Macrocyclic chelator assembled RGD multimers for tumor targeting.

Molecular Imaging Program at Stanford, Department of Radiology, Stanford University Medical Center, California 94305, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.33). 06/2011; 21(11):3423-6. DOI: 10.1016/j.bmcl.2011.03.110
Source: PubMed

ABSTRACT Macrocyclic chelators have been extensively used for complexation of metal ions. A widely used chelator, DOTA, has been explored as a molecular platform to assemble multiple bioactive peptides in this paper. The multivalent DOTA-peptide bioconjugates demonstrate promising tumor targeting ability.

  • [Show abstract] [Hide abstract]
    ABSTRACT: Positron emission tomography (PET) imaging of receptor integrin αv β3 expression may play a key role in the early detection of cancer and cardiovascular diseases, monitoring disease progression, evaluating therapeutic response, and aiding anti-angiogenic drugs discovery and development. The last decade has seen the development of new PET tracers for in vivo imaging of integrin αv β3 expression along with advances in PET chemistry. In this review, we will focus on the radiochemistry development of PET tracers based on arginine-glycine-aspartic acid (RGD) peptide, present an overview of general strategies for preparing RGD-based PET tracers, and review the recent advances in preparations of (18) F-labeled, (64) Cu-labeled, and (68) Ga-labeled RGD tracers, RGD-based PET multivalent probes, and RGD-based PET multimodality probes for imaging receptor integrin αv β3 expression.
    Journal of Labelled Compounds 05/2013; 56(5):264-279. DOI:10.1002/jlcr.2999
  • [Show abstract] [Hide abstract]
    ABSTRACT: Two bicyclic compounds containing Arg-Gly-Asp (RGD) motifs (RGDf and RGD) were synthesized by cyclizing the peptide sequence across the macrocyclic ring of DOTA via two non-adjacent carboxylate pendent arms. The Lu(3+) or Cu(2+) complexes of these compounds, c(DOTA-RGDf) and c(DOTA-RGD), showed a metal dependent affinity towards integrin α(v)β(3)in vitro and the (177)Lu(3+) or (64)Cu(2+) labelled derivatives showed specific tumour uptake in MCF7 and U87MG tumour bearing mice.
    Dalton Transactions 10/2012; 41(46). DOI:10.1039/c2dt31493b · 4.10 Impact Factor
  • Source
    [Show abstract] [Hide abstract]
    ABSTRACT: The development of chelating agents for copper radionuclides in positron emission tomography radiopharmaceuticals has been a highly active and important area of study in recent years. The rapid evolution of chelators has resulted in highly specific copper chelators that can be readily conjugated to biomolecules and efficiently radiolabeled to form stable complexes in vivo. Chelators are not only designed for conjugation to monovalent biomolecules but also for incorporation into multivalent targeting ligands such as theranostic nanoparticles. These advancements have strengthened the role of copper radionuclides in the fields of nuclear medicine and molecular imaging. This review emphasizes developments of new copper chelators that have most greatly advanced the field of copper-based radiopharmaceuticals over the past 5 years.
    Journal of Labelled Compounds 04/2014; 57(4). DOI:10.1002/jlcr.3165

Full-text (2 Sources)

Available from
Jun 4, 2014