Is there a 'lock' for all agonist 'keys' in 7TM receptors?

Article Abstract:

The seven transmembrane domain (7TM) receptors were thought to have a common molecular-activation system as evidenced by the structural similarities of the receptors. Mutational mapping and fluorescence spectroscopy were done to establish the binding site for catecholamines on adrenoceptors. The activating mechanisms were found in the main ligand-binding crevice of the adrenoceptors specifically at the AspIII:08, SerV:09, SerV:12 and PheVI:17. The results indicated a specific 'lock' for each agonist which is not common for all 7TM receptor 'keys.'

Usage, Fluorescence spectroscopy, Catecholamines, Radioligand assay

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Principles of agonism: undressing efficacy

Article Abstract:

The International Union of Pharmacology-sponsored meeting in Merano, Italy, focused on the principles of agonism. The link between efficacy and affinity was one of the conference's primary themes. Both notions are so closely interconnected that they cannot be measured separately. This means that if binding affects activation, then activation must affect binding. The identification of agonist-binding domains should take into account changes in receptor structure.

Conferences, meetings and seminars, Drugs, Cell receptors, Pharmacology, Cooperative binding (Biochemistry), Pharmacologists

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The dual nature of the tachykinin NK(sub 1) receptor

Article Abstract:

The widely-held theory which designated the tachykinin substance P (SP), neurokinin A (NKA) and neurokinin B (NKB) as the preferred ligands of the receptors NK(sub 1), NK(sub 2) and NK(sub 3), respectively, is analyzed. It is argued that in some systems, NKA rather than SP is the preferred ligand for NK(sub 1) receptors while NKB can also exert some of its actions through the NK(sub 1) and NK(sub 3) receptors.

Peptides, Tachykinins

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