[HTML][HTML] 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 …
AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors
As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide
range of physiological processes. Extensive efforts of structural biology have been made on …
range of physiological processes. Extensive efforts of structural biology have been made on …
Molecular recognition of morphine and fentanyl by the human μ-opioid receptor
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
[HTML][HTML] 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 …
GPCR activation and GRK2 assembly by a biased intracellular agonist
J Duan, H Liu, F Zhao, Q Yuan, Y Ji, X Cai, X He, X Li… - Nature, 2023 - nature.com
Phosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs)
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …
desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated …
[HTML][HTML] Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors
Glucose homeostasis, regulated by glucose-dependent insulinotropic polypeptide (GIP),
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
glucagon-like peptide-1 (GLP-1) and glucagon (GCG) is critical to human health. Several …
Structural basis for strychnine activation of human bitter taste receptor TAS2R46
W Xu, L Wu, S Liu, X Liu, X Cao, C Zhou, J Zhang, Y Fu… - Science, 2022 - science.org
Taste sensing is a sophisticated chemosensory process, and bitter taste perception is
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …
mediated by type 2 taste receptors (TAS2Rs), or class TG protein–coupled receptors …
Recognition of methamphetamine and other amines by trace amine receptor TAAR1
Trace amine-associated receptor 1 (TAAR1), the founding member of a nine-member family
of trace amine receptors, is responsible for recognizing a range of biogenic amines in the …
of trace amine receptors, is responsible for recognizing a range of biogenic amines in the …
Molecular basis for selective activation of DREADD-based chemogenetics
Designer receptors exclusively activated by designer drugs (DREADDs) represent a
powerful chemogenetic technology for the remote control of neuronal activity and cellular …
powerful chemogenetic technology for the remote control of neuronal activity and cellular …
Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism
Abstract Sphingosine-1-phosphate receptor 1 (S1PR1) is a master regulator of lymphocyte
egress from the lymph node and an established drug target for multiple sclerosis (MS) …
egress from the lymph node and an established drug target for multiple sclerosis (MS) …