Article
Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the beta(2)-adrenergic receptor.
British journal of pharmacology - 1 Apr 2002
Del Carmine Renata, Ambrosio Caterina, Sbraccia Maria, Cotecchia Susanna, Ijzerman Adriaan P, Costa Tommaso
Abstract excerpt
1. We compared the changes in binding energy generated by two mutations that shift in divergent directions the constitutive activity of the human beta(2) adrenergic receptor (beta(2)AR). 2. A constitutively activating mutant (CAM) and the double alanine replacement (AA mutant) of catechol-binding serines (S204A, S207A) in helix 5 were stably expressed in CHO cell lines, and used to measure the binding affinities...
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