Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A(3) Receptor

[Image: see text] The development of covalent ligands for G protein-coupled receptors (GPCRs) is not a trivial process. Here, we report a streamlined workflow thereto from synthesis to validation, exemplified by the discovery of a covalent antagonist for the human adenosine A(3) receptor (hA(3)AR)....

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Pubblicato in:J Med Chem
Autori principali: Yang, Xue, van Veldhoven, Jacobus P. D., Offringa, Jelle, Kuiper, Boaz J., Lenselink, Eelke B., Heitman, Laura H., van der Es, Daan, IJzerman, Adriaan P.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2019
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC6466477/
https://ncbi.nlm.nih.gov/pubmed/30869893
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b02026
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