Conformational changes and drug action

Fed Proc. 1981 Nov;40(13):2723-8.


Conformational changes induced or selected by drugs in receptors may be coupled to second sites on receptor molecules giving negative or positive cooperative binding. The structure-activity relationships may be changed depending on the predominant conformation. Some conformational changes can be identified by nuclear magnetic resonance spectroscopy. Conformational coupling between subunits is complex and provides a mechanism for modulation of receptor affinity.

MeSH terms

  • Animals
  • Binding Sites
  • Histidine / analysis
  • Humans
  • Kinetics
  • Magnetic Resonance Spectroscopy
  • NADP
  • Protein Binding
  • Protein Conformation
  • Receptors, Drug / drug effects
  • Receptors, Drug / metabolism*
  • Structure-Activity Relationship
  • Tetrahydrofolate Dehydrogenase / metabolism


  • Receptors, Drug
  • Histidine
  • NADP
  • Tetrahydrofolate Dehydrogenase