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Issue 6, 2015
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Insights into a defined secondary binding region on β-adrenoceptors and putative roles in ligand binding and drug design

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Abstract

Increasing evidence points to the possibility of one or more secondary binding sites being involved in the interaction of catecholamines on their receptors. However, the importance of these sites has not yet been clearly established. In this review, we examine the possibility that catecholamines reach a defined secondary binding region on beta adrenoceptors attempting to analyze the approach of these ligands to this binding site. Inferences are made as to the possible effects on receptor activity when a compound interacts with the orthosteric binding site, the secondary binding region, or both in a concerted manner. Consideration is given to prolonged ligand interaction with orthosteric and allosteric binding sites, biased signaling, and feasible cellular responses, as well as to the importance of these effects in physiological processes when these receptors are targets for drug design.

Graphical abstract: Insights into a defined secondary binding region on β-adrenoceptors and putative roles in ligand binding and drug design

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Publication details

The article was received on 10 Jan 2015, accepted on 09 Mar 2015 and first published on 12 Mar 2015


Article type: Review Article
DOI: 10.1039/C5MD00011D
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Citation: Med. Chem. Commun., 2015,6, 991-1002
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    Insights into a defined secondary binding region on β-adrenoceptors and putative roles in ligand binding and drug design

    M. A. Soriano-Ursúa, J. G. Trujillo-Ferrara, J. A. Arias-Montaño and R. Villalobos-Molina, Med. Chem. Commun., 2015, 6, 991
    DOI: 10.1039/C5MD00011D

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