The use of the novel substrate-heme complex approach in the derivation of a representation of the active site of the enzyme cholesterol side chain cleavage.
The previously reported substrate-heme complex approach is used to study the binding of type II inhibitors of the enzyme cholesterol side chain cleavage (CSCC), a cytochrome P-450 dependent enzyme involved in the oxidative cleaveage of the C(20)-C(22) bond of cholesterol. Using the derived model, we have rationalised the inhibitory activity of a number of compounds including aminoglutethimide and pyridoglutethimide and the enantiomers of ketoconazole.
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, Kingston upon Thames, KT1 2EE, United Kingdom. S.AHMED@KINGSTON.AC.UK
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D000818:Animals; D002784:Cholesterol / Q000378:metabolism*; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D006418:Heme / Q000378:metabolism; D006801:Humans; D010084:Oxidation-Reduction; D013379:Substrate Specificity
D006418:Heme; D003577:Cytochrome P-450 Enzyme System; D002784:Cholesterol