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Investigate direct functional interactions and reciprocal ligand binding modulation between purified bovine brain A1-adenosine receptors and purified Go,i G-proteins.

May 1, 1991Biochemical JournalOpen Access

Interactions of purified bovine brain A1-adenosine receptors with G-proteins. Reciprocal modulation of agonist and antagonist binding

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Authors

MFMichael FreissmuthPharmacology Research Institute ESEdgar SelzerÇanakkale Onsekiz Mart Üniversitesi WSWolfgang SchützUniversity of Vienna

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Implication

In vitro study reveals reciprocal ligand modulation of purified brain A1-adenosine receptors by G-proteins, indicating coupling occurs directly in detergent solution.

Key Points

Investigate direct functional interactions and reciprocal ligand binding modulation between purified bovine brain A1-adenosine receptors and purified Go,i G-proteins.
Purified bovine brain A1-adenosine receptors 8000-fold using xanthine-amine-congener (XAC)-Sepharose affinity chromatography.
Assayed agonist and antagonist binding alongside GTP[35S] binding in both detergent solution and reconstituted phospholipid vesicles in the presence of varying Go,i concentrations.
Addition of a 120-fold molar excess of Go,i decreased antagonist [3H]XAC binding capacity in detergent and vesicles, an effect reversed by GTP analogues.
Go,i induced guanine-nucleotide-sensitive high-affinity agonist binding in approximately 20% of receptors in lipid vesicles and 40% in detergent, exhibiting half-maximal modulation at a 10-fold molar excess.
Receptors accelerated GTP[35S] binding to Go,i; this rate was further enhanced by agonist activation and reduced by antagonist binding to baseline levels.

Cite This Study

Freissmuth et al. (1991) studied this question.

synapsesocial.com/papers/6a659b29eb7a5bf67ec4d5e2 https://doi.org/10.1042/bj2750651

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Implication

In vitro study reveals reciprocal ligand modulation of purified brain A1-adenosine receptors by G-proteins, indicating coupling occurs directly in detergent solution.

Interactions of purified bovine brain A1-adenosine receptors with G-proteins. Reciprocal modulation of agonist and antagonist binding

Discussion

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Implication

Key Points

Cite This Study

Interactions of purified bovine brain A1-adenosine receptors with G-proteins. Reciprocal modulation of agonist and antagonist binding

Discussion

Member takes

Implication

Key Points

Cite This Study

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