The three binding domain model of adenosine receptors: molecular modeling aspects

J Med Chem. 1992 Jan 24;35(2):211-6. doi: 10.1021/jm00080a002.

Abstract

Using molecular modeling, adenosine receptor ligands were fitted together to maximize correlations between the three most important factors controlling binding to the receptor, namely steric, hydrophobic, and electrostatic complimentarily. Structure-activity relationships can be explained by three binding domains on the receptors. These are hydrophobic, aromatic, and ribose binding domains. We propose that the N6, C2, and C8 hydrophobic binding domains are not discreet but occupy the same region of the receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives
  • Adenosine / chemistry
  • Adenosine / metabolism
  • Ligands
  • Models, Molecular
  • Molecular Conformation
  • Receptors, Purinergic / metabolism*
  • Structure-Activity Relationship
  • Xanthines / chemistry
  • Xanthines / metabolism

Substances

  • Ligands
  • Receptors, Purinergic
  • Xanthines
  • Adenosine