Voraussetzungen für den Einsatz von Antisense-Diagnostika in der Nuklearmedizin

Zusammenfassung

Mit dem Einsatz von radiomarkierten Antisense-Oligonukleotiden als Tracer in der Nuklearmedizin eröffnet sich eine vielversprechende Perspektive, neue Wege in der bildgebenden Diagnostik zu beschreiten. Vor allem in der Tumordiagnostik scheint eine quantitative Akkumulation von Antisense-Proben, welche gegen abundant exprimierte Onkogen-mRNAs gerichtet sind, vorstellbar. Dazu ist allerdings noch eine Optimierung folgender Parameter erforderlich: (i) eine schnelle und effiziente Radiomarkierung von Oligonukleotiden mit in der Nuklearmedizin gebräuchlichen Isotopen, (ü) eine rasche Penetration der Nukleinsäure ins Zielgewebe, (iii) eine zügige Internalisierung des Tracers in die Tumorzellen, (iv) eine hohe Spezifität der Hybridbildung mit der Target-mRNA, und (v) eine hohe Stabilität des gebildeten Hybrids gegenüber intrazellulären Nukleasen.

Summary

A new promising perspective in nuclear medicine is the use of radiolabeled antisense oligonucleotides as diagnostic markers. Especially for cancer diagnostics, a quantitative accumulation of antisense probes which are directed against abundantly expressed oncogene mRNAs seems to be reasonable. However, the development of this strategy still requires an optimization of several parameters: (i) rapid and efficient radiolabeling methods, (ii) a fast penetration of the probe into the target tissue, (iii) a fast internalization into the tumor cell, (iv) an oligonucleo-tide/mRNA hybrid formation with high specificity, and (v) a high stability of the hybrid against intracellular nucleases.

Schlüsselwörter

Antisense - Oligonukleotide - Onkologie - PET

Key words

Antisense - oligonucleotide - oncology - PET

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