ArticleMolecular pharmaceutics2014
Pycup--a bifunctional, cage-like ligand for (64)Cu radiolabeling.
Article in Molecular pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- First-in-human Evaluation of Safety and Dosimetry of [Molecular imaging and biology · 2025Article
- Dosimetry of [medRxiv : the preprint server for health sciences · 2024Article
- Enhancement of the Antioxidant Activity and Neurotherapeutic Features through Pyridol Addition to Tetraazamacrocyclic Molecules.Inorganic chemistry · 2019Article
- New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging.Inorganic chemistry · 2016Article
- Synthesis and crystal structure of [2,7,12-trimethyl-3,7,11,17-tetra-aza-bicyclo-[11.3.1]hepta-deca-1(17),13,15-triene-κ(4) N]copper(II) bis-(perchlorate).Acta crystallographica. Section E, Crystallographic communications · 2016Article
- Red Blood Cell-Facilitated Photodynamic Therapy for Cancer Treatment.Advanced functional materials · 2016Article
- Phosphonate Pendant Armed Propylene Cross-Bridged Cyclam: Synthesis and Evaluation as a Chelator for Cu-64.ACS medicinal chemistry letters · 2015Article
- Multisite Thrombus Imaging and Fibrin Content Estimation With a Single Whole-Body PET Scan in Rats.Arteriosclerosis, thrombosis, and vascular biology · 2015Article
- Multimodal Molecular Imaging Reveals High Target Uptake and Specificity of 111In- and 68Ga-Labeled Fibrin-Binding Probes for Thrombus Detection in Rats.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2015Article
- Radiation Dosimetry of the Fibrin-Binding Probe ⁶⁴Cu-FBP8 and Its Feasibility for PET Imaging of Deep Vein Thrombosis and Pulmonary Embolism in Rats.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2015Article
- Cu(2+)-RGDFRGDS: exploring the mechanism and high efficacy of the nanoparticle in antithrombotic therapy.International journal of nanomedicine · 2015Article
- In vivo molecular imaging of thrombosis and thrombolysis using a fibrin-binding positron emission tomographic probe.Circulation. Cardiovascular imaging · 2014Article
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9 authors.
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Abstract
In developing targeted probes for positron emission tomography (PET) based on (64)Cu, stable complexation of the radiometal is key, and a flexible handle for bioconjugation is highly advantageous. Here, we present the synthesis and characterization of the chelator pycup and four derivatives. Pycup is a cross-bridged cyclam derivative with a pyridyl donor atom integrated into the cross-bridge resulting in a pentadentate ligand. The pycup platform provides kinetic inertness toward (64)Cu dechelation and offers versatile bioconjugation chemistry. We varied the number and type of additional donor atoms by alkylation of the remaining two secondary amines, providing three model ligands, pycup2A, pycup1A1Bn, and pycup2Bn, in 3-4 synthetic steps from cyclam. All model copper complexes displayed very slow decomplexation in 5 M HCl and 90 °C (t1/2: 1.5 h for pycup1A1Bn, 2.7 h for pycup2A, 20.3 h for pycup2Bn). The single crystal crystal X-ray structure of the [Cu(pycup2Bn)](2+) complex showed that the copper was coordinated in a trigonal, bipyramidal manner. The corresponding radiochemical complexes were at least 94% stable in rat plasma after 24 h. Biodistribution studies conducted in Balb/c mice at 2 h postinjection of (64)Cu labeled pycup2A revealed low residual activity in kidney, liver, and blood pool with predominantly renal clearance observed. Pycup2A was readily conjugated to a fibrin-targeted peptide and labeled with (64)Cu for successful PET imaging of arterial thrombosis in a rat model, demonstrating the utility of our new chelator in vivo.
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