1. G Protein-coupled Receptor Kinases of the GRK4 Protein Subfamily Phosphorylate Inactive G Protein-coupled Receptors (GPCRs).

    Journal of Biological Chemistry 290(17):10775 (2015) PMID 25770216

    G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in homologous desensitization of GPCRs. It is widely assumed that most GRKs selectively phosphorylate only active GPCRs. Here, we show that although this seems to be the case for the GRK2/3 subfamily, GRK5/6 effectively phosphoryla...
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  2. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050 PMCID PMC4260607

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  3. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050 PMCID PMC4260607

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  4. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050 PMCID PMC4260607

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  5. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  6. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  7. Goniometer-based femtosecond crystallography with X-ray free electron lasers.

    PNAS 111(48):17122 (2014) PMID 25362050 PMCID PMC4260607

    The emerging method of femtosecond crystallography (FX) may extend the diffraction resolution accessible from small radiation-sensitive crystals and provides a means to determine catalytically accurate structures of acutely radiation-sensitive metalloenzymes. Automated goniometer-based instrumen...
  8. Covalent agonists for studying G protein-coupled receptor activation.

    PNAS 111(29):10744 (2014) PMID 25006259 PMCID PMC4115510

    Structural studies on G protein-coupled receptors (GPCRs) provide important insights into the architecture and function of these important drug targets. However, the crystallization of GPCRs in active states is particularly challenging, requiring the formation of stable and conformationally homo...
  9. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin

    Current Opinion in Cell Biology 27:136 (2014)

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR)...
  10. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin

    Current Opinion in Cell Biology 27:136 (2014)

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR)...
  11. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin.

    Current Opinion in Cell Biology 27:136 (2014) PMID 24534489 PMCID PMC3986065

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR). Although...
  12. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin.

    Current Opinion in Cell Biology 27:136 (2014) PMID 24534489 PMCID PMC3986065

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR). Although...
  13. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin.

    Current Opinion in Cell Biology 27:136 (2014) PMID 24534489 PMCID PMC3986065

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR). Although...
  14. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin

    Current Opinion in Cell Biology 27:136 (2014)

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR)...
  15. The role of protein dynamics in GPCR function: insights from the β2AR and rhodopsin.

    Current Opinion in Cell Biology 27:136 (2014) PMID 24534489 PMCID PMC3986065

    G protein-coupled receptors (GPCRs) are versatile signaling proteins that mediate complex cellular responses to hormones and neurotransmitters. Recent advances in GPCR crystallography have provided inactive and active state structures for rhodopsin and the β2 adrenergic receptor (β2AR). Although...
  16. Activation and allosteric modulation of a muscarinic acetylcholine receptor.

    Nature 504(7478):101 (2013) PMID 24256733 PMCID PMC4020789

    Despite recent advances in crystallography and the availability of G-protein-coupled receptor (GPCR) structures, little is known about the mechanism of their activation process, as only the β2 adrenergic receptor (β2AR) and rhodopsin have been crystallized in fully active conformations. Here we ...
  17. Activation and allosteric modulation of a muscarinic acetylcholine receptor.

    Nature 504(7478):101 (2013) PMID 24256733 PMCID PMC4020789

    Despite recent advances in crystallography and the availability of G-protein-coupled receptor (GPCR) structures, little is known about the mechanism of their activation process, as only the β2 adrenergic receptor (β2AR) and rhodopsin have been crystallized in fully active conformations. Here we ...
  18. Applications of molecular replacement to G protein-coupled receptors.

    Acta Crystallographica Section D 69(Pt 11):2287 (2013) PMID 24189241 PMCID PMC3817703

    G protein-coupled receptors (GPCRs) are a large class of integral membrane proteins involved in regulating virtually every aspect of human physiology. Despite their profound importance in human health and disease, structural information regarding GPCRs has been extremely limited until recently. ...
  19. Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody.

    Nature 502(7472):575 (2013) PMID 24056936 PMCID PMC3822040

    G-protein-coupled receptors (GPCRs) are integral membrane proteins that have an essential role in human physiology, yet the molecular processes through which they bind to their endogenous agonists and activate effector proteins remain poorly understood. So far, it has not been possible to captur...
  20. The role of ligands on the equilibria between functional states of a G protein-coupled receptor.

    Journal of the American Chemical Society 135(25):9465 (2013) PMID 23721409 PMCID PMC3763947

    G protein-coupled receptors exhibit a wide variety of signaling behaviors in response to different ligands. When a small label was incorporated on the cytosolic interface of transmembrane helix 6 (Cys-265), (19)F NMR spectra of the β2 adrenergic receptor (β2AR) reconstituted in maltose/neopentyl...