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- W3174440103 abstract "The β2-adrenergic receptor (β2AR) is a Gs-coupled receptor that promotes an agonist-dependent cyclic AMP (cAMP)-mediated reversal of bronchoconstriction that is therapeutic for airway diseases like asthma. Long-term use of β-agonists is associated with arrestin mediated desensitization of response to treatment. Gs-biased signaling through the β2AR would have clinical utility in promoting airway relaxation while avoiding desensitization of response to β-agonists. Using bioluminescence resonance energy transfer (BRET) for arrestin recruitment, cAMP ELISAs, radioligand assays, mutagenesis, X-ray crystallography, and ex vivo airway tissue models, we characterized compounds that inhibit arrestin recruitment to the β2AR without inhibiting cAMP production in the presence of β-agonists. Our data reveal a druggable allosteric site in the extracellular vestibule of the β2AR that can be targeted to modulate arrestin recruitment to the receptor without affecting Gs coupling. Here we characterize a small molecule that targets this site to promote β2AR specific, negative allosteric modulation of arrestin recruitment that is protective against agonist-induced desensitization in cells and airway tissue. Support or Funding Information Research funded by NIH training grant GM100836, P01 HL114471, and F31 HL139104. This abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal." @default.
- W3174440103 created "2021-07-05" @default.
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- W3174440103 date "2019-04-01" @default.
- W3174440103 modified "2023-10-16" @default.
- W3174440103 title "Negative Allosteric Modulation of Arrestin Recruitment to the β <sub>2</sub> ‐Adrenergic Receptor" @default.
- W3174440103 doi "https://doi.org/10.1096/fasebj.2019.33.1_supplement.503.15" @default.
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