Aromatase, estrone sulfatase, and 17β-hydroxysteroid dehydrogenase: structure-function studies and inhibitor development

Mol Cell Endocrinol. 2011 Jul 4;340(2):120-6. doi: 10.1016/j.mce.2010.09.012. Epub 2010 Oct 1.

Abstract

Aromatase, estrone sulfatase, and 17β-hydroxysteroid dehydrogenase type 1 are involved in the key steps of 17β-estradiol biosynthesis. Structure-function studies of aromatase, estrone sulfatase and 17β-hydroxysteroid dehydrogenase type 1 are important to evaluate the molecular basis of the interaction between these enzymes and their inhibitors. Selective and potent inhibitors of the three enzymes have been developed as antiproliferative agents in hormone-dependent breast carcinoma. New treatment strategies for hormone-dependent breast cancer are discussed.

Publication types

  • Review

MeSH terms

  • 17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
  • 17-Hydroxysteroid Dehydrogenases / chemistry
  • Animals
  • Aromatase / chemistry
  • Aromatase / metabolism*
  • Drug Design*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Structure-Activity Relationship
  • Sulfatases / antagonists & inhibitors*
  • Sulfatases / chemistry
  • Sulfatases / metabolism

Substances

  • Enzyme Inhibitors
  • 17-Hydroxysteroid Dehydrogenases
  • 3 (or 17)-beta-hydroxysteroid dehydrogenase
  • Aromatase
  • Sulfatases
  • estrone sulfatase