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The Wnt pathway: from signaling mechanisms to synthetic modulators
The Wnt pathway is central to a host of developmental and disease-related processes. The
remarkable conservation of this intercellular signaling cascade throughout metazoan …
remarkable conservation of this intercellular signaling cascade throughout metazoan …
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 …
GPCR activation mechanisms across classes and macro/microscales
Two-thirds of human hormones and one-third of clinical drugs activate~ 350 G-protein-
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
coupled receptors (GPCR) belonging to four classes: A, B1, C and F. Whereas a model of …
Structural basis of GABA reuptake inhibition
Abstract γ-Aminobutyric acid (GABA) transporter 1 (GAT1) regulates neuronal excitation of
the central nervous system by clearing the synaptic cleft of the inhibitory neurotransmitter …
the central nervous system by clearing the synaptic cleft of the inhibitory neurotransmitter …
A method for structure determination of GPCRs in various states
Q Guo, B He, Y Zhong, H Jiao, Y Ren, Q Wang… - Nature Chemical …, 2024 - nature.com
G-protein-coupled receptors (GPCRs) are a class of integral membrane proteins that detect
environmental cues and trigger cellular responses. Deciphering the functional states of …
environmental cues and trigger cellular responses. Deciphering the functional states of …
Structure determination of inactive-state GPCRs with a universal nanobody
Cryogenic electron microscopy (cryo-EM) has widened the field of structure-based drug
discovery by allowing for routine determination of membrane protein structures previously …
discovery by allowing for routine determination of membrane protein structures previously …
Cryo-EM structure determination of small proteins by nanobody-binding scaffolds (Legobodies)
X Wu, TA Rapoport - Proceedings of the National Academy of Sciences, 2021 - pnas.org
We describe a general method that allows structure determination of small proteins by single-
particle cryo-electron microscopy (cryo-EM). The method is based on the availability of a …
particle cryo-electron microscopy (cryo-EM). The method is based on the availability of a …
[HTML][HTML] New insights into GPCR coupling and dimerisation from cryo-EM structures
Over the past three years (2020–2022) more structures of GPCRs have been determined
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …
than in the previous twenty years (2000–2019), primarily of GPCR complexes that are large …
Structure, function and drug discovery of GPCR signaling
L Cheng, F **a, Z Li, C Shen, Z Yang, H Hou… - Molecular …, 2023 - Springer
G protein-coupled receptors (GPCRs) are versatile and vital proteins involved in a wide
array of physiological processes and responses, such as sensory perception (eg, vision …
array of physiological processes and responses, such as sensory perception (eg, vision …
Understanding the molecular mechanisms of odorant binding and activation of the human OR52 family
Structural and mechanistic studies on human odorant receptors (ORs), key in olfactory
signaling, are challenging because of their low surface expression in heterologous cells …
signaling, are challenging because of their low surface expression in heterologous cells …