Synthesis and preclinical evaluation of 68Ga-labeled collagelin analogs for imaging and quantification of fibrosis

Velikyan, Irina; Rosenström, Ulrika; Estrada, Sergio; Ljungvall, Ingrid; Häggström, Jens; Eriksson, Olof; Antoni, Gunnar

doi:10.1016/j.nucmedbio.2014.06.001

Cited by 23 publications

(64 citation statements)

References 8 publications

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“…Uptake of 99m Tc -collagelini n fibrotic regions was modestly increased compared with a scrambled peptidec ontrol.T wo PET versions of this probe ([68Ga]Ga-NO2A-Col and [68Ga]Ga-NODAGA-Col;F igure 6A) were reported, but no in vivo data were presented. [72] Another collagen-binding peptidel abeled with 99m Tc wasr eported recently. [73] Peptide CBP1495i sapeptide domain from pro-MMP-2, [74] which is ap recursor of the enzyme MMP-2 that interacts with type Ic ollagen.…”

Section: Pet/spectimagingmentioning

confidence: 99%

“…A) Structures of the collagelin PET probes targeted to the platelet receptorbinding siteo nc ollagens Ia nd III. [72] B) Structure of the collagen-binding SPECT probe 99m Tc -CBP1495 derivedf rom ap eptidedomain from pro-MMP-2. [73] C) Structures of the collagen-binding PET probes 64 Cu-CBP7, [77] Al 18 F-CBP9, [79] Al 18 F-CBP10, [79] and 68 Ga-CBP8.…”

Section: Molecular Imaging Of Fibrogenesismentioning

confidence: 99%

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Molecular Probes for Imaging Fibrosis and Fibrogenesis

Désogère

Montesi

Caravan

2018

Chemistry A European J

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Fibrosis, or the accumulation of extracellular matrix molecules that make up scar tissue, is a common result of chronic tissue injury. Advances in the clinical management of fibrotic diseases have been hampered by the low sensitivity and specificity of noninvasive early diagnostic options, lack of surrogate end points for use in clinical trials, and a paucity of noninvasive tools to assess fibrotic disease activity longitudinally. Hence, the development of new methods to image fibrosis and fibrogenesis is a large unmet clinical need. Herein, an overview of recent and selected molecular probes for imaging of fibrosis and fibrogenesis by magnetic resonance imaging, positron emission tomography, and single photon emission computed tomography is provided.

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Section: Pet/spectimagingmentioning

confidence: 99%

Section: Molecular Imaging Of Fibrogenesismentioning

confidence: 99%

Molecular Probes for Imaging Fibrosis and Fibrogenesis

Désogère

Montesi

Caravan

2018

Chemistry A European J

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“…We anticipated that the conjugation of biotin or NOTA to the N-terminus which is a 7 amino acid spacer away from the collagen-binding amino acid sequence would not appreciably affect the binding of the peptide to collagen. This notion was supported by Velikyan, et al [16] who reported that 68 Ga-labeled collagelin derivatives, [ 68 Ga]Ga-NOTA-PEG 2 -c[CPGRVMHGLHLGDDEGPC] and [ 68 Ga]Ga-NODAGA-PEG 2 -c[CPGRVMHGLHLGDDEGPC] bound to cryosections of the heart tissue with the equilibrium K D of 2.3 ± 0.8 μM and 2.1 ± 0.9 μM, respectively. These dissociation constants (K D ) are similar to that (K D , 0.9 ± 0.4 μM, n = 5) we determined by the interferometry assay using the biotin-labeled peptides.…”

Section: Discussionmentioning

confidence: 73%

“…One disadvantage of the 99m Tc-labeled collagelin was high background activity in abdomen due to high uptake in liver. Recently, Velikyan, et al [16] modified collagelin (Col) with NOTA-PEG 2 and NODAGA-PEG 2 and investigated the distribution and clearance of these collagelin analogues labeled with 68 Ga from the blood and the major organs of normal rats. The pharmacokinetic studies demonstrated that 68 Ga-NO2A-Col and 68 Ga-NODAGA-Col rapidly cleared from the blood and excreted via the renal system with low background radioactivity shown in the abdomen within 25 min post-injection.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and microbiodistribution of 64Cu-labeled collagen-binding peptides in chronic myocardial infarction

Kim¹,

Lee

Kim

et al. 2016

Nuclear Medicine Communications

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Objectives To evaluate the pharmacokinetics and microbiodistribution of 64Cu-labeled collagen binding peptides. Method The affinity constant (KD), association (ka) and dissociation rate constant (kd) for the peptide collagelin or its analogue (named CRPA) binding to collagen were measured by bio-layer interferometric analysis. Rats (n = 4–5) with myocardial infarction or normal were injected IV with the 64Cu-labeled peptides or 64Cu-DOTA as a control. Dynamic PET imaging was performed for 60 min at 7- to 8-week post-infarct. [18F]FDG PET imaging was performed to identify the viable myocardium. To validate the PET images, slices of heart samples from the base to the apex were analyzed using autoradiography and histology. Result The peptides bound to collagen with KD of ~ 0.9 μM. The 64Cu-peptides and 64Cu-DOTA accumulated in the infarct area (confirmed by autoradiography and histology images) within 1 minute of injection and were excreted rapidly via the renal system. The blood clearance curves were bi-phasic with the elimination half-lives, 21.9 ± 2.4, 26.2 ± 4.6 and 21.2 ± 2.1 min for 64Cu-CRPA, 64Cu-collagelin and the control 64Cu-DOTA, respectively. The clearance half-lives from the focal fibrotic tissue (24.1 ± 1.5, 25.6 ± 8.0 and 21.4 ± 1.3 min, respectively) and remote myocardium (20.8 ± 0.7, 21.0 ± 5.5 and 19.1 ± 2.4 min, respectively) were not significantly different. The uptake ratios of infarct-to-remote myocardium (1.93 ± 0.18, 2.15 ± 0.38 and 1.88 ± 0.08, respectively) for 64Cu-CRPA, 64Cu-collagelin and 64Cu-DOTA remained stable for the time period between 10 to 60 min. Conclusion The distribution of the 64Cu-collagelin probes corresponds to the heterogeneous distribution of expanded extracellular space in the setting of myocardial infarction. The overall washout rate from the fibrous tissue was determined by the slow washout rate (t1/2, ≥ 20 min) of the peptides from the extracellular space to the vasculature, not by the dissociation rate (t1/2, ≤ 2 min) of the 64Cu-peptides from collagen.

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“…In addition to the information provided on perfusion and metabolic outcomes, additional imaging could be applied to interrogate regional activation of critical receptors or enzymes within the myocardium, [24][25][26][27][28] neurohormonal changes, [29][30][31][32][33] along with regional changes in myocardial hypoxia, 34 apoptosis, 35,36 necrosis, 37 and fibrosis. 38 Unfortunately, the current study reported a high attrition (overall survival rate of 26%) with a major cause of death attributable to lethal arrhythmias during the perioperative period. However, chronic telemetry was not performed in these studies to establish an arrhythmic cause of death during the chronic experimental period.…”

Section: See Related Article Pp 655-665mentioning

confidence: 65%