Agonist-receptor efficacy. II. Agonist trafficking of receptor signals - PubMed (original) (raw)

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Agonist-receptor efficacy. II. Agonist trafficking of receptor signals

T Kenakin. Trends Pharmacol Sci. 1995 Jul.

Abstract

There is evidence to suggest that receptors with seven transmembrane domains can exist in G protein-activating conformations. It is not known how many activated receptor forms exist for each receptor. Furthermore, if there are multiple forms, does the chemical structure of the agonist determine which form dominates, and therefore, which response pathway is activated? This latter scheme is referred to as agonist-receptor trafficking, and is discussed in this, the second of two articles by Terry Kenakin. One way to approach these questions is to study receptors that couple to more than one G protein and, in essence, to try to allow the G protein to indicate the receptor state.

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• Conformational induction versus conformational selection: evidence from allosteric enhancers.
  Bruns RF. Bruns RF. Trends Pharmacol Sci. 1996 May;17(5):189; discussion 190-1. doi: 10.1016/0165-6147(96)20027-6. Trends Pharmacol Sci. 1996. PMID: 8669125 No abstract available.

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