Recent studies strongly suggest that receptors for nicotine play a significant role in lung cancer predisposition and natural history. These data give a new thrust to research efforts assessing the potential curative (antitumor) value of natural compounds that are well-known powerful antagonists to this family of molecules. Recent studies have shown that alpha 7 is the main nicotine acetylcholine receptor (nAChR) subunit that mediates the proliferative effects of nicotine in cancer cells. As a result, alpha 7 nAChR might be a valuable molecular target for therapy of cancers such as lung cancer and mesothelioma. Future studies involving the design of nAChR antagonists with improved selectivity might identify novel strategies for the treatment of tobacco-related cancers.