Agonist-Directed Desensitization of the β2-Adrenergic Receptor
作者： Vasiliy Goral , Yan Jin , Haiyan Sun , Ann M. Ferrie , Qi Wu
DOI: 10.1371/JOURNAL.PONE.0019282
关键词:
摘要: The β2-adrenergic receptor (β2AR) agonists with reduced tachyphylaxis may offer new therapeutic agents improved tolerance profile. However, desensitization assays are often inferred at the single signaling molecule level, thus ligand-directed is poorly understood. Here we report a label-free biosensor whole cell assay microfluidics to determine of β2AR. Together mechanistic deconvolution using small inhibitors, and resensitization patterns under short-term agonist exposure manifested long-acting agonism salmeterol, differentiated mechanisms agonist-directed between full epinephrine partial pindolol. This study reveals cellular agonist-selective β2AR level.
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