Many microRNAs are found to be androgen related, and their deregulation has correlated highly with initiation, progression and prognosis of human cancers. Given the hypothesis that many of the myriad changes can be observed from gene expression profiles of LH-mediated LHR activation in a human ovarian cancer cell line, we applied a large-scale transcriptomic analysis on the cells using an ovarian diseasespecific array. Our present analyses include three major steps: a) comparative analysis on microRNA and mRNA expression in response to LHR expression and activation in SKOV3 cells, b) computational TWS119 Prediction of microRNA/mRNA regulation pairs, in conjunction with experimental validated information and c) functional analysis on target mRNAs to infer the major role of their regulatory microRNA. During the 20 h exposure to LH, a total of 14,903 mRNAs exhibited elevated expression at one of the time points, which extend the above functions to posttranslational modification, RNA processing and modification, intracellular trafficking and secretion, signal transduction mechanisms and coenzyme metabolism, while 10,389 mRNAs were down-regulated, reflecting the cellular defense mechanism. The enriched pathway analysis shows that LHR expression in SKOV3 cells may have a positive impact on cellular gap junctions and relevant growth signaling pathways, while moderately suppressing apoptosis, mismatch repair and the RasIndependent pathway in NK cell-mediated cytotoxicity, which is overall an advantage to cell growth. LH, subsequently, regulated gene expression involved in the cell cycle, p53 and VEGF signaling, gap junction, immune responses and the complement and coagulation cascades, as well as on a few metabolic pathways. The transcriptome expression analysis reflects those pathway alterations that support the phenotypes observed in our previous study, as well as many others. Numerous recent studies have reported that the global expression of microRNAs is deregulated in most cancers, including epithelial ovarian cancer. We present here the first study demonstrating that LH regulates microRNA expression in LHR+ SKOV3 cells. With the continuous exposure of LH to the LHR+ cells, the highly correlated expression patterns observed between differential microRNAs and their target genes affirm the underlying predicted interactions and were then applied for inferring the involvement of microRNA regulation. One advantage of using a disease-specific array is the gathering of highly extensive mRNA data and microRNA information in ovarian cancer on the same chip which largely avoids the technical noise associated with profiling their expression in separate chips. Prediction of microRNA and mRNA regulation pairs is clearly a crucial component in this study, which is mainly through correlation analysis in conjunction with collective computational prediction.