Molecular mechanism of 7TM receptor activation--a global toggle switch model.

  title={Molecular mechanism of 7TM receptor activation--a global toggle switch model.},
  author={Thue W. Schwartz and Thomas M. Frimurer and Birgitte Holst and Mette Marie Rosenkilde and Christian E. Elling},
  journal={Annual review of pharmacology and toxicology},
The multitude of chemically highly different agonists for 7TM receptors apparently do not share a common binding mode or active site but nevertheless act through induction of a common molecular activation mechanism. A global toggle switch model is proposed for this activation mechanism to reconcile the accumulated biophysical data supporting an outward rigid-body movement of the intracellular segments, as well as the recent data derived from activating metal ion sites and tethered ligands… CONTINUE READING
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