Insights into the Structure, Function, and Regulation of Human Cytochrome P450 1A2.

Authors: Zhou SF, Chan E, Zhou ZW, Xue CC, Lai X, Duan W
CYP1A2 is one of the major CYPs in human liver ( approximately 13%) and metabolises a variety of clinically important drugs, such as clozapine, lidocaine, theophylline, tacrine, and leflunomide. CYP1A2 is one of the major enzymes that bioactivate a number of procarcinogens and thus induction of CYP1A2 may increase the carcinogenicity of these compounds. This enzyme also metabolizes several important endogenous compounds including steroids, retinols, melatonin, uroporphyrinogen and arachidonic acid. In the recently published crystal structure of CYP1A2 in complex with alpha-naphthoflavone, its compact active site is closed without clear solvent or substrate access channels. Not surprisingly, CYP1A2 has a relatively small volume of…

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