Literature DB >> 38405

Fundamental difference between the molecular interactions of agonists and antagonists with the beta-adrenergic receptor.

G A Weiland, K P Minneman, P B Molinoff.   

Abstract

Antagonist binding to the beta-adrenergic receptor is largely entropy driven, with only a small enthalpy component. The binding of agonists, on the other hand, is associated with a large decrease in enthalpy which permits a highly unfavourable decrease in entropy. The thermodynamic differences between the binding of agonists and antagonists may provide new insights into the molecular basis for hormone stimulation of adenylate cyclase activity.

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Year:  1979        PMID： 38405     DOI： 10.1038/281114a0

Source DB:  PubMed          Journal:  Nature        ISSN： 0028-0836            Impact factor:   49.962


  39 in total

1.  Thermodynamically distinct high and low affinity states of the A(1) adenosine receptor induced by G protein coupling and guanine nucleotide ligation states of G proteins.

Authors:  A Lorenzen; L Guerra; F Campi; H Lang; U Schwabe; P A Borea
Journal:  Br J Pharmacol       Date:  2000-06       Impact factor: 8.739

2.  Thermodynamic assessment of the stability of thrombin receptor antagonistic peptides in hydrophobic environments.

Authors:  Reinhard I Boysen; Agnes J O Jong; Milton T W Hearn
Journal:  Biophys J       Date:  2002-05       Impact factor: 4.033

3.  Agonist-induced conformational changes in the G-protein-coupling domain of the beta 2 adrenergic receptor.

Authors:  P Ghanouni; J J Steenhuis; D L Farrens; B K Kobilka
Journal:  Proc Natl Acad Sci U S A       Date:  2001-05-15       Impact factor: 11.205

4.  A rhodopsin exhibiting binding ability to agonist all-trans-retinal.

Authors:  Hisao Tsukamoto; Akihisa Terakita; Yoshinori Shichida
Journal:  Proc Natl Acad Sci U S A       Date:  2005-04-25       Impact factor: 11.205

5.  Thermodynamic analysis of ligands at cholecystokinin CCK2 receptors in rat cerebral cortex.

Authors:  E A Harper; S P Roberts; S B Kalindjian
Journal:  Br J Pharmacol       Date:  2007-06-25       Impact factor: 8.739

6.  On the stability of nucleic acid structures in solution: enthalpy-entropy compensations, internal rotations and reversibility.

Authors:  M S Searle; D H Williams
Journal:  Nucleic Acids Res       Date:  1993-05-11       Impact factor: 16.971

7.  Partial agonism of theophylline-7-riboside on adenosine receptors.

Authors:  A P IJzerman; E M van der Wenden; J K von Frijtag Drabbe Künzel; R A Mathôt; M Danhof; P A Borea; K Varani
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-12       Impact factor: 3.000

8.  Temperature related effects on the binding characteristics of beta-adrenergic receptor agonists and antagonists by rabbit lung.

Authors:  R J Altiere; J S Douglas; C N Gillis
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1981-07       Impact factor: 3.000

9.  Thermodynamics of antagonist binding to rat muscarinic M2 receptors: antimuscarinics of the pridinol, sila-pridinol, diphenidol and sila-diphenidol type.

Authors:  M Waelbroeck; J Camus; M Tastenoy; G Lambrecht; E Mutschler; M Kropfgans; J Sperlich; F Wiesenberger; R Tacke; J Christophe
Journal:  Br J Pharmacol       Date:  1993-06       Impact factor: 8.739

10.  Influence of the beta-adrenergic receptor concentration on functional coupling to the adenylate cyclase system.

Authors:  Y Severne; D Coppens; S Bottari; M Riviere; R Kram; G Vauquelin
Journal:  Proc Natl Acad Sci U S A       Date:  1984-08       Impact factor: 11.205
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