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Exploring Sequence Space to Identify Binding Sites for Regulatory RNA-Binding Proteins

Exploring Sequence Space to Identify Binding Sites for Regulatory RNA-Binding Proteins

Published on: August 9, 2019

Aptamers as therapeutic middle molecules.

Yoshikazu Nakamura¹

¹The Institute of Medical Science, The University of Tokyo, Minato-ku, Tokyo 108-8639, Japan; RIBOMIC Inc., Minato-ku, Tokyo 108-0071, Japan.

|October 21, 2017

Summary

Aptamers, nucleic acid analogs of antibodies, are emerging as potent middle-molecular weight therapeutics. This review highlights recent advancements in aptamer development for inhibiting protein-protein interactions (PPIs) and other targets.

Keywords:

Bone disease FGF2 PPI RNA aptamer SPR

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Area of Science:

Biochemistry and Molecular Biology
Drug Discovery and Development
Nucleic Acid Therapeutics

Background:

Therapeutic molecules are classified by molecular weight: low, middle, and high.
High-molecular weight drugs like antibodies have rapidly expanding clinical applications.
Aptamers, middle-molecular weight nucleic acid molecules, are selected in vitro for high target affinity, serving as potential nucleic acid analogs to antibodies.

Purpose of the Study:

To review recent achievements in aptamer development within our laboratory.
To focus on aptamer applications as inhibitors of protein-protein interactions (PPIs) and non-PPI targets.
To highlight the distinct and potentially superior characteristics of aptamers compared to antibodies.

Main Methods:

Selection of aptamers from large oligonucleotide libraries based on high affinity to target molecules.
In vitro screening and characterization of aptamer candidates.
Evaluation of aptamers as inhibitors for both protein-protein interactions and other therapeutic targets.

Main Results:

Demonstrated success in developing aptamers as therapeutic middle molecules.
Identified aptamers with significant inhibitory activity against specific PPIs.
Showcased aptamers effective in non-PPI inhibitory roles.

Conclusions:

Aptamers represent a promising class of middle-molecular weight therapeutics with unique advantages.
Recent laboratory achievements underscore the potential of aptamers in targeting PPIs and other disease mechanisms.
Further development of aptamers holds significant promise for novel therapeutic strategies.