Development of a Radiolabeled Irreversible Peptide Ligand for PET Imaging of Vascular Endothelial Growth Factor

Marquez, Bernadette V.; Ikotun, Oluwatayo F.; Parry, Jesse J.; Rogers, Buck E.; Meares, Claude F.; Lapi, Suzanne E.

doi:10.2967/jnumed.113.130898

Cited by 10 publications

(39 citation statements)

References 32 publications

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“…The factors that drive VEGF expression remain a critical unknown. Nonetheless, tracking VEGF expression (with positron emission tomography for example [18]) might be warranted in patients being treated with anti-VEGF therapies.…”

Section: Discussionmentioning

confidence: 99%

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Pérez-Torres

Schmidt

et al. 2015

Radiotherapy and Oncology

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Section: Discussionmentioning

confidence: 99%

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Pérez-Torres

Schmidt

et al. 2015

Radiotherapy and Oncology

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“…55 Co-NO2A-L19K-FDNB and 55 Co-DO3A-L19K-FDNB were prepared and radiolabeled similarly to the 64 Cu analogues described by Marquez and colleagues 32 and with a final specific activity of 3.7 MBq/μg. One hundred microliters of 74 kBq/μL 55 CoCl2, 37 kBq/μL 55 Co-NO2A-FDNB, or 37 kBq/μL 55 Co-DO3A-FDNB in saline was injected into HCT-116 tumor-bearing mice.…”

Section: Methodsmentioning

confidence: 99%

“…It has previously been established that changing the radiometal on peptides can have a drastic effect on the affinity of the peptide to its receptor. 35 Using 55 Co to radiolabel the NO2A-or DO3A-peptides dramatically decreased the affinity for their tumor-associated target, vascular endothelial growth factor (VEGF), 32 as shown by their reduced tumor uptake compared to the 64 Cu-labeled analogue, which was radiolabeled at the same specific activity ( Figure S1, online version only). The 24-and 48-hour biodistribution studies of 55 Co-NO2A-L19K-FDNB and 55 Co-DO3A-L19K-FDNB were compared to free 55 CoCl 2 (see Table 1).…”

Section: Stability Of 55 Co-chelate Complexesmentioning

confidence: 99%

“…30,31 As a model system, we applied 55 Co to a peptide ligand, L19K-FDNB, which has been shown to have a long blood-clearance time. 32 This property makes this peptide an optimal system for studying the stability of 55 Co-chelate complexes as 55 Co-DO3A-L19K-FDNB and 55 Co-NO2A-L19K-FDNB in vivo at time points up to 48 hours. The biodistribution data for 55 CoCl 2 , 55 Co-NO2A-L19K-FDNB, and 55 Co-DO3A-L19K-FDNB were compared at 24 and 48 hours postinjection to establish the in vivo stability of 55 Co chelated with NO2A-and DO3A-peptide conjugates in tumor-bearing mice.…”

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confidence: 99%

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Cyclotron Production of High–Specific Activity ⁵⁵ Co and In Vivo Evaluation of the Stability of ⁵⁵ Co Metal-Chelate-Peptide Complexes

et al. 2015

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This work describes the production of high-specific activity 55Co and the evaluation of the stability of 55Co-metal-chelate-peptide complexes in vivo. 55Co was produced via the 58Ni(p,α)55Co reaction and purified using anion exchange chromatography with an average recovery of 92% and an average specific activity of 1.96GBq/µmol. 55Co-DO3A and 55Co-NO2A peptide complexes were radiolabelled at 3.7MBq/µg and injected into HCT-116 tumor xenografted mice. PET imaging and biodistribution studies were performed at 24 and 48 hours post injection and compared with that of 55CoCl2. Both 55Co-metal-chelate complexes demonstrated good in vivo stability by reducing the radiotracers’ uptake in the liver by 6-fold at 24 with ~1% ID/g and at 48 hours with ~0.5% ID/g, and reducing uptake in the heart by 4-fold at 24 hours with ~0.7% ID/g and 7-fold at 48 hours with ~0.35% ID/g. These results support the use of 55Co as a promising new radiotracer for Positron Emission Tomography (PET) imaging of cancer and other diseases.

