G protein-coupled receptors: structure-and function-based drug discovery
D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
(GPCRs) have experienced a transformation from random ligand screening to knowledge …
Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …
the human genome and are important therapeutic targets. During the last decade, the …
GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures
I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …
physiological processes and thus have long been attractive drug targets. With the crystal …
Smoothened stimulation by membrane sterols drives Hedgehog pathway activity
Hedgehog signalling is fundamental to embryonic development and postnatal tissue
regeneration. Aberrant postnatal Hedgehog signalling leads to several malignancies …
regeneration. Aberrant postnatal Hedgehog signalling leads to several malignancies …
Cholesterol access in cellular membranes controls Hedgehog signaling
Abstract The Hedgehog (Hh) signaling pathway coordinates cell–cell communication in
development and regeneration. Defects in this pathway underlie diseases ranging from birth …
development and regeneration. Defects in this pathway underlie diseases ranging from birth …
Biochemical mechanisms of vertebrate hedgehog signaling
Signaling pathways that mediate cell-cell communication are essential for collective cell
behaviors in multicellular systems. The hedgehog (HH) pathway, first discovered and …
behaviors in multicellular systems. The hedgehog (HH) pathway, first discovered and …
Structural basis of smoothened activation in hedgehog signaling
The seven-transmembrane-spanning protein Smoothened is the central transducer in
Hedgehog signaling, a pathway fundamental in development and in cancer. Smoothened is …
Hedgehog signaling, a pathway fundamental in development and in cancer. Smoothened is …
Fusion protein strategies for cryo-EM study of G protein-coupled receptors
Single particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine
structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or …
structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or …
A bright future for serial femtosecond crystallography with XFELs
X-ray free electron lasers (XFELs) have the potential to revolutionize macromolecular
structural biology due to the unique combination of spatial coherence, extreme peak …
structural biology due to the unique combination of spatial coherence, extreme peak …
Crystal structure of the Frizzled 4 receptor in a ligand-free state
Frizzled receptors (FZDs) are class-F G-protein-coupled receptors (GPCRs) that function in
Wnt signalling and are essential for develo** and adult organisms,. As central mediators …
Wnt signalling and are essential for develo** and adult organisms,. As central mediators …