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Perfluoroalkyl substances (PFASs) have been distributed in environment and human body worldwide. Due to their bioaccumulative and multiple organ toxic, these compounds have raised more and more attention in recent years. The precursors of PFASs can be metabolized to PFASs both in environment and human body, which makes an important contribution to human body burdens. Apart from transformation into PFASs, some of these precursors themselves or their metabolic intermediates also have toxicity effects, such as estrogen-like properties, protein binding, cytotoxicity and so on, and there might be a potential harmful impact on human health. In this paper, the toxicity and biotransformation of PFASs and their precursors were introduced briefly.