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Biochimie. 2018 Feb;145:22-33. doi: 10.1016/j.biochi.2017.10.006. Epub 2017 Oct 16.

Aptamers as therapeutic middle molecules.

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The Institute of Medical Science, The University of Tokyo, Minato-ku, Tokyo 108-8639, Japan; RIBOMIC Inc., Minato-ku, Tokyo 108-0071, Japan. Electronic address:


Therapeutic molecules can be classified as low-, middle- and high-molecular weight drugs depending on their molecular masses. Antibodies represent high-molecular weight drugs and their clinical applications have been developing rapidly. Aptamers, on the other hand, are middle-molecular weight molecules that are short, single-stranded nucleic acid sequences that are selected in vitro from large oligonucleotide libraries based on their high affinity to a target molecule. Hence, aptamers can be thought of as a nucleic acid analog to antibodies. However, several viewpoints hold that the potential of aptamers arises from interesting characteristics that are distinct from, or in some cases, superior to those of antibodies. Recently, therapeutic middle molecules gain considerable attention as protein-protein interaction (PPI) inhibitors. This review summarizes the recent achievements in aptamer development in our laboratory in terms of PPI and non-PPI inhibitors.


Bone disease; FGF2; PPI; RNA aptamer; SPR

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