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.
Ahmed
S
S
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, Kingston upon Thames, KT1 2EE, United Kingdom. S.AHMED@KINGSTON.AC.UK
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