Three-dimensional model of cytochrome P450 human aromatase

J Enzyme Inhib Med Chem. 2005 Dec;20(6):581-5. doi: 10.1080/14756360500220574.

Abstract

A three-dimensional (3-D) structure of human aromatase (CYP 19) was modeled on the basis of the crystal structure of rabbit CYP2C5, the first solved X-ray structure of an eukaryotic cytochrome P450 and was evaluated by docking S-fadrozole and the steroidal competitive inhibitor (19R)-10-thiiranylestr-4-ene-3,17-dione, into the enzyme active site. According to a previous pharmacophoric hypothesis described in the literature, the cyano group of S-fadrozole partially mimics the steroid backbone C(17) carbonyl group of (19R)-10-thiiranylestr-4-ene-3,17-dione, and was oriented in a favorable position for H-bonding with the newly identified positively charged residues Lys 119 and Arg435. In addition, this model is consistent with the recent combined mutagenesis/modeling studies already published concerning the roles ofAsp309 and His480 in the aromatization of the steroid A ring.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Aromatase / chemistry*
  • Aromatase / drug effects
  • Binding Sites / drug effects
  • Binding, Competitive
  • Crystallography, X-Ray
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Estrenes / chemistry*
  • Estrenes / pharmacology
  • Fadrozole / chemistry*
  • Fadrozole / pharmacology
  • Humans
  • Hydrogen Bonding
  • Models, Molecular*
  • Molecular Sequence Data
  • Molecular Structure
  • Rabbits
  • Sequence Alignment
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Estrenes
  • 10-thiirane-4-estrene-3,17-dione
  • Aromatase
  • Fadrozole