Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

Active tumor pretargeting using peptide nucleic acid bioconjugates as complementary system

Zarschler, K.

The ability of early-stage diagnosis of tumor malignancies and personalized treatment ultimately relies on the availability of highly tumor-affine compounds with purposeful pharmacological profile. In this regard, monoclonal antibodies (mAbs) are particularly valuable as these molecules bind to tumor-associated epitopes with high specificity and affinity. The conventional concept of directly radiolabeled tumor-specific mAbs for radioimmunodetection (RID) and -therapy (RIT) has certainly several drawbacks, most prominently the prolonged radiation exposure of healthy tissues and organs. Fortunately, however, several of these shortcomings can be eliminated by implementing the pretargeting strategy allowing for the rational use of long circulating, high-affinity mAbs for both non-invasive cancer RID and RIT [1].
This keynote lecture will give a general overview about the pre-targeting strategy and present the different approaches for specific radionuclide delivery to pretargeted tissues. Furthermore, the different in vivo recognition systems will be introduced, with particular emphasis on synthetic complementary oligonucleotides such as peptide nucleic acid (PNA) derivatives. Regarding the latter, their synthesis as well as characterization will be described and, finally, an active tumor pretargeting approach using PNA bioconjugates will be exemplified [2].

[1] M. Patra, K. Zarschler, H.-J. Pietzsch, H. Stephan and G. Gasser, Chem Soc Rev 45 (2016) 6415-6431.
[2] A. Leonidova, C. Foerster, K. Zarschler, M. Schubert, H.-J. Pietzsch, J. Steinbach, R. Bergmann, N. Metzler-Nolte, H. Stephan, and G. Gasser, Chem Sci 6 (2015) 5601-5616.

  • Invited lecture (Conferences)
    2nd Internacional Caparica Christmas Congress on Translational Chemistry 2017 - IC3TC, 04.-07.12.2017, Caparica, Portugal

Publ.-Id: 25780