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

09 September 2020, Version 1


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.


Supplementary materials

SI ChemRxiv


Comments are not moderated before they are posted, but they can be removed by the site moderators if they are found to be in contravention of our Commenting Policy [opens in a new tab] - please read this policy before you post. Comments should be used for scholarly discussion of the content in question. You can find more information about how to use the commenting feature here [opens in a new tab] .
This site is protected by reCAPTCHA and the Google Privacy Policy [opens in a new tab] and Terms of Service [opens in a new tab] apply.