Small-molecule approaches toward the targeting of oncogenic miRNAs: roadmap for the discovery of RNA modulators

miRNAs are a recently discovered class of small noncoding RNAs implicated in the regulation of gene expression. The deregulation of miRNAs levels has been linked to the development of various cancers where oncogenic miRNAs are overexpressed and tumor suppressor miRNAs are underexpressed. Here we rep...

Full description

Saved in:
Bibliographic Details
Published in:Future medicinal chemistry 2016-05, Vol.8 (7), p.803-816
Main Authors: Di Giorgio, Audrey, Tran, Thi Phuong Anh, Duca, Maria
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Chemical Sciences
Drug Screening Assays, Antitumor
Gene Expression
High-Throughput Screening Assays
Humans
Ligands
Medicinal Chemistry
MicroRNAs - antagonists & inhibitors
MicroRNAs - metabolism
Molecular Targeted Therapy
Neoplasms - drug therapy
Neoplasms - genetics
Neoplasms - metabolism
Small Molecule Libraries - chemistry
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:miRNAs are a recently discovered class of small noncoding RNAs implicated in the regulation of gene expression. The deregulation of miRNAs levels has been linked to the development of various cancers where oncogenic miRNAs are overexpressed and tumor suppressor miRNAs are underexpressed. Here we report the three main strategies developed in order to discover small-molecule drugs able to selectively interfere with oncogenic miRNAs: the high throughput screening of large libraries of compounds, the focused screening of small libraries of molecules that are known to be able to interact with RNA thus being supposed modulators of miRNAs pathway and the design of small molecules based on the secondary structure of targeted RNA and/or three-dimensional structure of enzymes involved in miRNAs pathway.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2016-0018