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MicroRNAs (miRNAs) are short, non-coding RNA molecules that regulate gene expression by translational repression or deregulating of messenger RNAs. Accumulating evidence suggests miRNAs play various roles in the development and progression of lung cancers. Although their precise roles in targeted cancer therapy are currently unclear, miRNAs have been shown to affect the sensitivity of tumors to anticancer drugs. A large number of recent studies have demonstrated that some anticancer drugs
exerted antitumor activities by affecting the expression of miRNAs and their targeted genes. These studies have elucidated the specific biological mechanism of drugs in tumor suppression, which provides a new idea or basis for their clinical application. In this review, we summarized the therapeutic mechanisms of drugs in lung cancer therapy through their effects on miRNAs and their targeted genes, which highlights the roles of miRNAs as targets in lung cancer therapy.