Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). Both phenomena exploit topographically distinct binding sites to promote unique GPCR conformations that can lead to diff...

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Detalhes bibliográficos
Main Authors: Valant, Celine, May, Lauren T., Aurelio, Luigi, Chuo, Chung Hui, White, Paul J., Baltos, Jo-Anne, Sexton, Patrick M., Scammells, Peter J., Christopoulos, Arthur
Formato: Artigo
Idioma:Inglês
Publicado em: National Academy of Sciences 2014
Assuntos:
Biological Sciences
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3970544/
https://ncbi.nlm.nih.gov/pubmed/24619092
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1320962111
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