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 …
GABAkines–Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors
Positive allosteric modulators of γ-aminobutyric acid-A (GABA A) receptors or GABAkines
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …
have been widely used medicines for over 70 years for anxiety, epilepsy, sleep, and other …
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 …
GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors
Summary Serotonin (or 5-hydroxytryptamine, 5-HT) is an important neurotransmitter that
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
activates 12 different G protein-coupled receptors (GPCRs) through selective coupling of G …
Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1
X Yang, X Wang, Z Xu, C Wu, Y Zhou, Y Wang… - Nature Chemical …, 2022 - nature.com
Given the promising clinical value of allosteric modulators of G protein-coupled-receptors
(GPCRs), mechanistic understanding of how these modulators alter GPCR function is of …
(GPCRs), mechanistic understanding of how these modulators alter GPCR function is of …
Structures of the glucocorticoid-bound adhesion receptor GPR97–Go complex
Adhesion G-protein-coupled receptors (GPCRs) are a major family of GPCRs, but limited
knowledge of their ligand regulation or structure is available,–. Here we report that …
knowledge of their ligand regulation or structure is available,–. Here we report that …
Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4
S Lin, S Han, X Cai, Q Tan, K Zhou, D Wang, X Wang… - Nature, 2021 - nature.com
The metabotropic glutamate receptors (mGlus) have key roles in modulating cell excitability
and synaptic transmission in response to glutamate (the main excitatory neurotransmitter in …
and synaptic transmission in response to glutamate (the main excitatory neurotransmitter in …
Membranes under the magnetic lens: a dive into the diverse world of membrane protein structures using Cryo-EM
Membrane proteins are highly diverse in both structure and function and can, therefore,
present different challenges for structure determination. They are biologically important for …
present different challenges for structure determination. They are biologically important for …
Identification and mechanism of G protein-biased ligands for chemokine receptor CCR1
Z Shao, Q Shen, B Yao, C Mao, LN Chen… - Nature chemical …, 2022 - nature.com
Biased signaling of G protein-coupled receptors describes an ability of different ligands that
preferentially activate an alternative downstream signaling pathway. In this work, we …
preferentially activate an alternative downstream signaling pathway. In this work, we …
Molecular mechanisms of metabotropic GABAB receptor function
Metabotropic γ-aminobutyric acid G protein–coupled receptors (GABAB) represent one of
the two main types of inhibitory neurotransmitter receptors in the brain. These receptors act …
the two main types of inhibitory neurotransmitter receptors in the brain. These receptors act …