International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

Gaussian accelerated molecular dynamics: Principles and applications

J Wang, PR Arantes, A Bhattarai… - Wiley …, 2021 - Wiley Online Library
Gaussian accelerated molecular dynamics (GaMD) is a robust computational method for
simultaneous unconstrained enhanced sampling and free energy calculations of …

[HTML][HTML] Structural insights into the human D1 and D2 dopamine receptor signaling complexes

Y Zhuang, P Xu, C Mao, L Wang, B Krumm, XE Zhou… - Cell, 2021 - cell.com
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …

[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs

A Inoue, F Raimondi, FMN Kadji, G Singh, T Kishi… - Cell, 2019 - cell.com
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …

GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors

S Huang, P Xu, DD Shen, IA Simon, C Mao, Y Tan… - Molecular cell, 2022 - cell.com
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 …

Cryo-EM in drug discovery: achievements, limitations and prospects

JP Renaud, A Chari, C Ciferri, W Liu… - Nature reviews Drug …, 2018 - nature.com
Cryo-electron microscopy (cryo-EM) of non-crystalline single particles is a biophysical
technique that can be used to determine the structure of biological macromolecules and …

Molecular basis of β-arrestin coupling to formoterol-bound β1-adrenoceptor

Y Lee, T Warne, R Nehmé, S Pandey… - Nature, 2020 - nature.com
Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …

Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling

SK Huang, A Pandey, DP Tran, NL Villanueva, A Kitao… - Cell, 2021 - cell.com
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …

Molecular mechanism of biased signaling in a prototypical G-protein-coupled receptor

CM Suomivuori, NR Latorraca, LM Wingler… - Biophysical …, 2020 - cell.com
Over one-third of current drugs target G-protein-coupled receptors (GPCRs). Leveraging the
phenomenon of biased signaling, where different ligands that bind to the same GPCR …

Recognition of methamphetamine and other amines by trace amine receptor TAAR1

H Liu, Y Zheng, Y Wang, Y Wang, X He, P Xu, S Huang… - Nature, 2023 - nature.com
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 …