Dynamic ligand binding dictates partial agonism at a G protein–coupled receptor

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Agonists with supraphysiological efficacy at the muscarinic M2ACh receptor

(2012) R Schrage et al.   BRITISH JOURNAL OF PHARMACOLOGY

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

(2012) Andreas Bock et al.   Nature Communications

Efficacy of the β2-adrenergic receptor is determined by conformational equilibrium in the transmembrane region

(2012) Yutaka Kofuku et al.   Nature Communications

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Applying label-free dynamic mass redistribution technology to frame signaling of G protein–coupled receptors noninvasively in living cells

(2011) Ralf Schröder et al.   Nature Protocols

Deconvolution of complex G protein–coupled receptor signaling in live cells using dynamic mass redistribution measurements

(2010) Ralf Schröder et al.   NATURE BIOTECHNOLOGY

Coupling of receptor conformation and ligand orientation determine graded activity

(2010) John B Bruning et al.   Nature Chemical Biology

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Convergent, short synthesis of the muscarinic superagonist iperoxo

(2010) Jessica Kloeckner et al.   TETRAHEDRON LETTERS

The structure and function of G-protein-coupled receptors

(2009) Daniel M. Rosenbaum et al.   NATURE

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

(2008) Johannes Antony et al.   FASEB JOURNAL

Fluorescence Resonance Energy Transfer Analysis of  2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes

(2008) A. Zurn et al.   MOLECULAR PHARMACOLOGY