Mechanism based inhibition of hydroxysteroid dehydrogenases.
Steroid hormone action can be regulated not only at the receptor level but also by the enzymes that are responsible for the synthesis and degradation of biologically active steroids. Traditionally the pharmacological intervention of steroid hormone action has focused on the development of steroidal and nonsteroidal hormone receptor agonists and antagonists with appropriate pharmacokinetics. Recently, the development of selective inhibitors/inactivators of steroid metabolizing enzymes has gained momentum. This review will concentrate on the development of mechanism-based inhibitors for one class of steroid hormone transforming enzymes, the hydroxysteroid dehydrogenases.
Penning
T M
TM
Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia 19104-6084.
Ricigliano
J W
JW
D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005260:Female; D006801:Humans; D006913:Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007700:Kinetics; D008297:Male; D008322:Mammals; D008962:Models, Theoretical; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors / Q000502:physiology; D013256:Steroids / Q000378:metabolism / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D011956:Receptors, Cell Surface; D013256:Steroids; D006913:Hydroxysteroid Dehydrogenases