ArticleInorganic chemistry2012
H(2)azapa: a versatile acyclic multifunctional chelator for (67)Ga, (64)Cu, (111)In, and (177)Lu.
Article in Inorganic chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- Chemical Tools to Characterize the Coordination Chemistry of Radionuclides for Radiopharmaceutical Applications.Chemical reviews · 2025Review
- Tuning the Properties of Rigidified Acyclic DEDPAInorganic chemistry · 2024Article
- Cyclohexanediamine Triazole (CHDT) Functionalization Enables Labeling of Target Molecules with AlBioconjugate chemistry · 2024Article
- Article
- Approaches to Reducing Normal Tissue Radiation from Radiolabeled Antibodies.Pharmaceuticals (Basel, Switzerland) · 2024Review
- TowardInorganic chemistry · 2023Article
- Modern Developments in Bifunctional Chelator Design for Gallium Radiopharmaceuticals.Molecules (Basel, Switzerland) · 2022Review
- A review of advances in the last decade on targeted cancer therapy usingAmerican journal of nuclear medicine and molecular imaging · 2021Review
- Oxyaapa: A Picolinate-Based Ligand with Five Oxygen Donors that Strongly Chelates Lanthanides.Inorganic chemistry · 2020Article
- Recent Advances in Zirconium-89 Chelator Development.Molecules (Basel, Switzerland) · 2018Review
- Coordination Chemistry of Bifunctional Chemical Agents Designed for Applications inInorganic chemistry · 2017Article
- Evaluation ofJournal of the American Chemical Society · 2017Article
- Click Chemistry and Radiochemistry: The First 10 Years.Bioconjugate chemistry · 2016Review
- Brightly Luminescent and Kinetically Inert Lanthanide Bioprobes Based on Linear and Preorganized Chelators.Bioconjugate chemistry · 2016Article
- New surface radiolabeling schemes of super paramagnetic iron oxide nanoparticles (SPIONs) for biodistribution studies.Nanoscale · 2015Article
- What a difference a carbon makes: H₄octapa vs H₄C3octapa, ligands for In-111 and Lu-177 radiochemistry.Inorganic chemistry · 2014Article
- Pycup--a bifunctional, cage-like ligand for (64)Cu radiolabeling.Molecular pharmaceutics · 2014Article
- H6phospa-trastuzumab: bifunctional methylenephosphonate-based chelator with 89Zr, 111In and 177Lu.Dalton transactions (Cambridge, England : 2003) · 2014Article
- Non-cross-bridged tetraazamacrocyclic chelator for stable (64)cu-based radiopharmaceuticals.ACS medicinal chemistry letters · 2013Article
- H(4)octapa-trastuzumab: versatile acyclic chelate system for 111In and 177Lu imaging and therapy.Journal of the American Chemical Society · 2013Article
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10 authors.
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Abstract
Preliminary experiments with the novel acyclic triazole-containing bifunctional chelator H2azapa and the radiometals (64)Cu, (67)Ga, (111)In, and (177)Lu have established its significant versatile potential as an alternative to 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) for metal-based radiopharmaceuticals. Unlike DOTA, H2azapa radiolabels quantitatively with (64)Cu, (67)Ga, (111)In, and (177)Lu in 10 min at room temperature. In vitro competition experiments with human blood serum show that (64)Cu remained predominantly chelate-bound, with only 2% transchelated to serum proteins after 20 h. Biodistribution experiments with [(64)Cu(azapa)] in mice reveal uptake in various organs, particularly in the liver, lungs, heart, intestines, and kidneys. When compared to [(64)Cu(DOTA)](2-), the lipophilic neutral [(64)Cu(azapa)] was cleared through the gastrointestinal tract and accumulated in the liver, which is common for lipophilic compounds or free (64)Cu. The chelator H2azapa is a model complex for a click-based bifunctional chelating agent, and the lipophilic benzyl "place-holders" will be replaced by hydrophilic peptides to modulate the pharmacokinetics and direct activity away from the liver and gut. The solid-state molecular structure of [In(azapa)(H2O)][ClO4] reveals a very rare eight-coordinate distorted square antiprismatic geometry with one triazole arm bound, and the structure of [(64)Cu(azapa)] shows a distorted octahedral geometry. The present study demonstrates significant potential for bioconjugates of H2azapa as alternatives to DOTA in copper-based radiopharmaceuticals, with the highly modular and "clickable" molecular scaffold of H2azapa easily modified into a variety of bioconjugates. H2azapa is a versatile addition to the "pa" family, joining the previously published H2dedpa ((67/68)Ga and (64)Cu), H4octapa ((111)In, (177)Lu, and (90)Y), and H5decapa ((225)Ac) to cover a wide range of important nuclides.
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