Kisspeptins are the protein products encoded by KiSS1 gene, an important tumor metastatic suppressor and pivotal master hormone of puberty. Although KiSS1 gene is expressed in both central and peripheral tissues, the molecular mechanisms that determine the temporal and spatial expression of KiSS1 gene are not well understood. This review provides an update on the latest studies and ideas about the expression of KiSS1 gene as a puberty gatekeeper and a metastasis suppressor, with special emphasis on the molecular mechanisms for the transcriptional regulation of KiSS1 gene expression.