Title : The enantiomer of progesterone (ent-progesterone) is a competitive inhibitor of human cytochromes P450c17 and P450c21.

Pub. Date : 2003 Jan 1

PMID : 12464252






5 Functional Relationships(s)
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1 The enantiomer of progesterone (ent-progesterone) is a competitive inhibitor of human cytochromes P450c17 and P450c21. ent-progesterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
2 To probe the active site topologies of these related enzymes, we synthesized the enantiomer of progesterone and determined if ent-progesterone is a substrate or inhibitor of CYP17 and CYP21. ent-progesterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
3 Neither enzyme metabolizes ent-progesterone; however, ent-progesterone is a potent competitive inhibitor of CYP17 (K(I)=0.2 microM). ent-progesterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
4 Neither enzyme metabolizes ent-progesterone; however, ent-progesterone is a potent competitive inhibitor of CYP17 (K(I)=0.2 microM). ent-progesterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
5 We conclude that CYP17 accommodates the stereochemically unnatural ent-progesterone better than CYP21. ent-progesterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens