4.7 Review

Trading places: Peptide and small molecule alternatives to oligonucleotidebased modulation of microRNA expression

Journal

DRUG DISCOVERY TODAY
Volume 27, Issue 11, Pages -

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2022.08.005

Keywords

microRNA; Peptides; Peptidomimetics; Peptide-miRNA interactions; Dicer processing

Funding

  1. Liverpool John Moores University Institute for Health Research PhD scholarship

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This review highlights the advances made in small molecule and peptide inhibitors of miRNA processing, with an emphasis on peptide features that regulate miRNA expression.
It is well established that microRNA (miRNA) dysregulation is involved in the development and progression of various diseases, especially cancer. Emerging evidence suggests that small molecule and peptide agents can interfere with miRNA disease pathways. Despite this, very little is known about structural features that drive drug-miRNA interactions and subsequent inhibition. In this review, we highlight the advances made in the development of small molecule and peptide inhibitors of miRNA processing. Specifically, we attempt to draw attention to peptide features that may be critical for interaction with the miRNA secondary structure to regulate miRNA expression. We hope that this review will help to establish peptides as exciting miRNA expression modulators and will contribute towards the development of the first miRNA-targeting peptide therapy.

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