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Fig. 1 | Genes and Environment

Fig. 1

From: Development of novel and safer anti-breast cancer agents, SS1020 and SS5020, based on a fundamental carcinogenic research

Fig. 1

Genotoxic mechanisms of tamoxifen, not toremifene, via metabolic activation. TAM (a) proceeds four steps leading to genotoxicity which are 1) α-hydroxylation by cytochrome p450, 2) sulfonation by sulfotransferase (SULT), and 3) formation of carbocation to react with DNA, particularly with 2′-deoxyguanosine (dG) [11]. In contrast, TOR (b) is also hydroxylated at α-position. However, this metabolite is not a good substrate for sulfotransferases because of steric hindrance of bulky chloride atom [14]. As a result, toremifene doesn’t produce stable DNA adducts

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