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Propylene Cross-Bridged Macrocyclic Bifunctional Chelator: A New Design for Facile Bioconjugation and Robust Cu-64 Complex Stability

Title
Propylene Cross-Bridged Macrocyclic Bifunctional Chelator: A New Design for Facile Bioconjugation and Robust Cu-64 Complex Stability
Authors
Pandya, DN[Pandya, Darpan N.]Bhatt, N[Bhatt, Nikunj]An, GI[An, Gwang Il]Ha, YS[Ha, Yeong Su]Soni, N[Soni, Nisarg]Lee, H[Lee, Hochun]Lee, YJ[Lee, Yong Jin]Kim, JY[Kim, Jung Young]Lee, W[Lee, Woonghee]Ahn, H[Ahn, Heesu]Yoo, J[Yoo, Jeongsoo]
DGIST Authors
Lee, H[Lee, Hochun]
Issue Date
2014-09-11
Citation
Journal of Medicinal Chemistry, 57(17), 7234-7243
Type
Article
Article Type
Article
Keywords
4,11 Bis(Carboxymethyl) 1,4,8,11 Tetraazabicyclo[6,6,3]Hexadecane Isothiocyanate Cyclic Arginylglycylaspartic AcidAlkeneAlkenesAlkylationAnimalAnimal ExperimentAnimal ModelAnimalsArginyl-Glycyl-Aspartic AcidBinding AffinityCarboxylic AcidChelating AgentChelating AgentsChemical ModelChemical StructureChemistryComplex FormationControlled StudyCoordination ComplexesCoordination CompoundCopperCopper 64Copper RadioisotopesCyclamDeprotection ReactionDrug ConjugationDrug DesignDrug DistributionDrug StabilityDrug SynthesisElectrochemistryFemaleGlioblastomaHeterocyclic CompoundHeterocyclic CompoundsHigh Performance Liquid ChromatographyHumanHumansIsotope LabelingMacrocyclic CompoundMacrocyclic CompoundsMetabolismMiceMice, NudeModels, ChemicalMolecular StructureMouseNon-HumanNude MouseOligopeptideOligopeptidesPartition CoefficientPathologyPositron-Emission TomographyPositron-Emission Tomography (PET)ProceduresPropyleneRatRatsSynthesisTissue DistributionTransplantation, HeterologousUnclassified DrugXenograft
ISSN
0022-2623
Abstract
The first macrocyclic bifunctional chelator incorporating propylene cross-bridge was efficiently synthesized from cyclam in seven steps. After the introduction of an extra functional group for facile conjugation onto the propylene cross-bridge, the two carboxylic acid pendants could contribute to strong coordination of Cu(II) ions, leading to a robust Cu complex. The cyclic RGD peptide conjugate of PCB-TE2A-NCS was prepared and successfully radiolabeled with 64Cu ion. The radiolabeled peptide conjugate was evaluated in vivo through a biodistribution study and animal PET imaging to demonstrate high tumor uptake with low background. © 2014 American Chemical Society.
URI
http://hdl.handle.net/20.500.11750/3036
DOI
10.1021/jm500348z
Publisher
American Chemical Society
Related Researcher
  • Author Lee, Ho Chun Electrochemistry Laboratory for Sustainable Energy(ELSE)
  • Research Interests 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
Files:
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Collection:
Energy Science and EngineeringElectrochemistry Laboratory for Sustainable Energy(ELSE)1. Journal Articles


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