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“…e two peptides, HLys-DOTA and AB1-HLys-DOTA, were radiolabeled with 64 CuCl 2 buffered in 0.1 M NH 4 OAc, pH 6, at 56°C according to modified previously published methods [31,32]. Briefly, radiolabeling of the peptides was achieved by adding 50 μg of HLys-DOTA or AB1-HLys-DOTA into 120-130 MBq (3.2-3.5 mCi) of 64 CuCl 2 in 1450 μL of 0.1 M NH 4 OAc, pH 6. e reactions were incubated on a mixer with 800 rpm agitation at 56°C for 45 min, and radiolabeling was also attempted at lower temperature.…”

Section: Radiolabeling Of Hlys-dota and Ab1-hlys-dota Peptidesmentioning

confidence: 99%

Radiolabeled Cationic Peptides for Targeted Imaging of Infection

Aweda

Müftüler²,

Massicano

et al. 2019

Contrast Media & Molecular Imaging

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Molecular probes targeting bacteria provide opportunities to target bacterial infections in vivo for both imaging and therapy. In the current study, we report the development of positron emission tomography (PET) probes for imaging of live bacterial infection based on the small molecules HLys-DOTA, a polycationic peptide synthesized as the D-isomer (RYWVAWRNRG) conjugated to 1, 4, 7, 10-tetraazacyclododecane-N′,N″,N‴,N-tetraacetic acid (DOTA) and AB1-HLys-DOTA, which includes an unnatural amino acid AB1 that preferentially binds to bacteria membrane lipids with amine groups via formation of iminoboronates. HLys-DOTA and AB1-HLys-DOTA peptides were radiolabeled with 64Cu and investigated as PET imaging agents to track bacterial infection in vitro and in intramuscularly infected (IM) mice models. Cell uptake studies at 37°C in Staphylococcus aureus (SA) show higher uptake of 64Cu-AB1-HLys-DOTA; 98.47 ± 3.54% vs 64Cu-HLys-DOTA; 39.12 ± 3.27% at 24 h. Standard uptake values (SUV) analysis of the PET images resulted in mean SUV of 0.70 ± 0.08, 0.49 ± 0.04, and 0.31 ± 0.01 for 64Cu-AB1-HLys-DOTA and 0.17 ± 0.06, 0.16 ± 0.02, and 0.13 ± 0.01 for 64Cu-HLys-DOTA at 1, 4, and 24 h post injection, respectively, in the infected muscles. Similarly, in the biodistribution studies, dose uptake in the infected muscles was 4 times higher in the targeted 64Cu-AB1-HLys-DOTA group than in the 64Cu-HLys-DOTA group and 2‐3 times higher than in the PBS control group at 1, 4, and 24 h post injection. 64Cu-AB1-HLys-DOTA was able to distinguish between SA-infected muscle and Pseudomonas aeruginosa (PA) infected muscle with lower mean SUV of 0.28 ± 0.10 at 1 h post injection. This illustrates the utility of the AB1 covalently targeting group in synergy with the HLys peptide, which noncovalently binds to bacterial membranes. These results suggest that 64Cu-labeled AB1-HLys-DOTA peptide could be used as an imaging probe for detection of bacterial infection in vivo with specificity for Gram-positive bacteria.

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Development of a Radiolabeled Irreversible Peptide Ligand for PET Imaging of Vascular Endothelial Growth Factor

Cited by 10 publications

References 32 publications

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Cyclotron Production of High–Specific Activity ⁵⁵ Co and In Vivo Evaluation of the Stability of ⁵⁵ Co Metal-Chelate-Peptide Complexes

Radiolabeled Cationic Peptides for Targeted Imaging of Infection

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Development of a Radiolabeled Irreversible Peptide Ligand for PET Imaging of Vascular Endothelial Growth Factor

Cited by 10 publications

References 32 publications

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Specificity of vascular endothelial growth factor treatment for radiation necrosis

Cyclotron Production of High–Specific Activity 55 Co and In Vivo Evaluation of the Stability of 55 Co Metal-Chelate-Peptide Complexes

Radiolabeled Cationic Peptides for Targeted Imaging of Infection

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Product

Resources

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Cyclotron Production of High–Specific Activity ⁵⁵ Co and In Vivo Evaluation of the Stability of ⁵⁵ Co Metal-Chelate-Peptide Complexes