs, making it helpful in targeting bone metastases. This study provides valuable information for further research on the development of this drug for potential clinical applications.

show abstract

PET imaging of VEGFR and integrins in glioma tumor xenografts using 89Zr labelled heterodimeric peptide

Cited by 9 publications

References 34 publications

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

Effective Treatment of SSTR2-Positive Small Cell Lung Cancer Using ²¹¹At-Containing Targeted α-Particle Therapy Agent Which Promotes Endogenous Antitumor Immune Response

Exploring the Potential of Zirconium-89 in Diagnostic Radiopharmaceutical Applications: An Analytical Investigation

Contact Info

Product

Resources

About

PET imaging of VEGFR and integrins in glioma tumor xenografts using 89Zr labelled heterodimeric peptide

Cited by 9 publications

References 34 publications

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling

Effective Treatment of SSTR2-Positive Small Cell Lung Cancer Using 211At-Containing Targeted α-Particle Therapy Agent Which Promotes Endogenous Antitumor Immune Response

Exploring the Potential of Zirconium-89 in Diagnostic Radiopharmaceutical Applications: An Analytical Investigation

Contact Info

Product

Resources

About

Effective Treatment of SSTR2-Positive Small Cell Lung Cancer Using ²¹¹At-Containing Targeted α-Particle Therapy Agent Which Promotes Endogenous Antitumor Immune Response