The Development of tooth similar to other organs is controlled by sequential and reciprocal molecular interactions. Early studies on tooth development were primarily focused on morphological observations. Recently, due to dramatic advancement of cellular and molecular biotechnology, molecular mechanisms concerning regulation of tooth development have been studied extensively while not been integrated very well. The purpose of the present paper is to summarize the molecular mechanisms of tooth development. Molecular mechanisms of cement genesis and periodontal development and how to use these knowledge and tissue engineering techniques to facilitate periodontal regeneration will be discussed in the next paper.