Biased Signaling in Mutated Variants ofβ2-Adrenergic Receptor: Insights from Molecular Dynamics Simulations
Midhun K. Madhu,
Kunal Shewani,
Rajesh K. Murarka
Abstract:The molecular basis of receptor bias in G protein-coupled receptors (GPCRs) caused by mutations that preferentially activate specific intracellular transducers over others remains poorly understood. Two experimentally identified biased variants of β2-adrenergic receptors (β2AR), a prototypical GPCR, are a triple mutant (T68F, Y132A, and Y219A) and a single mutant (Y219A); the former bias the receptor towards the β-arrestin pathway by disfavoring G protein engagement, while the latter induces G protein signalin… Show more
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