Radioiodinated Pentixather for SPECT Imaging of Expression of the Chemokine Receptor CXCR4 in Rat Myocardial-Infarction–Reperfusion Models

Li, Jindian; Peng, Chenyu; Guo, Zhide; Shi, Changrong; Zhuang, Rongqiang; Hong, Xingfang; Wang, Xiangyu; Xu, Duo; Zhang, Pu; Zhang, Deliang; Liu, Ting; X, Su; Zhang, Xianzhong

doi:10.1021/acs.analchem.8b02553

Cited by 16 publications

(25 citation statements)

References 32 publications

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“…published data. 23,27 Thackeray et al reported a significantly increased I/R at day 3 as compared to the control group with a significant decline up to day 7. 23 Li et al investigated the CXCR4 expression in a rat ischemiareperfusion model (I/R) with 125 I-pentixather and found a maximum uptake 3 days after I/R.…”

Section: Discussionmentioning

confidence: 99%

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Molecular imaging of cardiac CXCR4 expression in a mouse model of acute myocardial infarction using a novel 68Ga-mCXCL12 PET tracer

Zacherl

Todica

Wängler

et al. 2021

Journal of Nuclear Cardiology

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Background The chemokine receptor CXCR4 and its ligand CXCL12 have been shown to be a possible imaging and therapeutic target after myocardial infarction (MI). The murine-based and mouse-specific 68Ga-mCXCL12 PET tracer could be suitable for serial in vivo quantification of cardiac CXCR4 expression in a murine model of MI. Methods and Results At days 1-6 after MI, mice were intravenously injected with 68Ga-mCXCL12. Autoradiography was performed and the infarct-to-remote ratio (I/R) was determined. In vivo PET imaging with 68Ga-mCXCL12 was conducted on days 1-6 after MI and the percentage of the injected dose (%ID/g) of the tracer uptake in the infarct area was calculated. 18F-FDG-PET was performed for anatomical landmarking. Ex vivo autoradiography identified CXCR4 upregulation in the infarct region with an increasing I/R after 12 hours (1.4 ± 0.3), showing a significant increase until day 2 (4.5 ± 0.6), followed by a plateau phase (day 4) and decrease after 10 days (1.3 ± 1.0). In vivo PET imaging identified similar CXCR4 upregulation in the infarct region which peaked around day 3 post MI (9.7 ± 5.0 %ID/g) and then subsequently decreased by day 6 (2.8 ± 1.0 %ID/g). Conclusion Noninvasive molecular imaging of cardiac CXCR4 expression using a novel, murine-based, and specific 68Ga-mCXCL12 tracer is feasible both ex vivo and in vivo.

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Section: Discussionmentioning

confidence: 99%

“…Signal decreased after 3 days but was still visible 7 days after MI. 27 However, with our PET imaging approach, the exact source of the cellular signal remains unclear. In fact, the image displays a composition of different cell types, which are present in the respective myocardial region.…”

Section: Discussionmentioning

confidence: 99%

Molecular imaging of cardiac CXCR4 expression in a mouse model of acute myocardial infarction using a novel 68Ga-mCXCL12 PET tracer

Zacherl

Todica

Wängler

et al. 2021

Journal of Nuclear Cardiology

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“…Saturation binding experiments were performed by using PR‐positive MCF‐7 cells according to the published procedures . There were approximately 2 × 10 5 cells in each well of a 24‐well plate to which eight different concentrations of 131 I‐EIPBA or 131 I‐EIPB were used, ranging from 1 to 150 nmol/L.…”

Section: Methodsmentioning

confidence: 99%

Radioiodinated progesterone derivative for progesterone receptor targeting with enhanced nucleus uptake via phenylboronic acid conjugation

Gao

Peng

et al. 2019

Labelled Comp Radiopharmac

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A novel 131I‐radiolabeled probe with aromatic boronate motif (131I‐EIPBA) was designed to target progesterone receptor (PR)–positive breast cancer with enhanced nucleus uptake. Acetylene progesterone was conjugated with pegylated phenylboronic acid via click reaction and radiolabeled with 131I to afford 131I‐EIPBA. Meanwhile, 131I‐EIPB without boronate was prepared as control agent. After determination of the lipophilicity and stability of these tracers, in vitro cell uptake studies and in vivo biodistribution in rats were performed to verify the enhanced nucleus uptake and PR targeting ability of 131I‐EIPBA. 131I‐EIPBA was obtained with moderate radiochemical yield (40.35 ± 3.52%) and high radiochemical purity (>98%). As expected, the high binding affinity (39.58 nM) of 131I‐EIPBA for PR was determined by cell binding assay. The internalization ratio of 131I‐EIPBA was remarkably higher than that of 131I‐EIPB in PR‐positive MCF‐7 cells. Furthermore, the enhanced nucleus uptake of 131I‐EIPBA (0.59 ± 0.02%) was found to be significantly higher than that of 131I‐EIPB (0.13 ± 0.01%) in MCF‐7 cells. A novel 131I‐EIPBA compound was developed for PR targeting with improved cellular nucleus uptake. Furthermore, the introduction of aromatic boronate motif provides a worthwhile strategy for enhancing the nuclear receptor targeting of tracers.

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“…CXCR4 plays a pivotal role in recruiting immune cells and homing stem cells and progenitor cells 182-184. CXCR4 is overexpressed on multiple human tumor types including esophageal, prostate, ovarian, and renal cell carcinoma, boosting tumor proliferation and metastasis 185, 186.…”

Section: Small Molecules For Imaging Cancer Immunotherapymentioning

confidence: 99%

Small molecules as theranostic agents in cancer immunology

Li¹,

Valkenburgh²,

Hong³

et al. 2019

Theranostics

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With further research into the molecular mechanisms and roles linking immune suppression and restraint of (pre)malignancies, immunotherapies have revolutionized clinical strategies in the treatment of cancer. However, nearly 70% of patients who received immune checkpoint therapeutics showed no response. Complementary and/or synergistic effects may occur when extracellular checkpoint antibody blockades combine with small molecules targeting intracellular signal pathways up/downstream of immune checkpoints or regulating the innate and adaptive immune response. After radiolabeling with radionuclides, small molecules can also be used for estimating treatment efficacy of immune checkpoint blockades. This review not only highlights some significant intracellular pathways and immune-related targets such as the kynurenine pathway, purinergic signaling, the kinase signaling axis, chemokines, etc., but also summarizes some attractive and potentially immunosuppression-related small molecule agents, which may be synergistic with extracellular immune checkpoint blockade. In addition, opportunities for small molecule-based theranostics in cancer immunology will be discussed.

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Radioiodinated Pentixather for SPECT Imaging of Expression of the Chemokine Receptor CXCR4 in Rat Myocardial-Infarction–Reperfusion Models

Cited by 16 publications

References 32 publications

Molecular imaging of cardiac CXCR4 expression in a mouse model of acute myocardial infarction using a novel 68Ga-mCXCL12 PET tracer

Molecular imaging of cardiac CXCR4 expression in a mouse model of acute myocardial infarction using a novel 68Ga-mCXCL12 PET tracer

Radioiodinated progesterone derivative for progesterone receptor targeting with enhanced nucleus uptake via phenylboronic acid conjugation

Small molecules as theranostic agents in cancer immunology

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