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 …

[HTML][HTML] Structure of a hallucinogen-activated Gq-coupled 5-HT2A serotonin receptor

K Kim, T Che, O Panova, JF DiBerto, J Lyu, BE Krumm… - Cell, 2020 - cell.com
Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl
phenylalkylamines are widely used recreationally with psilocybin being considered as a …

[HTML][HTML] Crystal structure of an LSD-bound human serotonin receptor

D Wacker, S Wang, JD McCorvy, RM Betz… - Cell, 2017 - cell.com
The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the
crystal structure of LSD in complex with the human serotonin receptor 5-HT 2B. The complex …

Large-scale production and protein engineering of G protein-coupled receptors for structural studies

D Milić, DB Veprintsev - Frontiers in pharmacology, 2015 - frontiersin.org
Structural studies of G protein-coupled receptors (GPCRs) gave insights into molecular
mechanisms of their action and contributed significantly to molecular pharmacology. This is …

Structural basis for allosteric regulation of GPCRs by sodium ions

W Liu, E Chun, AA Thompson, P Chubukov, F Xu… - Science, 2012 - science.org
Pharmacological responses of G protein–coupled receptors (GPCRs) can be fine-tuned by
allosteric modulators. Structural studies of such effects have been limited due to the medium …

Structural features for functional selectivity at serotonin receptors

D Wacker, C Wang, V Katritch, GW Han, XP Huang… - Science, 2013 - science.org
Drugs active at G protein–coupled receptors (GPCRs) can differentially modulate either
canonical or noncanonical signaling pathways via a phenomenon known as functional …

Structure of the human glucagon class B G-protein-coupled receptor

FY Siu, M He, C De Graaf, GW Han, D Yang, Z Zhang… - Nature, 2013 - nature.com
Binding of the glucagon peptide to the glucagon receptor (GCGR) triggers the release of
glucose from the liver during fasting; thus GCGR plays an important role in glucose …

[HTML][HTML] Microscale fluorescent thermal stability assay for membrane proteins

AI Alexandrov, M Mileni, EYT Chien, MA Hanson… - Structure, 2008 - cell.com
Systematic efforts to understand membrane protein stability under a variety of different
solution conditions are not widely available for membrane proteins, mainly due to technical …

Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists

V Katritch, VP Jaakola, JR Lane, J Lin… - Journal of medicinal …, 2010 - ACS Publications
The recent progress in crystallography of G-protein coupled receptors opens an
unprecedented venue for structure-based GPCR drug discovery. To test efficiency of the …

Mechanism of TRIM25 catalytic activation in the antiviral RIG-I pathway

JG Sanchez, JJ Chiang, KMJ Sparrer, SL Alam, M Chi… - Cell reports, 2016 - cell.com
Antiviral response pathways induce interferon by higher-order assembly of signaling
complexes called signalosomes. Assembly of the RIG-I signalosome is regulated by K63 …