Selection and Characterization of an α6β4 Integrin blocking DNA Aptamer

Berg K., Lange T., Mittelberger F., Schumacher U., Hahn U.Molecular Therapy—Nucleic Acids, 2016

Cancer cells use the α6β4 integrin/laminin-332 interaction to activate signaling pathways promoting tumor cell growth, invasion and metastasis, the inhibition of this interaction is of high therapeutic interest. Here, the authors report on the selection of a DNA aptamer inhibiting the interaction between α6β4 integrin and laminin-332. This Integrin α6β4-specific DNA Aptamer inhibits the adhesion of prostate cancer cells (PC-3) to laminin-332 with an IC50 value of 149 nmol/l. the aptamer was internalized into PC- 3-cells. Further characterization showed specificity to α6 integrins and a half-life in the murine blood plasma of 6 hours.