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

Abstract excerpt

G protein-coupled receptors (GPCRs) are the largest family of human receptors and drug targets, but how the signaling properties of receptors are encoded in their sequence is incompletely understood. Most GPCR drugs bind a conserved orthosteric pocket, which can result in non-specificity, toxicity and clinical failure. Precision modalities including biased signaling and allosteric modulation could lead to GPCR the...

Topics

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• Adrenergic beta-Agonists
• Cluster Analysis
• Evolution, Molecular
• GTP-Binding Proteins
• HEK293 Cells
• Isoproterenol
• Protein Domains
• Receptors, Adrenergic, beta-2

Identifiers and source

Literature Corpus work

b53594eb-9457-5067-9e84-e4161470fb22

DOI

10.1101/2025.05.30.656974