Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 81, Issue -, Pages 104-116Publisher
ELSEVIER
DOI: 10.1016/j.addr.2014.09.002
Keywords
MicroRNAs; Small molecules; Targeted therapies; Non-coding RNAs; Cancer
Categories
Funding
- NIH/NCI [1UH2TR00943-01, 1 R01 CA182905-01]
- Developmental Research Awards in Prostate Cancer, Multiple Myeloma, Leukemia [P50 CA100632]
- Head and Neck SPOREs [P50 CA097007]
- SINF MDACC_DKFZ grant in CLL
- SINF grant in colon cancer
- Kidney Cancer Pilot Project
- Duncan Family Institutional Seed Funds
- Blanton-Davis Ovarian Cancer
- Laura and John Arnold Foundation
- RGK Foundation
- Estate of C. G. Johnson, Jr
- CLL Global Research Foundation
- Department of Defense Breast Cancer Idea Award
- Direct For Mathematical & Physical Scien
- Division Of Chemistry [1411859] Funding Source: National Science Foundation
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One of the most fascinating discoveries in molecular oncology has been that cancer represents a disease in which genetic alterations in protein-coding, but also in non-coding genes complement each other. MicroRNAs (miRNAs) are a type of non-coding RNA (ncRNA) transcripts that can regulate gene expression primarily by disrupting messenger RNA (mRNA) translation and/or stability, or alternatively by modulating the transcription of target mRNAs. For the last decade, miRNAs have shown to be pivotal characters of every single one of the cancer hallmarks. Profiling studies have proven the significance of identifying over-expressed miRNAs (oncomiRs) causative of the activation of oncogenic pathways that lead to malignancy. Due to their crucial role in cancer, it has become a challenge to develop efficient miRNA-inhibiting strategies such as antagomiRs, locked nucleic acids or antisense oligonucleotides. However, to this date, the accessible delivery agents and their pharmacokinetic/ pharmacodynamic properties are not ideal. Thus there is an urgent, unmet need to develop miRNA-based inhibitory therapeutics. Herein we present a novel therapeutic strategy that is only at the tip of the iceberg: the use of small molecule inhibitors to target specific miRNAs (SMIRs). Furthermore we describe several high-throughput techniques to screen for SMIRs both in vitro and in silico. Finally we take you through the journey that has led to discovering the handful of SMIRs that have been validated to this date. Published by Elsevier B.V.
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