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Cyclic Peptidomimetics as Inhibitor for miR-155 Biogenesis.
Hao Yan1, Mi Zhou2, Umesh Bhattarai1
1Department of Chemistry and Chemical Biology , University of New Mexico , 300 Terrace Street NE , Albuquerque , New Mexico 87131 , United States.
Molecular Pharmaceutics
|January 3, 2019
Summary
Macrocyclic peptidomimetics can target RNA, offering a new approach for cancer therapy. Researchers identified a compound that inhibits the oncogenic microRNA-155 (miR-155), leading to cancer cell death.
Area of Science:
- Biochemistry
- Molecular Biology
- Medicinal Chemistry
Background:
- MicroRNA-155 (miR-155) is implicated in cancer development and is a potential therapeutic target.
- Developing small molecules to target RNA is challenging.
- Peptidomimetics are established ligands for proteins but underexplored for RNA targeting.
Purpose of the Study:
- To explore macrocyclic peptidomimetics as a novel scaffold for RNA targeting.
- To identify specific inhibitors of oncogenic miR-155 maturation.
Main Methods:
- Design and synthesis of a large library (320,000 compounds) of macrocyclic peptidomimetics.
- Affinity-based screening to identify RNA binders.
- In vitro and cellular assays to assess inhibition of miR-155 maturation and cancer cell apoptosis.
Main Results:
- Identification of a novel macrocyclic peptidomimetic that binds to pre-miR-155.
- Demonstration that the identified compound inhibits miR-155 maturation in vitro and in cancer cells.
- Induction of cancer cell apoptosis by the peptidomimetic compound.
Conclusions:
- Macrocyclic peptidomimetics represent a promising new scaffold for RNA-targeted therapeutics.
- This study validates a novel strategy for discovering RNA-targeting small molecules.
- The identified miR-155 inhibitor offers potential for anticancer drug development.
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