Cytochrome P450 monooxygenases inhibitors

Baudry J, Li W, Pan L, et al. Molecular docking of substrates and inhibitors in the catalytic site of CYP6B1, an insect cytochrome p450 monooxygenase. Protein Eng 2003 16 577-587. 

Figure 42 A hypothetical pathway for the novel branching inhibitor. Carotenoid cleavage dioxygenases (CCDs) and a cytochrome P450 monooxygenase (P450) are required for the synthesis of this novel hormone, whereas an F-box protein is probably involved in the perception or transduction of the hormonal signal.

Organophosphate insecticides with the P=S group are oxidatively desulfurated by cytochrome P450 monooxygenases of insects to their corresponding P=0 analogs. This reaction results in activation (increased toxicity), because the product, P=0, binds more tightly to the acetylcholinesterase than the parent compound and, thus, to more potent acetylcholinesterase inhibitors. For example, parathion is oxidatively desulfurated to paraoxon. 

SerizawaN, MatsuokaT (1991) A two component-type cytochrome P450 monooxygenase system in a prokaryote that catalyzes hydroxylation of ML-236B to pravastatin, a tissue-seleetive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase. Biochim BiophysActa 1084 35-40... 

K.J. McLean, K.R. Marshall, A. Richmond, l.S. Hunter, K. Fowler, T. Kieser, S.S. Gurcha, G.S. Besra, A.W. Munro, Azole antifungals are potent inhibitors of cytochrome P450 monooxygenases and bacterial growth in mycobacteria and stieptomycetes. Microbiology 148 (2002)... 

Proton Pump Inhibitors and Acid Pump Antagonists retinoid X receptor (RXR) and is also activated by various lipophilic compounds produced by the body such as bile acids and steroids. PXR heterodimerized with RXR stimulates the transcription of cytochrome P450 3A monooxygenases (CYP3A) and other genes involved in the detoxification and elimination of the... 

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