microRNAs (miRNAs) are a novel class of endogenous small non-coding RNAs which can regulate gene expression at the post-transcriptional level. The wide regulatory functions of miRNAs make them attractive biomarkers as well as therapeutic targets for various diseases. In recent years, miRNAs are emerging as novel endogenous targets for chemical biological studies. We are now collaborating with Prof. Chenyu Zhang’s group to investigate miRNA-involved cellular processes with corresponding multi-functional probes. Through using the probes based on oligonucleotides or small molecules that can regulate endogenous miRNAs, we have developed a novel strategy for intracellular target identification of miRNAs and revealed a novel signaling transduction pathway in muscle cells (J. Am. Chem. Soc. 2016, 138, 15943; Chem. Biol. 2014, 21, 1265; Chem. Soc. Rev., 2014, 43, 506).