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Human hydroxysteroid dehydrogenases and pre-receptor regulation: insights into inhibitor design and evaluation.


ABSTRACT: Hydroxysteroid dehydrogenases (HSDs) represent a major class of NAD(P)(H) dependent steroid hormone oxidoreductases involved in the pre-receptor regulation of hormone action. This is achieved by HSDs working in pairs so that they can interconvert ketosteroids with hydroxysteroids resulting in a change in ligand potency for nuclear receptors. HSDs belong to two protein superfamilies the aldo-keto reductases and the short-chain dehydrogenase/reductases. In humans, many of the important enzymes have been thoroughly characterized including the elucidation of their three-dimensional structures. Because these enzymes play fundamental roles in steroid hormone action they can be considered to be drug targets for a variety of steroid driven diseases, e.g. metabolic syndrome and obesity, inflammatio

SUBMITTER: Penning TM 

PROVIDER: S-EPMC3104102 | biostudies-literature | 2011 May

REPOSITORIES: biostudies-literature