The HIV-1 Rev protein, which traffics through nucleolus and shuttles between nucleus and cytoplasm, facilitates export of unspliced and singly spliced viral transcripts containing RRE RNA by the CRM1 export pathway. Inhibitions of the various stages of Rev-mediated RNA transport can arrest HIV-1 transcriptional process. The current understanding to the mechanism of Rev function, Rev-RRE interaction, as well as inhibitors hereof is reviewed.