Conformational induction versus conformational selection: evidence from allosteric enhancers

Article Abstract:

Receptor activation by agonist can take the form of conformational induction where the agonist activates the receptor by forcing a conformational change in the receptor or by conformational selection where an agonist binds to a suddenly active site in the receptor. Bruns' study of allosteric enhancers showed only conformational induction as responsible for receptor activation. Kenakin's response reasoned that reaction dynamics or energy landscape evaluation can show that receptor response may take the form of induction or selection, as 'extremes' of the same activation mechanism.

Cellular signal transduction, Enzyme kinetics, Protein conformation

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Agonist-specific receptor conformations

Article Abstract:

The concept of receptor proteins traveling an energy landscape for the adoption of several protein confirmations is explained. Some protein agonists 'traffic' stimulus to various G proteins indicating agonist selectivity in therapeutics. Also, evidence exists regarding ligands' production of conformations not exhibited as a physiological reaction. A better understanding of the energy landscape spectrum can be explained through the unitary probabilistic concept of allosteric transition. With this concept, stimulus trafficking is better visualized.

Cell receptors, G proteins, Allosteric proteins

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Pharmacological proteus?

Article Abstract:

The knowledge of constitutively active receptor systems and studies of inverse agonism has raised the possibility of detecting a new class of ligand. Under such a possibility, inverse agonism may be observed. Research will be dependent upon system parameters where there is conceivable formation of the activated receptor state. Inverse agonism will result once conversion to the inactivated receptor form is observed.

Radioligand assay

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