Structure-Activity Relationships for Non-Steroidal Inhibitors of Aromatase

Abstract A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.

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Bibliographische Detailangaben
Veröffentlicht in:	Journal of enzyme inhibition 1988, Vol.2 (3), p.215-229
Hauptverfasser:	Banting, L., Smith, H. J., James, M., Jones, G., Nazareth, W., Nicholls, P. J., Hewlins, M. J. E., Rowlands, M. G.
Format:	Artikel
Sprache:	eng
Schlagworte:	aminoglutethimide androsten-dedione Androstenedione - analogs & derivatives Androstenedione - chemical synthesis Androstenedione - pharmacology Aromatase Aromatase Inhibitors Binding Sites Cholesterol Side-Chain Cleavage Enzyme - antagonists & inhibitors Computer Simulation Female Humans Kinetics Models, Molecular Molecular Conformation Molecular Structure Placenta - enzymology Pregnancy reversible inhibitors structure-activity Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Abstract A model is described for the binding of non-steroidal inhibitors of aromatase to the enzyme with interaction of a ligand with the Fe3+-haem of the cytochrome. The model suggests that the inhibitors utilise a common binding site with ring A of the steroidal substrates.
ISSN:	1475-6366 8755-5093 1475-6374
DOI:	10.3109/14756368809040728