Cited 17 time in
Cited 17 time in
New Bifunctional Chelator for Cu-64-Immuno-Positron Emission Tomography
- New Bifunctional Chelator for Cu-64-Immuno-Positron Emission Tomography
- Pandya, DN[Pandya, Darpan N.]; Bhatt, N[Bhatt, Nikunj]; Dale, AV[Dale, Ajit V.]; Kim, JY[Kim, Jung Young]; Lee, H[Lee, Hochun]; Ha, YS[Ha, Yeong Su]; Lee, JE[Lee, Ji-Eun]; An, GI[An, Gwang Il]; Yoo, J[Yoo, Jeongsoo]
- DGIST Authors
- Lee, H[Lee, Hochun]
- Issue Date
- Bioconjugate Chemistry, 24(8), 1356-1366
- Article Type
- 1,8-N,N′-Bis-(Carboxymethyl)-4-N″-(4′-Isothiocyanatophenethyl)-1,4,8,11-Tetraazacyclotetradecane; Animal; Animal Experiment; Animal Model; Animalia; Animals; Antibodies, Monoclonal; Atom; Breast Neoplasms; Breast Tumor; Carboxylic Acid; Cell Line, Tumor; Chelating Agent; Chelating Agents; Chemical Analysis; Chemistry; Conjugation; Controlled Study; Copper; Copper 64; Copper Complex; Copper Radioisotopes; Cupric Ion; Cyclic Potentiometry; Diagnostic Use; Drug Synthesis; Female; Functional Group; Geometry; Heterocyclic Compounds, 1-Ring; Immunology; Isothiocyanates; Isothiocyanic Acid Derivative; Macrocyclic Compound; Mice; Monoclonal Antibody; Mouse; Nitrogen; Non-Human; Oxygen; Pentetic Acid; Positron-Emission Tomography; Positron-Emission Tomography (PET); Procedures; Room-Temperature; Scintiscanning; Single Heterocyclic Rings; Tetraxetan; Trastuzumab; Tumor Cell Line; X Ray Crystallography
- A new tetraazamacrocyclic bifunctional chelator, TE2A-Bn-NCS, was synthesized in high overall yield from cyclam. An extra functional group (NCS) was introduced to the N-atom of TE2A for specific conjugation with antibody. The Cu complex of TE2A-Bn-NCS showed high kinetic stability in acidic decomplexation and cyclic voltammetry studies. X-ray structure determination of the Cu-TE2A-Bn-NH2 complex confirmed octahedral geometry, in which copper atom is strongly coordinated by four macrocyclic nitrogens in equatorial positions and two carboxylate oxygen atoms occupy the elongated axial positions. Trastuzumab was conjugated with TE2A-Bn-NCS and then radiolabeled with 64Cu quantitatively at room temperature within 10 min. Biodistribution studies showed that the 64Cu-labeled TE2A-Bn-NCS-trastuzumab conjugates maintain high stability in physiological conditions, and NIH3T6.7 tumors were clearly visualized up to 3 days by 64Cu-immuno-positron emission tomography imaging in animal models. © 2013 American Chemical Society.
- American Chemical Society
- Related Researcher
Electrochemistry Laboratory for Sustainable Energy(ELSE)
Lithium-ion batteries; Novel Materials for rechargeable batteries; Novel energy conversion;storage systems; Electrochemistry; 리튬이차전지; 이차전지용 신규 전극 및 전해액; 신규 에너지변환 및 저장 시스템; 전기화학
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- Department of Energy Science and EngineeringElectrochemistry Laboratory for Sustainable Energy(ELSE)1. Journal Articles
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