GPCR-MAPS: high-resolution functional and allosteric mapping of G-protein-coupled receptor activation functions and bias.

GPCR-MAPS generated over 7,500 dose-response curves for the β2 adrenergic receptor, revealing a modular activation architecture with a core network plus residues shaping quantitative parameters and bias.

• Why it matters: Precision GPCR therapeutics need high-resolution functional and allosteric annotations, but current structure-to-function mapping is limited, especially for allosteric modulation and biased signaling beyond the orthosteric site.
• What they did: The approach builds multimodal functional and allosteric maps by quantifying direct protein recruitment and deconvolving amino-acid substitution effects on receptor expression, then applying it to the β2 adrenergic receptor.
• The result: Using the resulting maps, the study identified multiple allosteric surface pockets and suggests that applying GPCR-MAPS across the GPCR superfamily could support rational design of precision GPCR therapeutics.

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