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A DNA Aptamer That Inhibits the Formation of Unliganded Receptor Dimer and Ligand-Independent Signaling in Cancer Cells

preprint
submitted on 08.09.2020 and posted on 09.09.2020 by Akihiro Eguchi, Ayaka Ueki, Junya Hoshiyama, Keiko Kuwata, Satoru Nagatoishi, Kouhei Tsumoto, Ryosuke Ueki, Shinsuke Sando

Growth factor receptors are activated through dimerization by the binding of their ligands and play pivotal roles in normal cell function. However, in cancer cells, the overexpression of receptors often causes the formation of unliganded receptor dimers, which can be activated in a ligand-independent manner. Thus, the unliganded receptor dimer is a promising target to inhibit aberrant signaling in cancer. Here, we report an aptamer that inhibits ligand-independent receptor activation via preventing the formation of unliganded receptor dimer. By biasing the receptor monomer–dimer equilibrium to the monomer, this aptamer inhibited aberrant cell signaling caused by the unliganded receptor dimer. This work presents a new possibility of oligonucleotide-based therapeutics for cancer.

History

Email Address of Submitting Author

ssando@chembio.t.u-tokyo.ac.jp

Institution

The University of Tokyo

Country

Japan

ORCID For Submitting Author

0000-0003-0275-7237

Declaration of Conflict of Interest

No conflict of interest

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